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About Us Selleck Chemicals
Sellecks Bioactive Screening Libraries consist of over 2,500 small molecules with validated biological and pharmacological activities. The safety and effectiveness of these molecules has been demonstrated through preclinical and clinical research, and many of them are FDA-approved compounds.
Selleck Chemicals supplies over 3,000 inhibitors used in the study of cell signaling pathways. We actively tracks the latest science so our customers can rely on us to be the leading supplier of the newest inhibitors.
Selleck is a Licensed Supplier of Pfizer Compounds
All bioactive compounds are licensed by Pfizer and have been marketed and/or have been clinically demonstrated to be safe and efficacious in humans
These compounds span a range of potential uses: from anti-cancer compounds (e.g. Bosutinib) to a glycylcycline antiobiotic (Tigecycline) to combat the growing prevalence of antibiotic resistance
Reliability Guarantee: all Pfizer licensedcompounds are developed, and validated by Pfizer, and some even manufactured by Pfizer
Quality Assurance: all compounds are validated using NMR and HPLC
Detailed preclinical research data and safety information available
In 2013, Selleck became a licensed supplier of Pfizer pharmaceuticals. This has granted our customers access to Pfizers exclusive and high quality compounds. Purchased individually or as a library, these compounds have a wide range of applications in preclinical research of human diseases.
Inhibitors
PI3K/Akt/mTORProtein Tyrosine Kinase
Cell Cycle
EpigeneticsOthers
MAPK
Apoptosis
For Selleck customers located in Boston and Houston, we offer same day rush courier service as an option. For other U.S. based customers, we guarantee that over 90% of orders placed by 2:30 p.m. (U.S. CST) will arrive the next day before 10:30 a.m (U.S. local time). Selleck Chemicals has an established network of sophisticated warehouse systems in Europe, and Asia. No matter where you are located across the globe, if your purchased items are in stock, Selleck will initiate the shipping process within 24 hours.
Quick Delivery:
At Selleck Chemicals, we have a professional expert team dedicated to ensuring our customers are completely satisfied with their purchase. Dont hesitate to contact us by phone or email.Phone: (832) 582-8158 x3 E-mail: [email protected] (We strive to reply to all email inquiries within one business day)
Techical Support:
The quality of our products is strictly monitored and controlled. In the first ten months of 2013, 610 scientific articles referenced Selleck products in their work. Among them, 11 were published in top-notch scientific journals (IF>30):
Quality & Validation:
Our Product Portfolio
Why is Selleck Your Best Choice Compared to Other Suppliers?
top-notch scientific journals (IF>30):
Nature, 2013, 500(7461): 222-6. Nature, 2013, 498(7452): 109-12. Nature, 2013, 501(7466): 237-41. Nature, 2013, 496(7446): 523-7. Nature, 2013, 493(7430): 51-5. Nat Genet, 2013, 45(9): 1013-20. Cell, 2013, 154(5): 1036-46. Cell, 2013, 153(4): 840-54. Science, 2013, 339(6120): 700-4.Nat Biotechnol, 2013, 31(7): 630-7. Nat Biotechnol, 2013, 31(10): 898-907.
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Table of ContentsPI3K
mTOR
Akt
GSK-3
ATM/ATR
PDK-1
S6 Kinase
AMPK (AMP-activated Protein Kinase)
DNA-PK
1
6
9
11
12
13
13
14
14
VEGFR
EGFR
PDGFR
c-Met
HER2
IGF-1R
FLT3 (Fms-like Tyrosine Kinase)
FGFR
c-Kit
ALK (Anaplastic Lymphoma Kinase, CD246)
Tie-2
c-RET
Trk Receptor (Tropomyosin Receptor Kinase Receptor)
Ephrin Receptor
Axl (AXL Receptor Tyrosine Kinase)
CSF-1R (Colony stimulating factor 1 receptor)
15
22
26
28
30
31
32
33
34
35
36
36
36
36
37
37
PI3K/Akt/mTOR
Protein Tyrosine Kinase
VEGFR
JAK
EGFR
PDGFR
HER2
FLT3 (Fms-like Tyrosine Kinase)
FGFR
ALK (Anaplastic Lymphoma Kinase, CD246)
HIF
VDA (Vascular-targeting Agent)
Bcr-Abl
Src
Syk (Spleen Tyrosine Kinase)
FAK
BTK (Bruton's Tyrosine Kinase)
38
38
38
38
38
38
38
38
39
39
39
41
41
42
42
Angiogenesis
c-RET
Bcl-2
Caspase
p53
TNF-alpha
Mdm2
Survivin
IAP (Inhibitor of apoptosis protein)
43
43
45
45
45
46
46
46
Apoptosis
EGFR
JAK
STAT
Pim (Proto-oncogene Serine/threonine-protein Kinase)
47
47
50
50
JAK/STAT
MEK
Raf
p38 MAPK
JNK
ERK
51
54
55
57
57
MAPK
Akt
Bcr-Abl
FAK
Wnt/beta-catenin
PKC
Rac (Ras-related C3 botulinum toxin substrate)
HSP (e.g. HSP90)
Kinesin
Microtubule Associated
PAK (p21 activated kinases)
Dynamin
Integrin
58
58
58
58
59
60
60
62
62
63
63
63
Cytoskeletal Signaling
Rac (Ras-related C3 botulinum toxin substrate)
CDK
Aurora Kinase
Chk
ROCK
PLK
APC
Wee1
c-Myc
64
64
68
71
71
72
73
73
73
Cell Cycle
-
GSK-3
JAK
STAT
TGF-beta/Smad
ROCK
Wnt/beta-catenin
Gamma-secretase
Hedgehog/Smoothened
87
87
87
87
87
87
88
89
Stem Cells and Wnt
Proteasome
DUB
E1 Activating
Autophagy
E2 conjugating
E3 Ligase
91
91
92
92
94
94
Ubiquitin
85
86
DNA Methyltransferase
Histone Methyltransferase
PARP
Pim (Proto-oncogene Serine/threonine-protein Kinase)
Aurora Kinase
JAK
HIF
Sirtuin
HDAC
Histone Demethylases
Histone Acetyltransferase
Epigenetic Reader Domain
82
82
82
82
82
82
82
85
85
85
Epigenetics
Bcr-Abl
PKC
ROCK
TGF-beta/Smad
74
74
74
74
TGF-beta/Smad
HDAC
ATM/ATR
DNA-PK
PARP
DNA/RNA Synthesis
Sirtuin
Topoisomerase
Telomerase
76
76
76
76
78
80
80
81
DNA Damage
Gamma-secretase
Beta Amyloid
5-HT Receptor
COX
GluR
Adrenergic Receptor
AChR
Histamine Receptor
Dopamine Receptor
Opioid Receptor
GABA Receptor
P-gp (Permeability Glycoprotein)
P2 Receptor
OX Receptor (Orexin Receptor)
MT Receptor (Melatonin Receptor)
BACE (Beta-secretase)
95
95
95
96
97
97
98
98
99
99
99
100
100
100
100
100
Neuronal Signaling
HDAC
NF-B
IB/IKK (IB/IB Kinase)
NOD1 (Nucleotide-binding Oligomerization Domain-containing Protein 1)
101
101
101
101
NF-B
104
104
104
Protease-activated Receptor
Vasopressin Receptor
CaSR (Calcium-sensing Receptor)
5-HT Receptor
Adrenergic Receptor
Histamine Receptor
Dopamine Receptor
Opioid Receptor
Hedgehog/Smoothened
OX Receptor (Orexin Receptor)
MT Receptor (Melatonin Receptor)
Cannabinoid Receptor
Endothelin Receptor
S1P Receptor (Sphingosine 1-phosphate Receptor)
SGLT (Sodium-dependent Glucose Cotransporter)
LPA Receptor (Lysophosphatidic Acid Receptor)
CGRP Receptor (Calcitonin Gene-related Peptide Receptor)
PAFR (Platelet-activating Factor Receptor)
cAMP
CXCR
102
102
102
102
102
102
102
102
103
103
103
103
103
104
104
104
104
GPCR & G Protein
-
HCV Protease
HIV Protease
Integrase
Reverse Transcriptase
CCR (C-C Chemokine Receptor)
121
121
121
122
122
Microbiology
Cathepsin K
FXR (Farnesoid X Receptor)
gp120/CD4
IL Receptor
123
123
123
123
Others
123
123
123
123
123
123
Thrombin
TRPV (Transient Receptor Potential Vanilloid)
Liver X Receptor
Phosphorylase
PKA
Substance P
Bioactive Screening Libraries
Customize Your Library
Bioactive Compound Library
Kinase Inhibitor Library
FDA-approved Drug Library
Inhibitor Library
Epigenetics Compound Library
Target Selective Inhibitor Library
Natural Product Library
GPCR Compound Library
Anti-cancer Compound Library
Tyrosine Kinase Inhibitor Library
Stem Cell Signaling Compound Library
Cambridge Cancer Compound Library
Pfizer Licensed Compound Library
Autophagy Compound Library
Ion Channel Ligand Library
PI3K/Akt Inhibitor Library
Apoptosis Compound Library
MAPK Inhibitor Library
Protease Inhibitor Library
Anti-infection Compound Library
Anti-diabetic Compound Library
124
125
125
126
126
127
127
128
128
129
129
130
130
131
131
131
132
132
132
133
133
133
Product Alphabetical Index
Product Catalog Number Index
View More Online
134
143
148
IndicesCaspase
Gamma-secretase
Proteasome
HCV Protease
DPP-4
HIV Protease
MMP (Matrix Metalloproteinase)
118
118
118
119
120
120
120
Proteases
Opioid Receptor
5-alpha Reductase
Estrogen/progestogen Receptor
Androgen Receptor
RAAS
Aromatase
GPR (Glycoprotein Receptor)
105
105
105
106
107
108
108
Endocrinology & Hormones
GABA Receptor
P-gp (Permeability Glycoprotein)
Calcium Channel
Sodium Channel
ATPase
Potassium Channel
Proton Pump
CFTR (Cystic Fibrosis Transmembrane Conductance Regulator)
109
109
109
110
110
110
111
111
Transmembrane Transporters
HSP (e.g.HSP90)
PPAR
P450 (e.g. CYP17)
PDE
Hydroxylase
Factor Xa
DHFR (Dihydrofolate Reductase)
Aminopeptidase
Dehydrogenase
Phospholipase (e.g. PLA)
Carbonic Anhydrase
MAO (Monoamine Oxidase)
FAAH (Fatty Acid Amide Hydrolase)
HMG-CoA Reductase
112
112
113
113
115
115
115
115
115
116
116
116
116
116
Metabolism
Transferase
IDO (Indoleamine-2,3-dioxygenase)
CETP (Cholesteryl Ester Transfer Protein)
Procollagen C Proteinase Bone Morphogenetic Protein 1 (BMP1)
117
117
117
117
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[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORPI3K
CAL-101 is a selective p110 inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110 than p110//, and 400- to 4000-fold more selectivity to p110 than C2, hVPS34, DNA-PK and mTOR. Phase 3.
S2226 CAL-101 (Idelalisib, GS-1101) PI3K p110 selective
Product Citations:Blood, 2012, 120(19): 3978-85Haematologica, 2013, 98(1): 57-64
Data from [ Blood, 2012, 120(19): 3978-85 ]CAL-101 purchased from Selleck
Product Citation:Cancer Cell, 2012, 21(2): 155-67
BKM120 is a selective PI3K inhibitor of p110/// with IC50 of 52 nM/166 nM/116 nM /262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4K. Phase 1/2.
S2247 BKM120 (NVP-BKM120, Buparlisib)
Data from [ Cancer Cell, 2012, 21(2): 155-67 ]BKM120 purchased from Selleck
NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 M.
S2638 NU7441 (KU-57788)
Product Citation:Nucleic Acids Res, 2013, ahead of print
******
******* *
***
+ + + ++++
+lgMCAL-101
% v
iabl
e ce
lls
0
25
50
75
100
ABT-737
GAPDH
S6
pS6
AKT
pAKT (Ser473)DM
SOBE
Z-235
(5uM
)
BEZ-2
35 (1
uM)
BKM-
120 (
5uM)
BKM-
120 (
1uM)
RAD-
001 (
5uM)
RAD-
001 (
1uM)
Cyclo
pami
ne (2
.5uM)
Cyclo
pami
ne (1
uM)
Data independently produced by Dr. Zhang of Tianjin Medical UniversityNU7441 purchased from Selleck
PI-103 is a third multi-targeted PI3K inhibitor, mostly for p110 with IC50 of 2 nM (less potent to p110//), also inhibits mTORC1/2 and DNA-PK with IC50 of 20 nM/83 nM and 8 nM, respectively.
S1038 PI-103
Product Citations:Leukemia, 2013, 27(3): 650-60Leukemia, 2012, 26(5): 927-33
Data from [ J Cell Mol Med, 2013, 17(5): 648-56 ]PI-103 purchased from Selleck
TGX-221 is a p110-specific inhibitor with IC50 of 5 nM, 1000-fold more selective for p110 than p110.
S1169 TGX-221
Product Citations:J Pharmacol Exp Ther, 2012, 341(1): 104-14Mol Med, 2012, 18: 336-45
PI3K p110 selective
Data from [ Mol Med, 2012, 18: 336-45 ]TGX-221 purchased from Selleck
AKT
p-AKT
NU-7441 (uM) EGF+ EGF-0.01 0.1 1.0 1.0
10 mM/1 mL in DMSO 5 mg 200 mg10 mgSize
A66 is a potent and specific p110 inhibitor with IC50 of 32 nM, >100 fold selectivity for p110 over other class-I PI3K isoforms.
S2636 A66
Product Citation:Genes Dev, 2012, 26(14): 1573-86
PI3K p110 selective
Data from [ Genes Dev, 2012, 26(14): 1573-86 ]A66 purchased from Selleck
10 mM/1 mL in DMSO5 mg 100 mg25 mg
Size
GDC-0941 is a potent inhibitor of PI3K/ with IC50 of 3 nM, with modest selectivity against p110 (10-fold) and p110 (25-fold).
S1065 GDC-0941
Product Citations:Cell Stem Cell, 2012, 10(2): 210-7Proc Natl Acad Sci U S A, 2012, 109(31): E2127-33
Data from [ J Cell Sci, 2012, 125(Pt 5): 1259-73 ]GDC-0941 purchased from Selleck
no ATP
no GST-
Akt1
no Ric
tor Ab
TGF- (min)
mTO
RC
2kin
ase
assa
y
Insulin (min)SB431542GDC-0941
pAktS473Akt
RictormTOR
15 30 30 30 30 3030 30
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 100 mg25 mg
Size
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
GDC-0032 is a potent, next-generation isoform-sparing PI3K inhibitor targeting PI3K// with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3K.
S7103 GDC-0032
5 mg 50 mgSize
BYL719 is a potent and selective PI3K inhibitor with IC50 of 5 nM, and minimal effect on PI3K//. Phase 1/2.
S2814 BYL719 PI3K selective
new
N
O
N
NN
NN
N
OH2N
N
O
HN
O
H2N
SN
N
F
FF
Excellent Validation, Technical Support and Prompt Delivery1
PI3KPI
3K/A
kt/mT
OR
BEZ235 (NVP-BEZ235) is a dual ATP- competitive PI3K and mTOR inhibitor for p110/// and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poorly inhibitory to Akt and PDK1. Phase 1/2.
S1009 BEZ235 (NVP-BEZ235)
PI3K/Akt/mTOR Pathway
PI3K Inhibitors
Product Citations:Nature, 2012, 487(7408): 505-9Blood, 2011, 118(14): 3911-21
Data from [ Cancer Res, 2011, 71(15): 5067-74 ]BEZ235 purchased from Selleck
10 mM/1 mL in DMSO100 mg50 mg
Size10 mM/1 mL in DMSO
25 mg 200 mg10 mg
Size
LY294002 is the first synthetic molecule known to inhibit PI3K// with IC50 of 0.5 M /0.57 M/0.97 M, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
S1105 LY294002
Product Citations:Clin Cancer Res, 2011, 17(22): 7116-26Oncogene, 2012, 31(27): 3277-86
Data from [ Oncogene, 2012, 31(27): 3277-86 ]LY294002 purchased from Selleck
contr
ol
Inhibitor: none PI3K(LY294002)MAPK(AZD6244)
pERK
pAKT S473
p110
p37
contr
olp1
10p3
7
contr
olp1
10p3
7
Data from [Cancer Res 2011.August;71:5067-74] BEZ235 purchased from SelleckMEK1/2, rather than B-RAF, targeting in combination with dual PI3K and mTORC1/2 suppression augments apoptosis induction. Live (green) versus dead (orange) cells in PPRM spheroids treated with DMSO, 1 mol/L PLX4032, 1 mol/L AZD6244, 0.1 mol/L BEZ235, or the indicated combinations (dosed every 48 hours) for 6 days.
DMSO PLX4032 AZD6244 BEZ235
PLX4032 +
BEZ235
AZD6244 +
BEZ235
M22
9 R
5M
238
R1
P148
R
PI3K
PI3K
PI3K
PI3K
RTK GPCR Cytokines BCR
Cell Cycle
Apoptosis
Cyclin D1
C-Abl SykRas
PKC
Bcl-2
NF-B
mTOR
ROCK
GSK-3
Wee1Akt
PDK-1
CaspaseMDM2
p53
Bcl-2
Bax
Bim
Foxo3A
eNOS
NO
Cardiovascular Homeostasis
HSP
DNA-PK
Rictor GBL
mTOR
mTOR
DEPTOR
DEPTOR
GBL Raptor
p70S6K S6
Protein Synthesis
Ca2+
mTO
RC
2
mTO
RC
1
PDK-1 inhibitorsBX-912BX-795
OSU-03012PHT-427
BEZ235LY294002GDC-0941
Selective PI3K inhibitorsBYL719(p110)
GSK2636771(p110)TGX-221(p110)
AS-252424(p110)CAL-101(p110)IPI-145(p110)
Pan-PI3K inhibitors
Selective mTOR inhibitors
Pan-mTOR inhibitors
PF-04691502(mTORC1)
AZD8055INK 128
Rapamycin
Everolimus(mTORC1)
Pan-GSK3 inhibitorsCHIR-99021CHIR-98014LY2090314
Selective GSK3 inhibitorsSB 216763(GSK-3)Tideglusib(GSK-3)
TWS119(GSK-3)
CCT128930(Akt2)
Pan-Akt inhibitorsMK-2206
GSK690693GDC-0068
Selective Akt inhibitorsA-674563(Akt1)
Pan-mTOR inhibitorsAZD8055INK 128
Selective mTOR inhibitorsPF-04691502(mTORC1)Everolimus(mTORC1)
Rapamycin
S6 kinase inhibitorsBI-D1870
H 89PF-4708671
FMKAT7867
DNA-PK inhibitorsNU7441PI-103
NU7026PIK-75
-
Excellent Validation, Technical Support and Prompt Delivery3
PI3KPI
3K/A
kt/mT
OR
ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM, mostly PI3K.
S1072 ZSTK474
Product Citation:J Biomol Screen, 2012, 17(8): 1018-29
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of MedicineZSTK474 purchased from Selleck
10 mM/1 mL in DMSO10 mg 50 mg
Size
XL147 (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3K// with IC50 of 39 nM/36 nM/23 nM, less potent to PI3K. Phase 1/2.
S1118 XL147
Product Citation:Autophagy, 2012, 8(6): 903-14
Data independently produced by Dr. Chunrong Yu of RoswelI Park Cancer Institute XL147 purchased from Selleck
10 mg 200 mg50 mgSize
5 mg 100 mg10 mgSize
AS-605240 selectively inhibits PI3K with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3K than PI3K/ and PI3K, respectively.
S1410 AS-605240
Product Citation:PLoS One, 2013, 8(2): e57809
PI3K selective
Data independently produced by Dr. Zhang of Tianjin Medical UniversityAS-605240 purchased from Selleck
PIK-75 is a p110 inhibitor with IC50 of 5.8 nM (200-fold more potently than p110), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.
S1205 PIK-75
Product Citation:Mol Carcinog, 2013, 52(9): 667-75
PI3K p110 selective
10 mg 200 mg25mgSize
Data from [ Mol Carcinog, 2013, 52(9): 667-75 ]PIK-75 purchased from Selleck
10 mM/1 mL in DMSO50 mg 500 mg
Size
3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3K with IC50 of 25 M and 60 M; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.
S2767 3-Methyladenine
Data independently produced by Magorzata Durbas from Jagiellonian University Poland 3-Methyladenine purchased from Selleck
10 mM/1 mL in DMSO5 mg 200 mg10 mg
Size
XL765 is a dual inhibitor of mTOR/PI3K, mostly for p110 with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
S1523 SAR245409 (XL765)
Product Citation:Endocrinology, 2013, 154(3): 1247-59
Data from [ Endocrinology, 2013, 154(3): 1247-59 ]SAR245409 purchased from Selleck
2 mg 50 mg10 mgSize
GSK2126458 is a highly selective and potent inhibitor of p110///, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM, respectively. Phase 1.
S2658 GSK2126458 (GSK458)
Data independently produced by one customerGSK2126458 purchased from Selleck
-actin
Akt
P-Akt
mTOR
P-mTOR
0 0.03 0.1 0.3 1 3GSK2126458 (M)
PIK-75 (M)
BRCA1-siRNAControl-siRNA
00
20
40
60
80
100
120
0.01 0.1 1
% o
f Con
trol
* *
* * * * * *
5 mg 50 mg10 mgSize
IC-87114 is a selective PI3K inhibitor with IC50 of 0.5 M, 58-fold more selective for PI3K than PI3K, and over 100-fold more selective than PI3K/.
S1268 IC-87114
Product Citations:Clin Cancer Res, 2012, 18(21): 5878-87J Inves Der, 2011, 131(2): 495-503
PI3K selective
Data from [ J Inves Der, 2011, 131(2): 495-503 ]IC-87114 purchased from Selleck
IC87114 (mol l-1)0 2.5 7.5 1050
20406080
100120140
Viab
ility
(%)
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORPI3K
10 mg 200 mg50 mgSize
10 mg 50 mgSize
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical CenterPIK-90 purchased from Selleck
Data independently produced by Antonino Maria Spart from University of BolognaGSK1059615 purchased from Selleck
PIK-90 is a PI3K// inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3K.
S1187 PIK-90
Product Citation:J Cell Biol, 2012, 198(2): 185-94
GSK1059615 is a dual inhibitor of PI3K// / (reversible) and mTOR with IC50 of 0.4 nM /0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
S1360 GSK1059615
30 kDa35 kDa
Caspase 7
CTRL
GSK-105
9615
Product Citation:Nature, 2012, 486(7404): 532-36
MIC50 2.678
R square 0.9450
-3
0
20
40
60
80
100
-2 2-1 10
% In
hibi
tion
vs C
TRL
Log[C], (M)
10 mM/1 mL in DMSO5 mg 200 mg10 mg
Size
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPIK-294 purchased from Selleck
PIK-294 is a highly selective p110 inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3K//, respectively.
S2227 PIK-294 PI3K p110 selective
Product Citation:Mol Cell Biol, 2012, 32(12): 2268-78
10 mM/1 mL in DMSO2 mg 100 mg25 mg
Size
Data independently produced by Dr. Zhang of Tianjin Medical UniversityAS-604850 purchased from Selleck
AS-604850 is a selective, ATP-competitive PI3K inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3K than PI3K/, and 18-fold more selective for PI3K than PI3K.
S2681 AS-604850 PI3K selective
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
Data independently produced by Dr. Zhang of Tianjin Medical UniversityCAY10505 purchased from Selleck
CAY10505 is dehydroxyl of AS-252424, which is a PI3K inhibitor with IC50 of 33 nM.
S2682 CAY10505 PI3K selective
5 mg 50 mg10 mgSize
5 mg 200 mg10 mgSize
10 mM/1 mL in DMSO5 mg 200 mg10 mg
Size
10 mM/1 mL in DMSO5 mg 100 mg25 mg
Size
AZD6482 is a PI3K inhibitor with IC50 of 10 nM, 8-, 86- and 109-fold more selective to PI3K than PI3K, PI3K and PI3K. Phase 1.
S1462 AZD6482
Product Citation:Diabetologia, 2013, 56(6): 1339-49
Data independently produced by one customerAZD6482 purchased from Selleck
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPF-05212384 purchased from Selleck
Data independently produced by Dr.Wang Wei from NanFang HospitalGDC-0980 purchased from Selleck
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPIK-93 purchased from Selleck
PKI-587 is a highly potent dual inhibitor of PI3K, PI3K and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.
S2628 PF-05212384 (PKI-587)
GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3K/// with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases. Phase 2.
S2696 GDC-0980 (RG7422)
GDC-0980(M)P-mTOR
0 0.03 0.1 0.3 1 3
mTOR
P-Akt
Akt
-actin
PIK-93 is the first potent, synthetic PI4K (PI4KIII) inhibitor with IC50 of 19 nM; shown to inhibit PI3K with IC50 of 39 nM.
S1489 PIK-93
WM9WM46WM88WM164451LUWM983B1205LUWM1366WM3451WM3692WM3918
Gro
wth
Inhi
bitio
n
10 2 0.4 0.080.0
160.0
32
0.000
64
0.000
128
0.000
0256
0.000
0051
20
0.2
0.4
0.6
0.8
1
1.2 uM AZD6482
PF-04691502 is an ATP-competitive PI3K (///)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
S2743 PF-04691502
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPF-04691502 purchased from Selleck
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
PF-04691502(M)P-Akt
0.01 0.1 1.0 10EGF+ EGF-
Akt
Licensed by Pfizer
Product Citation:J Pharmacol Exp Ther, 2013, ahead of print
-
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORPI3K / mTOR
PI-103
GDC-0941
ZSTK474
LY294002
XL147
TGX-221
PIK-90
PIK-75
TG100-115
GSK1059615
AS-605240
AZD6482
PIK-93
XL765
PIK-293
CAL-101
PIK-294
BKM120
PF-05212384
A66
NU7441
AS-252424
AS-604850
CAY10505
GDC-0980
CH5132799
PKI-402
PF-04691502
3-Methyladenine
BAY80-6946
TG 100713
IPI-145
GSK2636771
S1038
S1065
S1072
S1105
S1118
S1169
S1187
S1205
S1352
S1360
S1410
S1462
S1489
S1523
S2207
S2226
S2227
S2247
S2628
S2636
S2638
S2671
S2681
S2682
S2696
S2699
S2739
S2743
S2767
S2802
S2870
S7028
S8002
+++
+++
++
+++
++
++
+++
++++
+
+
++++
++
+
+++
++++
++
++
+
++
+++
+++
+++
+++
+++
++++
+
8 nM [IC50]
3 nM [IC50]
16 nM [IC50]
0.5 M [IC50]
39 nM [IC50]
11 nM [IC50]
5.8 nM [IC50]
0.4 nM [IC50]
60 nM [IC50]
1.4 M [IC50]
39 nM [IC50]
39 nM [IC50]
100 M [IC50]
52-99 nM [IC50]
0.4 nM [IC50]
32 nM [IC50]
5 M [IC50]
935 nM [IC50]
4.5 M [IC50]
0.94 M [IC50]
5 nM [IC50]
14 nM [IC50]
2 nM [IC50]
1.8 nM [Ki]
0.469 nM [IC50]
165 nM [IC50]
+
++
++
+++
+
+++
+
++++
+
++
+
+
+
+
++
+
+
++
++
+++
+++
+++
+
+
88 nM [IC50]
33 nM [IC50]
44 nM [IC50]
0.97 M [IC50]
383 nM [IC50]
8.5 nM [IC50]
350 nM [IC50]
0.6 nM [IC50]
270 nM [IC50]
21 nM [IC50]
0.59 M [IC50]
113 nM [IC50]
25 M [IC50]
490 nM [IC50]
166 nM [IC50]
>20 M [IC50]
20 M [IC50]
27 nM [IC50]
0.12 M [IC50]
7 nM [IC50]
2.1 nM [Ki]
3.72 nM [IC50]
215 nM [IC50]
61 nM [IC50]
++
+++
++
+++
++
+
+
+++
+
+
+
++
+++
+++
+++
++
+
+
+++
++
++
+++
++
++++
48 nM [IC50]
3 nM [IC50]
4.6 nM [IC50]
0.57 M [IC50]
36 nM [IC50]
58 nM [IC50]
235 nM [IC50]
2 nM [IC50]
300 nM [IC50]
80 nM [IC50]
0.12 M [IC50]
43 nM [IC50]
0.24 M [IC50]
2.5 nM [IC50]
10 nM [IC50]
116 nM [IC50]
>20 M [IC50]
20 M [IC50]
7 nM [IC50]
0.5 M [IC50]
14 nM [IC50]
1.6 nM [Ki]
24 nM [IC50]
1 nM [IC50]
+
+
++
++
++
+
+++
+++
+
++++
+++
++
+
+
+++
+++
++++
+
++
+++
++
+++
+
++
++
105 nM [IC50]
75 nM [IC50]
49 nM [IC50]
33 nM [IC50]
18 nM [IC50]
83 nM [IC50]
5 nM [IC50]
8 nM [IC50]
1.2 M [IC50]
16 nM [IC50]
9 nM [IC50]
10 M [IC50]
160 nM [IC50]
262 nM [IC50]
5.4 nM [IC50]
33 nM [IC50]
250 nM [IC50]
30 M [IC50]
14 nM [IC50]
36 nM [IC50]
16 nM [IC50]
1.9 nM [Ki]
60 M [IC50]
50 nM [IC50]
50 nM [IC50]
+ 25 M [IC50]
Inhibitory Selectivityp110 p110 p110 p110 Vps34-likeCat.No. Inhibitor Name
Product Citations:Cancer Cell, 2012, 21(2): 155-67Clin Cancer Res, 2013, 19(3): 598-609
Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.
S1120 Everolimus (RAD001)
Data from [ Cancer Cell, 2012, 21(2): 155-67 ]Everolimus purchased from Selleck
10 mM/1 mL in DMSO100 mg25 mg
Size
GAPDH
S6
pS6
AKT
pAKT (Ser473)DM
SOBE
Z-235
(5uM
)
BEZ-2
35 (1
uM)
BKM-
120 (
5uM)
BKM-
120 (
1uM)
RAD-
001 (
5uM)
RAD-
001 (
1uM)
Cyclo
pami
ne (2
.5uM)
Cyclo
pami
ne (1
uM)
mTOR Inhibitors
Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM.
S1039 Rapamycin (Sirolimus, AY22989, NSC226080)
Product Citations:Cancer Cell, 2011, 19(6): 792-804Cell Res, 2012, 22(6): 1003-21
10 mM/1 mL in DMSO100 mg5 mg
Size
Data from [ Cancer Cell, 2011, 19(6): 792-804 ]Rapamycin purchased from Selleck
Licensed by Pfizer
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
Excellent Validation, Technical Support and Prompt Delivery5
PI3KPI3
K/Akt/
mTOR
BAY 80-6946 is a potent and highly selective reversible PI3K inhibitor for PI3K/ with IC50 of 0.469 nM/3.72 nM. Phase 1.
S2802 BAY80-6946
10 mM/1 mL in DMSO
5 mg 200 mg50 mgSize10 mM/1 mL in DMSO
5 mg 200 mg50 mgSize10 mM/1 mL in DMSO
5 mg10 mM/1 mL in DMSO 50 mg25 mgSize
5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
TG100-115 is a PI3K/ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3K/. Phase 1/2.
S1352 TG100-115
YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110 and insensitive to Fabl (yeast orthologue).
S1219 YM201636
CH5132799 inhibits class I PI3Ks, particularly PI3K with IC50 of 14 nM; less potent to PI3K//, while sensitive in PIK3CA mutations cell lines. Phase 1.
S2699 CH5132799 PI3K selective
NVP-BGT226 is a novel class I PI3K/mTOR inhibitor for PI3K// with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
S2749 NVP-BGT226 (BGT226)
CUDC-907 is a dual PI3K and HDAC inhibitor for PI3K and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.
S2759 CUDC-907 PI3K selective
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPIK-293 purchased from Selleck
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
PI3K selective
PIK-293 is a PI3K inhibitor, mostly for PI3K with IC50 of 0.24 M, 500-, 100- and 50-fold less potent to PI3K//, respectively.
S2207 PIK-293
HN
NN
N
O
O
N
O
O
NN
NH2
5 mg10 mM/1 mL in DMSO 20 mg10 mgSize
10 mg10 mM/1 mL in DMSO 200 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg10 mgSize
Data independently produced by Dr. Zhang of Tianjin Medical UniversityAS-252424 purchased from Selleck
10 mM/1 mL in DMSO2 mg 100 mg25 mg
Size
PI3K selective
AS-252424 is a novel, potent PI3K inhibitor with IC50 of 30 nM with 30-fold selectivity for PI3K than PI3K, and low inhibitory activity towards PI3K/.
S2671 AS-252424
10 mg 200 mgSize
TG 100713 is a pan-PI3K inhibitor against PI3K, PI3K, PI3K and PI3K with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
S2870 TG 100713
IPI-145 (INK1197) is a novel and selective PI3K / inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM, highly selective PI3K / than other protein kinases. Phase 2.
S7028 IPI-145 (INK1197)
GSK2636771 is a potent, orally bioavailable, PI3K-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
S8002 GSK2636771 PI3K selective
5 mg 200 mg50 mgSize
PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3K/// and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3K mutants E545K and H1047R.
S2739 PKI-402
Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K inhibitors, but little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM. Phase 4.
S2758 Wortmannin
Product Citation:J Cell Sci, 2013, 126(Pt 3): 715-21
N
NN
N
NH2
H2N
OH
N
N
FF
F
N
O OH
O
N
Cl O
NHN
N
HNN
-
Excellent Validation, Technical Support and Prompt Delivery7
mTORPI
3K/A
kt/mT
OR
10 mg 50 mg25 mgSize
AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (~1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.
S1555 AZD8055
Data from [ Autophagy, 2013, 9(1): 74-92 ]AZD8055 purchased from Selleck
Product Citations:Autophagy, 2013, 9(1): 74-92Biochem Pharmacol, 2012, 83(9): 1183-94
INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
S2811 INK 128
10 mM/1 mL in DMSO10 mg 50 mg
Size
Product Citation:Autophagy, 2012, 8(6): 903-14
Data from [ Autophagy, 2012, 8(6): 903-14]PP242 purchased from Selleck
PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3K or PI3K//, respectively.
S2218 PP242
Data independently produced by one customerINK 128 purchased from Selleck
30 kDa35 kDa
Caspase 7
CTRL
INK-12
8
MIC50 1.868
R square 0.9637
Log[C], (M)
S1009 BEZ235 (NVP-BEZ235)
BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110/// and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poorly inhibitory to Akt and PDK1. Phase 1/2.
S1038 PI-103PI-103 is a third multi-targeted PI3K inhibitor, mostly for p110 with IC50 of 2 nM (less potent to p110//), also inhibits mTORC1/2 and DNA-PK with IC50 of 20 nM/83 nM and 8 nM, respectively.
10 mM/1 mL in DMSO5 mg 100 mg10 mg
Size
10 mM/1 mL in DMSO10 mg 50 mg
Size
Page 2
Page 1
N
N NN
NH2
NO NH2
Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM; exhibits 1000-fold selectivity for mTOR than PI3K.
S2827 Torin 1
GSK2126458 is a highly selective and potent inhibitor of p110///, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM, respectively. Phase 1.
Product Citation:Mol Genet Meta, 2010, 100(4): 309-15
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 100 mg50 mg
Size
Data from [ Mol Genet Meta, 2010, 100(4): 309-15 ]Ridaforolimus purchased from Selleck
Deforolimus (Ridaforolimus MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin.
S1022 Ridaforolimus (Deforolimus)
Data from [ Tuberc Respir Dis (Seoul), 2012, 72(4): 343-51 ]Temsirolimus purchased from Selleck
Temsirolimus (CCI-779, Torisel) is a specific mTOR inhibitor with IC50 of 1.76 M.
S1044 Temsirolimus (CCI-779, NSC-683864)
Product Citations:Autophagy, 2011, 7(2): 176-87Tuberc Respir Dis (Seoul), 2012, 72(4): 343-51
Control GSK690693
A549Temsirolimus GSK690693+Temsirolimus
Product Citations:Cell Stem Cell, 2012, 10(2): 210-7Circ Res, 2010, 107(10): 1265-74
Data from [ Circ Res, 2010, 107(10): 1265-74]Ku-0063794 purchased from Selleck
KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM; no effect on PI3Ks.
S1226 Ku-0063794
S2658 GSK2126458 (GSK458)
Page 3
Page 3
S1523 SAR245409 (XL765)XL765 is a dual inhibitor of mTOR/PI3K, mostly for p110 with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
N
N
ON
FFF
NN
O
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORmTOR
10 mM/1 mL in DMSO 5 mg 50 mg10 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
PF-04691502 is an ATP-competitive PI3K(///)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
S2743 PF-04691502 mTORC1 selective
PKI-587 is a highly potent dual inhibitor of PI3K, PI3K and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.
S2628 PF-05212384 (PKI-587)
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
Product Citation:Exp Eye Res, 2013, 113C: 9-18
Data from [ Exp Eye Res, 2013, 113C: 9-18 ]OSI-027 purchased from Selleck
OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3K, PI3K, PI3K or DNA-PK.
S2624 OSI-027
WYE-125132 is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
S2661 WYE-125132 (WYE-132)
WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3K (>100-fold) and PI3K (>500-fold).
S2668 WYE-687
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively.
S2817 Torin 2
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPalomid 529 purchased from Selleck
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
Palomid 529 inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3S9, and pS6 but no effect observed on pMAPK or pAktT308. Phase 1.
S2238 Palomid 529 (P529)
S2696 GDC-0980 (RG7422)
AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms (///). Phase 2.
S2783 AZD2014
10 mM/1 mL in DMSO5 mg 200 mg10 mg
Size
Data independently produced by Dr. Milica Pesic from Institute for Biological ResearchAZD2014 purchased from Selleck
WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3K (>100-fold) and PI3K (>500-fold).
S1266 WYE-354
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
Data from [ Mol Cancer Res, 2012, 10(6): 821-33 ]WYE-354 purchased from Selleck
Product Citation:Mol Cancer Res, 2012, 10(6): 821-33
GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3K/// with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases. Phase 2.
Page 4
Page 4
Page 4
GSK1059615 is a dual inhibitor of PI3K/// (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
S1360 GSK1059615
Page 4
CH5132799 inhibits class I PI3Ks, particularly PI3K with IC50 of 14 nM; less potent to PI3K//, while sensitive in PIK3CA mutations cell lines. Phase 1.
S2699 CH5132799
Page 5
5 mg 200 mg50 mgSize
N N
N
NO
NH
O
N
O
N
N
O
FFF
NH2N
-
Excellent Validation, Technical Support and Prompt Delivery9
mTOR / AktPI
3K/A
kt/mT
OR
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 5 mg 50 mgSize
Data from [ J Clin Invest, 2011, 121(9): 3623-34 ]MK-2206 2HCl purchased from Selleck
Product Citations:J Clin Invest, 2011, 121(9): 3623-34Mol Cell, 2012, 47(3): 422-33
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.
S1078 MK-2206 2HCl
Akt Inhibitors
10 mM/1 mL in DMSO50 mg5 mg
Size
PI-103
Ku-0063794
OSI-027
Torin 1
S1038
S1226
S2624
S2827
++
+++
++
+++
20 nM [IC50]
10 nM [IC50]
22 nM [IC50]
0.29-2 nM [IC50]
+
+++
+
+++
83 nM [IC50]
10 nM [IC50]
65 nM [IC50]
0.29-2 nM [IC50]
p110,DNA-PK,p110,p110,p110
Inhibitory SelectivityCat.No. Inhibitor Name mTORC1 mTORC2 Other
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPP-121 purchased from Selleck
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
S2622 PP-121
NVP-BGT226 is a novel class I PI3K/mTOR inhibitor for PI3K// with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
S2749 NVP-BGT226 (BGT226)
Page 5
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORAkt
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 10 mg 100 mg50 mgSize
GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM /18 nM/8 nM, 620-fold selectivity over PKA. Phase 2.
S2808 GDC-0068
Product Citations:Mol Cancer Ther, 2012, 11(7): 1510-17J Biol Chem, 2013, 286(43): 37389-98
Data from [ Mol Cancer Ther, 2012, 11(7): 1510-17 ]GSK690693 purchased from Selleck
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also selective for Akt as compared to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
S1113 GSK690693
Data independently produced by Lee lay hoon from National University of SingaporeA-674563 purchased from Selleck
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
S2670 A-674563
controlH
3 Inc
orpo
ratio
nR848 akti
50nM
TLR7 induced cell proliferation isdependent on AKT
100nM 1uM 10uM 50uM500nMakti akti akti akti akti
0
2000
4000
6000
8000
10000
12000
Triciribine phosphate (TCN-P, NSC-280594, API-2), the active metabolite of TCN, is a potent Akt inhibitor with IC50 of 130 nM, that inhibits the phosphorylation of Akt in intact cells but not in vitro, more active in cells lacking adenosine kinase. Phase 1/2.
S2732 Triciribine phosphate
S2743 PF-04691502PF-04691502 is an ATP-competitive PI3K(///)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
Page 4
5 mg 100 mg50 mgSize
50 mg 500 mg100 mgSize
50 mg 200 mg50 mgSize
N
N
O
NH
Cl
N
N
HO
Product Citations:Cancer Research, 2012, 72(5): 1229-38PLoS One, 2013, 8(2): e57508
Data from [ PLoS One, 2013, 8(2): e57508 ]AT7867 purchased from Selleck
AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.
S1558 AT7867
Input
pAktS473
FLAG
HA
HA
FLAGIP: FLAG
FKBP51TPR_mut_FLAGHA_Akt1
inhibi
tor V
III
AT78
67
DMSO
+ + + + + ++ + + + + +
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 100 mg50 mg
Size
NH
HN N
Cl
Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 M and 8.1 M in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
S3056 Miltefosine
N+
OPOO-
O
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
Product Citation:Blood, 2011, 118(10): 2840-8
Data from [ Blood, 2011, 118(10): 2840-8 ]PHT-427 purchased from Selleck
PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 M and 5.2 M, respectively.
S1556 PHT-427
Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.
S2310 Honokiol
Triciribine (TCN, API-2) is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
S1117 Triciribine
CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
S2635 CCT128930 Akt2 selective
WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3K (>100-fold) and PI3K (>500-fold).
S2689 WAY-600
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3K and other 266 kinases. Phase 1.
S8040 GDC-0349
HN O
NH
N
NN
O
N
O
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Data from [ PLoS Biol, 2011, 9(9): e1001148 ]Perifosine purchased from Selleck
Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 M, targets pleckstrin homology domain of Akt. Phase 2.
S1037 Perifosine (KRX-0401)
Product Citations:Cell, 2012, 149(3): 656-70PLoS Biol, 2011, 9(9): e1001148
-
Excellent Validation, Technical Support and Prompt Delivery11
Akt / GSK-3PI
3K/A
kt/mT
OR
GSK690693
AT7867
CCT128930
A-674563
GDC-0068
AZD5363
S1113
S1558
S2635
S2670
S2808
S8019
+++
++
+++
+++
+++
2 nM [IC50]
32 nM [IC50]
11 nM [Ki]
5 nM [IC50]
3 nM [IC50]
++
++
+++
++
+++
13 nM [IC50]
17 nM [IC50]
6 nM [IC50]
18 nM [IC50]
8 nM [IC50]
+++
++
+++
+++
9 nM [IC50]
47 nM [IC50]
8 nM [IC50]
8 nM [IC50]
S6K1
PKA
PKA,Cdk2
Inhibitory SelectivityCat.No. Inhibitor Name AKT1 AKT2 AKT3 Other
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
5 mg 25 mgSize
50 mg 200 mgSize
TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics.
S7127 TIC10 new
N
N
N
N
O AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 1/2.
S8019 AZD5363
N
ONH
N
N
NH
Cl NH2
OH
10 mM/1 mL in DMSO 5 mg 25 mgSize
Product Citations:Nat Protoc, 2012, 8(1): 162-75Proc Natl Acad Sci U S A, 2012, 109(27): E1848-57
Data from [ Carcinogenesis, 2012, 33(3): 529-37 ]CHIR-99021 HCl purchased from Selleck
CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3/ inhibitor with IC50 of 10 nM/6.7 nM; ability to distinguish between GSK-3 and its closest homologs Cdc2 and ERK2.
S2924 CHIR-99021 (CT99021) HCl
GSK-3 Inhibitors
10 mM/1 mL in DMSO100 mg2 mg
Size
SB 216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM; low inhibitory effect exhibited on GSK-3.
S1075 SB 216763 GSK-3 selective
N
NHNN
H
NN
HN
N
ClCl
HCl
TWS119 is a GSK-3 inhibitor with IC50 of 30 nM; capable of inducing neuronal differentiation and may be useful to stem cell biology.
S1590 TWS119 GSK-3 selective
10 mM/1 mL in DMSO 10 mg 50 mg25 mgSize
new
Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3 inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 1/2.
S2823 Tideglusib GSK-3 selective
SN
N
O
O
SB 415286 is a potent GSK3 inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3.
S2729 SB 415286
10 mM/1 mL in DMSO25 mg5 mg
Size
Product Citation:Stem Cells Dev, 2013, 22(13): 1893-906
Data from [ Stem Cells Dev, 2013, 22(13): 1893-906 ]CHIR-98014 purchased from Selleck
CHIR-98014 is a potent GSK-3/ inhibitor with IC50 of 0.65 nM/0.58 nM, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
S2745 CHIR-98014
Beta-catenin expression in hESCs(20X magnification)
no GSKicontrol
CHIR99021
CHIR98014
10 mM/1 mL in DMSO 5 mg 100 mg10 mgSize
10 mM/1 mL in DMSO 10 mg 10 mgSize
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORGSK-3 / ATM/ATR
SB 216763
TWS119
SB 415286
CHIR-98014
Tideglusib
CHIR-99021 HCl
TDZD-8
LY2090314
S1075
S1590
S2729
S2745
S2823
S2924
S2926
S7063
++
+
++++
+++
+++
34.3 nM [IC50]
78 nM [IC50]
0.65 nM [IC50]
10 nM [IC50]
1.5 nM [IC50]
++
+
++++
+
+++
++
++++
30 nM [IC50]
~78 nM [IC50]
0.58 nM [IC50]
60 nM [IC50]
6.7 nM [IC50]
2 M [IC50]
0.9 nM [IC50]
Inhibitory SelectivityCat.No. Inhibitor Name GSK-3 GSK-3
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
5 mg 50 mgSize
LY2090314 is a potent GSK-3 inhibitor for GSK-3/ with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2.
S7063 LY2090314 new
N
N
N
O
NH
O
O
N
N
TDZD-8 is a non-ATP competitive GSK-3 inhibitor with IC50 of 2 M; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
S2926 TDZD-8 GSK-3 selective
SN N
O
O
KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM, 270- and 1,600-fold selective for ATM than DNA-PK and ATR, a highly effective radiosensitizer.
S1570 KU-60019
Product Citation:Brain Pathol, 2012, 22(5): 677-88
Product Citations:Autophagy, 2012, 8(2): 236-51Sci Signal, 2013, 6(259): ra5
Data from [ Autophagy, 2012, 8(2): 236-51 ]KU-55933 purchased from Selleck
KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM, highly selective to DNA-PK, PI3K/PI4K, ATR and mTOR.
S1092 KU-55933
ATM/ATR Inhibitors
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
25 mg
VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3K.
S8007 VE-821
Product Citations:PLoS One, 2012, 7(11): e50423J Neurooncol, 2012, 110(3): 349-57
2 mg 5 mgSize
Data from [ PLoS One, 2012, 7(11): e50423 ]CP-466722 purchased from Selleck
CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibit PI3K or PIKK family members in cells.
S2245 CP-466722
N
N
O
NH SO
O
H2N
10 mM/1 mL in DMSO 10 mg 50 mgSize
10 mM/1 mL in DMSO 10 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 10 mg 50 mg25 mgSize
S
O
ONH
NO
NO
O
-
Excellent Validation, Technical Support and Prompt Delivery13
ATM/ATR / PDK-1 / S6 KinasePI
3K/A
kt/mT
OR
Inhibitory Selectivity
KU-55933
KU-60019
Wortmannin
VE-821
S1092
S1570
S2758
S8007
++
++
1.8 M [IC50]
13 nM [Ki]
+++
+++
2.2 nM [Ki]
6.3 nM [IC50]DNA-PK
Cat.No. Inhibitor Name ATR ATM Other
S2758 Wortmannin
Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K inhibitors, but little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM. Phase 4.
S1009 BEZ235 (NVP-BEZ235)
BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110/// and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poorly inhibitory to Akt and PDK1. Phase 1/2.
Page 1
Page 5
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
10 mg 50 mgSize
10 mg 50 mgSize
10 mg 50 mgSize
KU59403 is a novel ATM inhibitor with IC50 of 3 nM.
S7166 KU59403 new
S2817 Torin 2
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM, respectively.
Page 8
SS O N
O
O
NH
O
NN
CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
S7136 CGK 733 new
FNO2
HN
HN
S
CCl3
HN O
Product Citations:Am J Physiol Renal Physiol, 2011, 302(4): F466-76Eukaryot Cell, 2012, 12(1): 12-22
10 mM/1 mL in DMSO5 mg 100 mg25 mg
Size
Data from [ Am J Physiol Renal Physiol, 2011, 302(4): F466-76 ]OSU-03012 purchased from Selleck
OSU-03012 is a potent inhibitor of recombinant PDK-1 with IC50 of 5 M and 2-fold increase in potency over OSU-02067.
S1106 OSU-03012 (AR-12)
BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3, MARK3, CK1 and Aurora B.
S2843 BI-D1870
S6 Kinase Inhibitors
HO
F
F
NH
N
N
N
N O
10 mM/1 mL in DMSO 5 mg 50 mg10 mgSize
BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PKD1 than PKA and PKC, respectively. In comparison to GSK3, selectivity for PDK1 is 600-fold.
S1275 BX-912
PDK-1 Inhibitors
BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC, respectively. Meanwhile, in comparison to GSK3 more than 100-fold selectivity observed for PDK1.
S1274 BX-795
S1556 PHT-427
PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 M and 5.2 M, respectively.
GSK2334470 is a potent and highly selective PDK1 inhibitor with IC50 of ~10 nM.
S7087 GSK2334470 new
N N
N
HN
NH
N
NH2
O
NH
Page 10
10 mM/1 mL in DMSO 10 mg 100 mg50 mgSize
10 mM/1 mL in DMSO 2 mg 100 mg50 mgSize
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
PI3K/Akt/mTORS6 Kinase / AMPK / DNA-PK
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinase RSK2 (wt) with IC50 of 15 nM, > 600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants.
S7064 FMK
AT7867
BI-D1870
PF-4708671
S1558
S2843
S2163
++
++
17 nM [IC50]
20 nM [Ki]++ 31 nM [IC50] ++ 24 nM [IC50] ++ 18 nM [IC50] ++ 15 nM [IC50]
Inhibitory SelectivityCat.No. Inhibitor Name S6K1 RSK1 RSK2 RSK3 RSK4 Other
AKT3,AKT2,AKT1
S1558 AT7867AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.
Page 10
Notes: 1."+" indicates inhibitory effect. The more "+" are, the stronger inhibition is. 2.Black "+" corresponds to IC50 or Ki values in nMs, gray "+" refers to values in Ms.
50 mg 200 mgSize
N
N
N
NH2
O F
HO
S1038 PI-103
PI-103 is a third multi-targeted PI3K inhibitor, mostly for p110 with IC50 of 2 nM (less potent to p110//), also inhibits mTORC1/2 and DNA-PK with IC50 of 20 nM/83 nM and 8 nM, respectively.
NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 M, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.
S2893 NU7026
S1205 PIK-75
PIK-75 is a p110 inhibitor with IC50 of 5.8 nM (200-fold more potently than p110), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.
S2622 PP-121
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
DNA-PK Inhibitors
S2638 NU7441 (KU-57788)
NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 M.
Page 2
Page 2
Page 3
Page 9
O
N
O
O
PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.
S2163 PF-4708671 Licensed and Manufactured by Pfizer
HN
N
N
N
N
N
FF
F
10 mM/1 mL in DMSO 5 mg 50 mg10 mgSize
Acadesine results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPKK. Phase 3.
S1802 Acadesine
Phenformin hydrochloride is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class.
S2542 Phenformin HCl
Product Citation:Biochem Biophys Res Commun, 2013, ahead of print
AMPK Activators
A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 M, little effect on GPPase/FBPase activity.
S2697 A-769662
NH
NH
NH
NH NH2 HCl
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 50 mgSize
5 mg 100 mg25 mgSize
5 mg 200 mg50 mgSize
-
VEGFRPr
otein
Tyros
ine K
inase
Protein Tyrosine Kinase
Excellent Validation, Technical Support and Prompt Delivery15
Product Citations:Nature, 2011, 478(7369): 349-55Cell Death Differ, 2010, 17(9): 1381-91
Data from [ Mol Cancer Ther, 2011, 11(3): 690-9 ]Nintedanib purchased from Selleck
BIBF1120 (Vargatef) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFR/ with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.
S1010 Nintedanib (BIBF 1120)
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Product Citation:Surgery, 2012, 152(6): 1238-47
Data from [ Surgery, 2012, 152(6): 1238-47 ]XL-184 purchased from Selleck
XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
S1119 XL-184 (Cabozantinib, BMS907351) VEGFR2 selective
VEGFR Inhibitors
Phospho-RET(Tyr905)
Phospho-mTOR(Ser2448)
Phospho-4E-BP1(Thr37/46)
Phospho-p706S kinase
Phospho-ERK1/2(Thr42/Tyr44)ERK1/2
actin
Phospho-Akt(Ser473)Akt
RET
XL184[M]12h 24h
0 0.5 1 3 6 0 0.5 1 3 6
mTOR
4E-BP1
P70 S6 kinase
10 mM/1 mL in DMSO5 mg 200 mg10 mg
Size
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
Protein Tyrosine KinaseVEGFR
Product Citations:Cancer Res, 2011, 71(5): 1637-46Dis Model Mech, 2010, 3(5-6): 343-53
Data from [ Dis Model Mech, 2010, 3(5-6): 343-53 ]Sunitinib Malate purchased from Selleck
Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFR with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
S1042 Sunitinib Malate VEGFR2 selective
0.1% DMSO
sibl
ing
vhl-/
-
10M 676475 0.2M sunitinib
VEGFR2 selective
Product Citations:Cancer Cell, 2012, 22(5): 656-67Exp Hematol, 2013, 41(4): 335-45
Data from [ Cancer Cell, 2012, 22(5): 656-67 ]Ponatinib purchased from Selleck
AP24534 is a novel, potent multi-target inhibitor of Abl, PDGFR, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
S1490 Ponatinib (AP24534)
VEGFR2 selective
Product Citations:Blood, 2012, 120(19): 4104-15Cell Death Differ, 2012, 19(12): 2029-39Clin Cancer Res, 2011, 17(24): 7595-604
Data from [ Haematologica, 2012, 97(11): 1722-30 ]Sorafenib purchased from Selleck
Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
S1040 Sorafenib
10 mM/1 mL in DMSO100 mg5 mg
Size
Licensed by Pfizer
10 mM/1 mL in DMSO50 mg 500 mg100 mg
Size
Product Citations:Hypertension, 2011, 58(1): 85-92Antivir Res, 2010, 89(1): 64-70
Data from [ Hypertension, 2011, 58(1): 85-92 ]Vandetanib purchased from Selleck
Vandetanib (Zactima, ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
S1046 Vandetanib (ZD6474)
Product Citations:Cancer Discov, 2013, 3(6): 636-47J Virol, 2011, 85(5): 2296-303
Data from [ Cancer Discov, 2013, 3(6): 636-47 ]Pazopanib HCl purchased from Selleck
Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
S1035 Pazopanib HCl (GW786034 HCl)
Product Citations:Cancer Discov, 2012, 2(4): 344-55Glia, 2012, 60(6): 936-47
Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
S1005 Axitinib
Data from [ Cancer Discov, 2012, 2(4): 344-55 ]Axitinib purchased from Selleck
Licensed by Pfizer
10 mM/1 mL in DMSO50 mg 100 mg
Size
10 mM/1 mL in DMSO10 mg 100 mg25 mg
Size
10 mM/1 mL in DMSO25 mg 500 mg100 mg
Size
10 mM/1 mL in DMSO10 mg 200 mg50 mg
Size
E
E
E
E
L
L
C
C
C C
C
C
C
C
C CC
F
F
FF F F F
F
F
F
FFF
FF
F
F
A
A
F
KinaseFibronectinCysteine RichLeucine Rich
EGF-LikeAcid boxCadherin
IG-LikeGlycine Rich
EGFR
HER2/ErbB2ErbB3ErbB4
INSRIGF-1R
IRR
FGFR PDGFRCSF1R
KitFlk2
VEGFR Met
RonSea
TrkATrkBTrkC
TieTie2
EphEckEekErkElk
Ros Ret LtkAlk
PLC
PDK-1
Akt
PKC
IKK
Syk Bcr-Abl
Ras
Raf
c-Src
GSK-3
c-Jun c-Fos
JAK ROCK
RhoPAK
JAK
STATPI3K/AktPathway
NF-BPathway
MAPKPathway
Cell-Cycle
JAK/STATPathway
HER2 inhibitors Pan-FGFR inhibitorsPan-PDGFR inhibitors Pan-VEGFR inhibitors
Pan-Trk receptor inhibitor c-RET inhibitors
ALK inhibitorsTie-2 inhibitors
c-Met inhibitorsc-Kit inhibitorsIGF-1R inhibitorsPan-ErbB inhibitors
Selective ErbB inhibitors
Selective Trk receptor inhibitorSelective VEGFR inhibitorsSelective PDGFR inhibitors
Lapatinib Ditosylate
AfatinibAG-490
Lapatinib
Erlotinib(ErbB1/EGFR)Gefitinib(ErbB1/EGFR)
CP-724714(HER2/ErbB2)
BGJ398 ImatinibBIBF1120
BMS-754807 Danusertib
TAE684Tie2 kinase inhibitor
CrizotinibCrizotinibLinsitinibGSK1904529ANVP-ADW742NVP-AEW541BMS-536924
GSK1838705A
AmuvatinibOSI-930
DasatinibSunitinib Malate
Imatinib Mesylate
ForetinibPHA-665752
SU11274PF-04217903
XL-184XL-184 free base
MGCD-265
CH5424802GSK1838705A
Crizotinib
TG101209AmuvatinibGW441756(TrkA)
PazopanibAxitinib
ZM 306416(VEGFR1)XL-184(VEGFR2)
Vandetanib(VEGFR2)SAR131675(VEGFR3)
PP-121
Crenolanib(PDGFR)Sunitinib Malate(PDGFR)
BIBF1120
CP 673451(PDGFR)
AZD4547BIBF1120
PD173074(FGFR1)Ponatinib(FGFR1)
Selective FGFR inhibitors
CP-724714MubritinibNeratinibAZD8931Afatinib
-
Excellent Validation, Technical Support and Prompt Delivery17
VEGFRPr
otein
Tyros
ine K
inase
VEGFR2 selective
Product Citations:Science, 2011, 331(6019): 912-16PLoS Genet, 2012, 8(2): e1002500Mol Cell Proteomics, 2012, 11(9): 745-57
Data from [ Science, 2011, 331(6019): 912-16 ]PD173074 purchased from Selleck
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selectivity over PDGFR and c-Src.
S1264 PD173074
Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFR, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
S1178 Regorafenib (BAY 73-4506)
Product Citations:Nat Genet, 2012, 44(8): 852-60Cancer Res, 2011, 71(15): 5255-64
Data from [ Nat Genet, 2012, 44(8): 852-60 ]Foretinib purchased from Selleck
Foretinib (GSK1363089, XL880) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFR/ and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
S1111 Foretinib (GSK1363089)
pAXL
tAXL
GAPDH
Par
enta
l
Vect
or
AX
L W
T
AX
L L6
20M
AX
L K
D K
567R
Vect
or
AX
L W
T
AX
L L6
20M
AX
L K
D K
567R
XL880(1M) : - +
Product Citation:Hepatology, 2012, 56(6): 2363-74
RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-RafV600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.
S2161 RAF265 (CHIR-265) VEGFR2 selective
Licensed by Pfizer
HN
O
HN
OF
F
O
N
O
O
NO
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
10 mM/1 mL in DMSO 5 mg 100 mg10 mgSize
Product Citations:Haematologica, 2011, 96(6): 922-26Mol Cancer Ther, 2012, 11(3): 690-9
Data from [ Haematologica, 2011, 96(6): 922-26 ]Dovitinib purchased from Selleck
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
S1018 Dovitinib (TKI-258, CHIR-258)
Product Citation:Mol Cancer Ther, 2011, 10: 1028-35
Data from [ J Pharmacol Exp Ther, 2012, 341(2): 386-95 ]Cediranib purchased from Selleck
Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of 1000-fold selective more for VEGFR than PDGFR-, CSF-1R and Flt3, Phase 2/3.
S1017 Cediranib (AZD217)
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
Product Citation:Exp Eye Res, 2013, 112: 125-33
Data from [ Exp Eye Res, 2013, 112: 125-33 ]Tivozanib purchased from Selleck
Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met EGFR and IGF-1R. Phase 3.
S1207 Tivozanib (AV-951)
10 mM/1 mL in DMSO5 mg 50 mg10 mg
Size
10 mM/1 mL in DMSO10 mg 50 mg25 mg
Size
Cediranib Concentration (g/ml)0.1
0
2
4
6
8
10
12
14
1 10010
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
Protein Tyrosine KinaseVEGFR
10 mM/1 mL in DMSO10 mg 100 mg50 mg
Size
Product Citations:Mol Cell Proteomics, 2012, 11(6): M112Liver Int, 2011, 32(3): 400-9
Data from [ Liver Int, 2011, 32(3): 400-9 ]Linifanib purchased from Selleck
Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFR with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Phase 3.
S1003 Linifanib (ABT-869)
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Product Citations:J Clin Invest, 2011, 121(8): 3005-23Circ Res, 2011, 108(10): 1190-8 Cell Res, 2011, 21(7): 1080-7
Data from [ Circ Res, 2011, 108(10): 1190-8 ]Vatalanib 2HCl purchased from Selleck
Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.
S1101 Vatalanib (PTK787) 2HCl
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
S1361 MGCD-265
Data independently produced by Dr. Zhang of Tianjin Medical UniversityMGCD-265 purchased from Selleck
SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
S2842 SAR131675 VEGFR3 selective
NN
O HN
O
NH2HOO
10 mM/1 mL in DMSO 10 mg 50 mgSize
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical CenterBrivanib purchased from Selleck
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-. Phase 3.
S1084 Brivanib (BMS-540215)
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Product Citations:Mol Cell Proteomics, 2012, 11(9): 745-57Angiogenesis, 2012, 15(4): 569-80
Data from [ Angiogenesis, 2012, 15(4): 569-80 ]TSU-68 purchased from Selleck
SU6668 has greatest potency against PDGFR autophosphorylation with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
S1470 TSU-68 (SU6668)
10 mM/1 mL in DMSO2 mg 100 mg10 mg
Size
Product Citation:PLoS One, 2013, 8(5): e64369
Data from [ PLoS One, 2013, 8(5): e64369 ]E7080 purchased from Selleck
E7080 (Lenvatinib) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFR/. Phase 3.
S1164 E7080 (Lenvatinib)
Control Len Dex Len+Dex
Len+Bor +Dex
Len
+Bor
Bor
TF m
RNA
ratio
n
GAPDH
TF (283 bp)
10 mM/1 mL in DMSO 5 mg 100 mg10 mgSize
-
Excellent Validation, Technical Support and Prompt Delivery19
VEGFRPr
otein
Tyros
ine K
inase
Product Citation:Cardiovasc Res, 2011, 91(3): 402-11
Data from [ Cardiovasc Res, 2011, 91(3): 402-11 ]Motesanib Diphosphate purchased from Selleck
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 1/2.
S1032 Motesanib Diphosphate (AMG-706)
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Product Citation:J Virol, 2010, 85(5): 2296-303
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-/, and c-Kit.
S3012 Pazopanib
Product Citations:Haematolog, 2011, 96(6): 922-6Mol Cancer Ther, 2011, 10: 1028-35
Data from [ Brit J Cancer, 2010, 104(1): 75-82 ]Dovitinib Dilactic acid purchased from Selleck
Dovitinib Dilactic acid (TKI258 Dilactic acid) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
S2769 Dovitinib Dilactic acid (TKI258 Dilactic acid)
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 M, 1.266 M and 1.667 M, respectively.
S2202 NVP-BHG712
NVP-BHG712 purchased from Selleck
Data independently produced by Dr. Zhang of Tianjin Medical UniversityENMD-2076 purchased from Selleck
ENMD-2076 has selective activity against Aurora A and VEGFR(Flt3) with IC50 of 14 nM and 1.86 nM, 25-fold selective to Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFR. Phase 2.
S1181 ENMD-2076
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
S2859 Golvatinib (E7050) VEGFR2 selective
10 mM/1 mL in DMSO200 mg10 mg 50 mg
Size
CYC116 purchased from Selleck
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, less potent to VEGFR2 with Ki of 44 nM, with 50-fold more potent than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3/, CK2, Plk1 and SAPK2A. Phase 1.
S1171 CYC116
10 mM/1 mL in DMSO5 mg 200 mg50 mg
Size
10 mM/1 mL in DMSO10 mg 500 mg25 mg
Size
SO ONH2
NH
N
N
NNN
F HN
O
HN
OFO
NNH
N
O
NN
020406080
100120140160180
CX
CR
4 ex
pres
sion
(% C
ontro
l)
CtrlCM + - - - -+ +
++
++
+--- - --- - --- - -
VEGFCM
AMG
VEDFR2-1
MAZ
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
25 mg 100 mgSize
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
---USA and Canada only---www.selleckchem.com
Protein Tyrosine KinaseVEGFR
10 mM/1 mL in DMSO50 mg5 mg 25 mg
Size
10 mM/1 mL in DMSO50 mg5 mg 25 mg
Size
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center OSI-930 purchased from Selleck
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; modest activity to Flt-1, c-Raf and Lck, and low activity against PDGFR/, Flt-3 and Abl. Phase 1.
S1220 OSI-930
Product Citation:Biochem Pharmacol, 2012, 84(6): 766-74
Data from [ Mol Cell Proteomics, 2012, 11(9): 745-57 ]Ki8751 purchased from Selleck
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFR and FGFR-2, little activity to EGFR, HGFR and InsR.
S1363 Ki8751
Product Citations:J Exp Med, 2012, 209(3): 507-20Mol Cell Proteomics, 2012, 11(9): 745-57
VEGFR2 selective
10 mM/1 mL in DMSO10 mg 50 mg
Size
Data independently produced by one customerBrivanib alaninate purchased from Selleck
Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.
S1138 Brivanib alaninate (BMS-582664)
AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKC and CDK1/cyclin B. Phase 1/2.
S1486 AEE788 (NVP-AEE788)
KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-/ and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.
S1557 KRN 633
Apatinib (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
S2221 Apatinib VEGFR2 selective
ZM-323881 is a potent and selective VEGFR2 inhibitor with IC50 of
-
Excellent Validation, Technical Support and Prompt Delivery21
VEGFRPr
otein
Tyros
ine K
inase
BIBF1120
Cediranib
Dovitinib
Motesanib Diphosphate
Sunitinib Malate
Vandetanib
Brivanib
XL-184
Brivanib alaninate
E7080
CYC116
Regorafenib
ENMD-2076
Tivozanib
PD173074
MGCD-265
Ki8751
AEE788
Ponatinib
KRN 633
BMS 794833
Apatinib
Telatinib
SAR131675
Semaxanib
Golvatinib
ZM 323881 HCl
ZM 306416
Pazopanib
Cabozantinib malate
S1010
S1017
S1018
S1032
S1042
S1046
S1084
S1119
S1138
S1164
S1171
S1178
S1181
S1207
S1264
S1361
S1363
S1486
S1490
S1557
S2201
S2221
S2231
S2842
S2845
S2859
S2896
S2897
S3012
S4001
++
+++
++++
+
++
++
++++
+++
+
+++
+++
34 nM [IC50]
10nM [IC50]
2 nM [IC50]
380 nM [IC50]
22 nM [IC50]
13 nM [IC50]
0.21 nM [IC50]
3 nM [IC50]
170 nM [IC50]
0.33 M [IC50]
10 nM [IC50]
+++
++++
++
++++
+
++
++
++++
++
+++
++
+++
+
++++
+
+++
++++
+
+++
+
++
+++
+++
++
++
+++
++
++++
5 nM [IC50]
0.5 nM [IC50]
13 nM [IC50]
3 nM [IC50]
80 nM [IC50]
40 nM [IC50]
25 nM [IC50]
0.035 nM [IC50]
25 nM [IC50]
4 nM [IC50]
44 nM [IC50]
4.2 nM [IC50]
58.2 nM [IC50]
0.16 nM [IC50]
100-200 nM [IC50]
3 nM [IC50]
0.9 nM [IC50]
77 nM [IC50]
1.5 nM [IC50]
160 nM [IC50]
15 nM [IC50]
2.43 nM [IC50]
6 nM [IC50]
1.04 M [IC50]
16 nM [IC50]
1000-fold more sensitive for EGFR than human c-Src or v-Abl. Phase 3.
S1023 Erlotinib HCl (OSI-744)
EGFR Inhibitors
200 mg10 mg 50 mgSize
CI-1033 is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
S1019 Canertinib (CI-1033)
Data from [ Carcinogenesis, 2010, 31(11): 1948-55 ]Canertinib purchased from Selleck
Product Citation:Cancer Discov, 2012, 2(5): 458-71
EGFR selective
Data from [ Biochem Biophys Res Commun, 2013, 435(4): 533-9 ]AG-490 purchased from Selleck
10 mM/1 mL in DMSO10 mg 25 mg
Size
AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 M, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
S1143 AG-490
Product Citation:Prostate, 2013, 73(3): 267-77
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of
-
Excellent Validation, Technical Support and Prompt Delivery23
EGFRPr
otein
Tyros
ine K
inase
Data from [ Biochem Pharmacol , 2011, 82(10): 1457-66 ]Lapatinib Ditosylate purchased from Selleck
Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 nM and 9.2 nM, respectively.
S1028 Lapatinib Ditosylate (GW-572016)
Product Citations:Proc Natl Acad Sci U S A, 2012, 109(17): 6584-9Oncogene, 2013, 32(37): 4331-42Biochem Pharmacol , 2011, 82(10): 1457-66
Data from [ Cancer Discov, 2013, 3(2): 224-37 ]Neratinib purchased from Selleck
Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
S2150 Neratinib (HKI-272)
Product Citations:Cancer Discov, 2012, 2(5): 458-71Cancer Discov, 2013, 3(2): 168-81
10 mM/1 mL in DMSO50 mg5 mg 25 mg
Size
10 mM/1 mL in DMSO100 mg5 mg 25 mg
Size
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, IR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
S1167 CP-724714 HER2 selective
Data independently produced by Reto Baumann from ETH ZurichCP-724714 purchased from Selleck
CUDC-101 is a potent multi-target inhibitor targeting HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, inhibits both class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
S1194 CUDC-101
10 mM/1 mL in DMSO200 mg10 mg 50 mg
Size
Data independently produced by Dr. Zhang of Tianjin Medical UniversityCUDC-101 purchased from Selleck
10 mM/1 mL in DMSO25 mg 100 mg
Size
10 mM/1 mL in DMSO200 mg10 mg 50 mg
Size
Data from [ Mol Cancer Ther, 2012, 11(10): 2149-57 ]WZ4002 purchased from Selleck
Product Citations:Clin Cancer Res, 2012, 18(6): 1663-71Mol Cancer Ther, 2012, 11(10): 2149-57
WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM; does not inhibit ERBB2 phosphorylation (T798I).
S1173 WZ4002 EGFR selective
100 mg5 mg 25 mgSize
Data independently produced by Dr. Zhang of Tianjin Medical UniversityPD153035 HCl purchased from Selleck
EGFR selective
PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
S1079 PD153035 HCl
Product Citation:Antivir Res, 2010, 89(1): 64-70
AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 1/2.
S2192 AZD8931
EGFR selective
Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Phase 2.
S1392 Pelitinib (EKB-569)
Product Citation:J Immunol, 2012, 188(9): 4581-9
Data from [ J Immunol, 2012, 188(9): 4581-9 ]Pelitinib purchased from Selleck
10 mM/1 mL in DMSO100 mg5 mg 25 mg
Size
10 mM/1 mL in DMSO 5 mg 200 mg50 mgSize
[email protected] Free:(877)796-6397Phone:+1-832-582-8158
