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www.MedChemExpress.com 1
Inhibitors, Agonists, Screening
Librarieswww.MedChemExpress.com
Antibody-drug Conjugate/ADC Related
The antibody-drug conjugate (ADC), a humanized or human
monoclonal antibody conjugated with highly cytotoxic smallmolecules
(payloads) through chemical linkers, is a novel therapeutic format
and has great potential to make a paradigmshift in cancer
chemotherapy. The three components of the ADC together give rise to
a powerful oncolytic agent capableof delivering normally
intolerable cytotoxins directly to cancer cells, which then
internalize and release the cell-destroyingdrugs. At present, two
ADCs, Adcetris and Kadcyla, have received regulatory approval with
>40 others in clinicaldevelopment.ADCs are administered
intravenously in order to prevent the mAb from being destroyed by
gastric acids and proteolyticenzymes. The mAb component of the ADC
enables it to circulate in the bloodstream until it finds and binds
totumor-specific cell surface antigens present on target cancer
cells. Linker chemistry is an important determinant of thesafety,
specificity, potency and activity of ADCs. Linkers are designed to
be stable in the blood stream (to conform to theincreased
circulation time of mAbs) and labile at the cancer site to allow
rapid release of the cytotoxic drug. Firstgeneration ADCs made use
of early cytotoxins such as the anthracycline, doxorubicin or the
anti-metabolite/antifolateagent, methotrexate. Current cytotoxins
have far greater potency and can be divided into three main groups:
auristatins,maytansines and calicheamicins.The development of
site-specific conjugation methodologies for constructing
homogeneous ADCs is an especiallypromising path to improving ADC
design, which will open the way for novel cancer
therapeutics. References:[1] Tsuchikama K, et al. Protein
Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
https://www.MedChemExpress.com
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• ADC Cytotoxin 3
• ADC Linker 8
• Drug-Linker Conjugates for ADC 11
• PROTAC-linker Conjugate for PAC 15
Inhibitors, Agonists, Screening
Librarieswww.MedChemExpress.com
Target List in Antibody-drug Conjugate/ADC Related
2 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
https://www.MedChemExpress.com
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www.MedChemExpress.com 3
ADC Cytotoxin
ADC Cytotoxin are a large collection of toxins for
antibody-drugconjugate (ADC) development projects. The toxins that
can be usedas payloads should be soluble, amenable to conjugation,
and stable.There are myriads of cellular toxins in natural or
synthesized, but onlya few have been found adaptable for an ADC
concept.The toxins targeting tubulin filaments include
Maytansinoids,Auristatins, Taxol derivatives, etc. Amatoxins are a
class oftranscription-inhibiting agents. They bind to RNA
polymerase II,leading to cell apoptosis. Protein toxins function in
the similar MOA(mechanism of action) with cellular toxins, they
could inhibit proteinsynthesis and induce cell death. While
enzyme-based ADCs alter the
microenvironment of disease tissues to disturb their
functions.
https://www.MedChemExpress.com/Targets/ADC Cytotoxin.html
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Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 98.26%Clinical Data: Phase 4Size: 10mM x 1mL in
DMSO,
100 mg, 500 mg
Purity: 98.44%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 97.51%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.36%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg, 100 mg
Purity: 87.63%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg, 100 mg
Purity: 99.79%Clinical Data: No Development ReportedSize: 1 mg,
2 mg, 5 mg
Purity: 92.43%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg,
100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 10
mg, 50 mg
ADC Cytotoxin Inhibitors & Modulators
Bioactivity: 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel
derivativewith improved pharmacological features and higher
watersolubility. IC50 value: Target: Microtubule
inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell
cyclearrest and apoptosis as measured by flow cytometry, DNA…
Bioactivity: Aldoxorubicin (INNO-206) is an albumin-binding
prodrug ofdoxorubicin, which is released from albumin under
acidicconditions. Aldoxorubicin (INNO-206) has potent
antitumoractivities in various cancer cell lines and in murine
tumormodels.
Bioactivity: alpha-Amanitin is the principal toxin of several
deadlypoisonous mushrooms, exerting its toxic function by
inhibiting
.RNA-polymerase II
Bioactivity: Ansamitocin P 3' exhibits antitumour activity, is
an antibodydrug conjugate cytotoxin. The more information please
refer toAnsamitocin P-3 (HY-15739).
Bioactivity: Ansamitocin P-3 is a inhibitor. Ansamitocin
P-3microtubuleis a macrocyclic antitumor antibiotic.
Bioactivity: Auristatin E is a cytotoxic tubulin modifier with
potent andselective antitumor activity; MMAE analog and cytotoxin
inAntibody-drug conjugates.
Bioactivity: Auristatin F is a cytotoxic tubulin modifier with
potent andselective antitumor activity; MMAF analog and cytotoxin
inAntibody-drug conjugates.
Bioactivity: Calicheamicin is a cytotoxic agent that causes
double-strandDNA breaks.
Bioactivity: Campathecin is a potent DNA enzyme topoisomerase
Iinhibitor, with an of 679 nM.IC50
Bioactivity: D8-MMAD is a deuterated form of MMAD, which is a
disrupting agent.microtubule
4 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol;
10-Deacetylpaclitaxel 7-Xyloside; …) Cat. No.: HY-20584
Aldoxorubicin (INNO-206; DOXO-EMCH) Cat. No.: HY-16261
alpha-Amanitin (α-Amanitin; α-Amatoxin) Cat. No.: HY-19610
Ansamitocin P 3' (Antibiotic C 15003P3'; Maytansinol butyrate)
Cat. No.: HY-19839
Ansamitocin P-3 (Antibiotic C 15003P3; Maytansinol isobutyrate)
Cat. No.: HY-15739
Auristatin E Cat. No.: HY-15582
Auristatin F Cat. No.: HY-15583
Calicheamicin (Calicheamicin γ1) Cat. No.: HY-19609
Campathecin (Camptothecin; (S)-(+)-Camptothecin; CPT) Cat. No.:
HY-16560
D8-MMAD (Demethyldolastatin 10 D8; Monomethylauristatin D D8;
Monomethyl Dolastatin 10 D8) Cat. No.: HY-15581S
https://www.MedChemExpress.com/Targets/ADC
Cytotoxin.htmlhttps://www.MedChemExpress.com/10-deacetyl-7-xylosyl-paclitaxel.htmlhttps://www.MedChemExpress.com/INNO-206.htmlhttps://www.MedChemExpress.com/alpha-Amanitin.htmlhttps://www.MedChemExpress.com/Ansamitocin-P-3_acute_.htmlhttps://www.MedChemExpress.com/Ansamitocin-P-3.htmlhttps://www.MedChemExpress.com/Auristatin-E.htmlhttps://www.MedChemExpress.com/Auristatin-F.htmlhttps://www.MedChemExpress.com/Calicheamicin.htmlhttps://www.MedChemExpress.com/Campathecin.htmlhttps://www.MedChemExpress.com/D8-MMAD.html
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www.MedChemExpress.com 5
Purity: 98.99%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Purity: 99.47%Clinical Data: LaunchedSize: 10mM x 1mL in
DMSO,
50 mg, 100 mg, 200 mg, 500 mg, 1 g
Purity: >98%Clinical Data: LaunchedSize: 50 mg, 100 mg, 200
mg, 500 mg
Purity: 99.83%Clinical Data: Phase 2Size: 1 mg, 5 mg
Purity: 99.27%Clinical Data: LaunchedSize: 10mM x 1mL in
Water,
10 mg, 50 mg, 100 mg, 200 mg, 500 mg
Purity: >98%Clinical Data: LaunchedSize: 10 mg, 50 mg
Purity: 98.56%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
2 mg, 5 mg, 10 mg
Purity: 99.56%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg,
5 mg, 10 mg
Purity: 98.31%Clinical Data: No Development ReportedSize: 1 mg,
5 mg, 10 mg
Bioactivity: D8-MMAE is a deuterated labeled MMAE, a potent
mitoticinhibitor.
Bioactivity: D8-MMAF is a deuterated form of MMAF, which is a
disrupting agent.microtubule
Bioactivity: D8-MMAF hydrochloride is a deuterated form of
MMAFhydrochloride, which is a disrupting agent.microtubule
Bioactivity: Daun02 is a prodrug of the
inhibitortopoisomeraseDaunorubicin.
Bioactivity: Daunorubicin (RP 13057, Daunomycin, Rubidomycin) is
a inhibitor with potent antineoplastictopoisomerase II
activities. Daunorubicin inhibites inDNA and RNA
synthesissensitive and resistant Ehrlich ascites tumor cells.
Bioactivity: Daunorubicin Hydrochloride is a
inhibitortopoisomerase IIwith potent antineoplastic activities.
DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA
synthesisresistant Ehrlich ascites tumor cells.
Bioactivity: Angiotensin II human is a vasoconstrictor that acts
on the and the receptor.AT1 AT2
Bioactivity: Doxorubicin is a cytotoxic anthracycline antibiotic
for thetreatment of multiple cancers. The possible mechanisms
bywhich doxorubicin acts in the cancer cell are intercalationinto
DNA and disruption of -mediated DNAtopoisomerase-IIrepair.
Bioactivity: Doxorubicin hydrochloride is a cytotoxic
anthracyclineantibiotic for the treatment of multiple cancers. The
possiblemechanisms by which doxorubicin acts in the cancer cell
areintercalation into DNA and disruption of
-mediated DNA repair.topoisomerase-II
Bioactivity: Duocarmycin TM is an exceptionally potent
antitumorantibiotic.
D8-MMAE (D8-Monomethyl auristatin E) Cat. No.: HY-15162A
D8-MMAF (Monomethylauristatin F D8) Cat. No.: HY-15579S
D8-MMAF hydrochloride Cat. No.: HY-15579AS
Daun02 Cat. No.: HY-13061
Daunorubicin (RP 13057; Daunomycin; Rubidomycin) Cat. No.:
HY-13062A
Daunorubicin Hydrochloride (RP 13057 (Hydrochloride); Daunomycin
(Hydrochloride); Rubidomycin (Hydrochloride)) Cat. No.:
HY-13062
Dolastatin 10 (DLS 10; NSC 376128) Cat. No.: HY-15580
Doxorubicin (Hydroxydaunorubicin) Cat. No.: HY-15142A
Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride))
Cat. No.: HY-15142
Duocarmycin TM Cat. No.: HY-107769
https://www.MedChemExpress.com/d8-mmae.htmlhttps://www.MedChemExpress.com/D8-MMAF.htmlhttps://www.MedChemExpress.com/D8-MMAF_hydrochloride.htmlhttps://www.MedChemExpress.com/daun02.htmlhttps://www.MedChemExpress.com/daunorubicin.htmlhttps://www.MedChemExpress.com/Daunorubicin-Hydrochloride.htmlhttps://www.MedChemExpress.com/Dolastatin-10.htmlhttps://www.MedChemExpress.com/Doxorubicin.htmlhttps://www.MedChemExpress.com/Doxorubicin-hydrochloride.htmlhttps://www.MedChemExpress.com/Duocarmycin_TM.html
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Purity: 99.89%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
2 mg, 5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 2 mg,
5 mg, 10 mg
Purity: 99.92%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg, 100 mg
Purity: 99.45%Clinical Data: LaunchedSize: 10mM x 1mL in
DMSO,
5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg
Purity: 99.75%Clinical Data: LaunchedSize: 10mM x 1mL in
DMSO,
100 mg, 500 mg
Purity: 98.74%Clinical Data: Phase 2Size: 2 mg, 5 mg, 10 mg, 25
mg, 50 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg,
10 mg, 50 mg, 100 mg
Purity: >98%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg,
100 mg
Purity: 99.03%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg
Purity: 98.20%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Bioactivity: Dxd is a potent inhibitor, with an ofDNA
topoisomerase I IC500.31 μM, used as a conjugated drug of
HER2-targeting ADC(DS-8201a).
Bioactivity: Maytansinol inhibits microtubule assembly and
inducesmicrotubule disassembly in vitro. Target:
Microtubule/Tubulinin vitro: Maytansinol disrupts the mitotic
spindle andprevents mitotic exit in Drosophila. Maytansinol reduces
thegrowth and/or survival of HCT116 cells in a dose-dependent…
Bioactivity: MC-DOXHZN is an albumin-binding prodrug of
Doxorubicin, withacid-sensitive properties .[1]
Bioactivity: MC-DOXHZN hydrochloride is an albumin-binding
prodrug ofDoxorubicin, with acid-sensitive properties .[1]
Bioactivity: Mertansine (DM1) is a inhibitor and is
anmicrotubulinantibody-conjugatable maytansinoid that is developed
toovercome systemic toxicity associated with maytansine and
toenhance tumor-specific delivery. Mertansine can be attached toa
monoclonal antibody with a linker to create an antibody-drug…
Bioactivity: Methotrexate is a antagonist, with median of 78
nMfolate IC50in assay.in vitro
Bioactivity: Mitomycin C is an antitumor drug and antibiotic
that showsextraordinary ability to inhibit . Mitomycin C isDNA
synthesisa DNA cross-linking agent, which induces DNA damaging.
Bioactivity: MMAD is a potent inhibitor, is a toxin payload
intubulinantibody drug conjugates ( ).ADCs
Bioactivity: MMAF (Monomethylauristatin F) is an antitubulin
agent thatinhibit cell division; inhibits H3397 cell growth with an
IC50of 105 nM.
Bioactivity: MMAF hydrochloride is an antitubulin agent that
inhibit celldivision; inhibits H3397 cell growth with an of 105
nM.IC50
6 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
Dxd (Exatecan derivative for ADC) Cat. No.: HY-13631D
Maytansinol (Ansamitocin P-0) Cat. No.: HY-19474
MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat. No.:
HY-16261A
MC-DOXHZN hydrochloride
(Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat. No.:
HY-16261B
Mertansine (DM1; Maytansinoid DM1) Cat. No.: HY-19792
Methotrexate (Amethopterin; CL14377; WR19039) Cat. No.:
HY-14519
Mitomycin C (Ametycine) Cat. No.: HY-13316
MMAD (Demethyldolastatin 10; Monomethylauristatin D; Monomethyl
Dolastatin 10) Cat. No.: HY-15581
MMAF (Monomethylauristatin F) Cat. No.: HY-15579
MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat.
No.: HY-15579A
https://www.MedChemExpress.com/Dxd.htmlhttps://www.MedChemExpress.com/Maytansinol.htmlhttps://www.MedChemExpress.com/DOXO-EMCH.htmlhttps://www.MedChemExpress.com/MC-DOXHZN_hydrochloride.htmlhttps://www.MedChemExpress.com/Mertansine.htmlhttps://www.MedChemExpress.com/Methotrexate.htmlhttps://www.MedChemExpress.com/Mitomycin-C.htmlhttps://www.MedChemExpress.com/MMAD.htmlhttps://www.MedChemExpress.com/mmaf.htmlhttps://www.MedChemExpress.com/MMAF-Hydrochloride.html
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www.MedChemExpress.com 7
Purity: >98%Clinical Data: No Development ReportedSize: 1
mg
Purity: 99.96%Clinical Data: No Development ReportedSize: 5 mg,
10 mg, 50 mg
Purity: 99.05%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg
Purity: 99.90%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
5 mg, 10 mg, 50 mg
Purity: 96.84%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg, 50 mg
Purity: 99.68%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.97%Clinical Data: LaunchedSize: 10mM x 1mL in
DMSO,
50 mg, 100 mg, 500 mg
Purity: 99.94%Clinical Data: Phase 4Size: 10mM x 1mL in
DMSO,
1 mg, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 g
Purity: 96.88%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
2 mg, 5 mg, 10 mg
Bioactivity: MMAF-Ome belongs to ADC, and inhibits several tumor
cell lineswith s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM
forIC50MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 )
cell-
lines, respectively.
Bioactivity: Monomethyl auristatin E (MMAE; SGD-1010) is a
syntheticderivative of dolastatin 10 and functions as a potent
inhibitor by inhibiting tubulin polymerization.mitoticMMAE is
widely used as a cytotoxic component of antibody-drug
to treat several different cancer types.conjugates (ADCs)
Bioactivity: Paclitaxel (Taxol), a naturally occurring
antineoplasticagent, stabilizes , resulting intubulin
polymerizationarrest at the G2/M phase of the cell cycle and
apoptotic celldeath .[1] [2]
Bioactivity: PF-06380101 is a novel cytotoxic Dolastatin 10
analogue; withexcellent potencies in tumor cell proliferation
assays anddifferential ADME properties when compared to other
syntheticauristatin analogues that are used in the preparation of
ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and
N87…
Bioactivity: PNU-159682, a highly potent metabolite of the
anthracyclinenemorubicin with outstanding cytotoxicity, is a potent
ADCs
.cytotoxin
Bioactivity: Taltobulin (HTI-286; SPA-110) is an analogue of
Hemiasterlin;potent tubulin inhibitor; ADCs cytotoxin. IC50 value:
Target:tubulin in vitro: HTI-286 significantly
inhibitedproliferation of all three hepatic tumor cell lines (mean
IC50= 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no
decrease…
Bioactivity: Taltobulin hydrochloride is an analogue of
Hemiasterlin;potent tubulin inhibitor; ADCs cytotoxin. IC50 value:
Target:tubulin in vitro: HTI-286 significantly inhibits
proliferationof all three hepatic tumor cell lines (mean IC50 = 2
nmol/L+/- 1 nmol/L). Interestingly, no decrease in viable
primary…
Bioactivity: Taltobulin trifluoroacetate (HTI-286; SPA-110) is
an analogueof Hemiasterlin; potent tubulin inhibitor; ADCs
cytotoxin.IC50 value: Target: tubulin in vitro: HTI-286
significantlyinhibited proliferation of all three hepatic tumor
cell lines(mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro.
Interestingly,…
Bioactivity: Tubulysin A(TubA) is a myxobacterial product that
can functionas an antiangiogenic agent in many in vitro
assays;anti-microtubule, anti-mitotic, an apoptosis
inducer,anticancer, anti-angiogenic, and antiproliferative.
IC50value: Target: microtubule Tubulysin A is a novel
antibiotic,…
MMAF-OMe (Monomethyl auristatin F methyl ester) Cat. No.:
HY-79256
Monomethyl auristatin E (MMAE; SGD-1010) Cat. No.: HY-15162
Paclitaxel (Taxol) Cat. No.: HY-B0015
PF-06380101 Cat. No.: HY-12522
PNU-159682 Cat. No.: HY-16700
Taltobulin (HTI-286; SPA-110) Cat. No.: HY-15584
Taltobulin hydrochloride (HTI-286 hydrochloride; SPA-110
hydrochloride) Cat. No.: HY-15584B
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate; SPA-110
trifluoroacetate) Cat. No.: HY-15584A
Tubulysin A (TubA) Cat. No.: HY-15995
https://www.MedChemExpress.com/MMAF-OMe.htmlhttps://www.MedChemExpress.com/Monomethyl-auristatin-E.htmlhttps://www.MedChemExpress.com/Paclitaxel.htmlhttps://www.MedChemExpress.com/PF-06380101.htmlhttps://www.MedChemExpress.com/pnu-159682.htmlhttps://www.MedChemExpress.com/taltobulin.htmlhttps://www.MedChemExpress.com/Taltobulin-hydrochloride.htmlhttps://www.MedChemExpress.com/Taltobulin-trifluoroacetate.htmlhttps://www.MedChemExpress.com/Tubulysin-A.html
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ADC LinkerAntibody-drug conjugates linker
Antibody-drug conjugates (ADCs) consist of a desirable
monoclonalantibody, an active cytotoxic drug and an appropriate
linker. Anappropriate linker between the antibody and the cytotoxic
drugprovides a specific bridge, and thus helps the antibody to
selectivelydeliver the cytotoxic drug to tumor cells and accurately
releases thecytotoxic drug at tumor sites. In addition to
conjugation, the linkersmaintain ADCs’ stability during the
preparation and storage stages ofthe ADCs and during the systemic
circulation period.The ADCs currently undergoing clinical
evaluation contain linkers aremostly classified into two
categories: cleavable and noncleavable.Cleavable linkers rely on
processes inside the cell to liberate the toxin,
such as reduction in the cytoplasm, exposure to acidic
conditions in the lysosome, or cleavage by specific proteaseswithin
the cell. Noncleavable linkers require proteolytic degradation of
the antibody portion of the ADC for release ofthe cytotoxic
molecule, which will retain the linker and the amino acid by which
it was attached to the antibody.The selection of linker is target
dependent, based on the knowledge of the internalization and
degradation of theantibody-target antigen complex, and a
preclinical and activity comparison of conjugates. Moreover,in
vitro in vivothe choice of a linker is also influenced by which
cytotoxin is used, as each molecule has different chemical
constraints,and frequently the drug structure lends itself to a
specific linker.
8 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
https://www.MedChemExpress.com/Targets/ADC Linker.html
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www.MedChemExpress.com 9
Purity: 98.68%Clinical Data: No Development ReportedSize: 10 mg,
50 mg, 100 mg, 200 mg
Purity: 99.66%Clinical Data: No Development ReportedSize: 1
g
Purity: 96.13%Clinical Data: No Development ReportedSize: 50 mg,
100 mg
Purity: 98.13%Clinical Data: No Development ReportedSize: 10 mg,
50 mg, 100 mg, 500 mg
Purity: 98.67%Clinical Data: No Development ReportedSize: 50
mg
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg,
10 mg, 25 mg, 50 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg,
10 mg, 25 mg, 50 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 1
g
Purity: 99.96%Clinical Data: No Development ReportedSize: 50 mg,
100 mg, 500 mg
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg,
10 mg, 50 mg, 100 mg
ADC Linker Inhibitors & Modulators
Bioactivity: (Ac)Phe-Lys(Alloc)-PABC-PNP is a useful chemical
linker inantibody drug conjugates.
Bioactivity: 6-Maleimidohexanoic acid N-hydroxysuccinimide
ester(ECMS) is auseful protective group in antibody drug
conjugates.
Bioactivity: 6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)-
is anuseful linker for antibody-drug-conjugations (ADCs),
extractedfrom [Bioorg Chem. 2012 Apr-Jun;41-42:1-5.] compound
1i.
Bioactivity: DC1, an analogue of the minor groove-binding DNA
alkylatorCC-1065, is an antibody conjugate of cytotoxic DNA
alkylatorsfor the targeted treatment of cancer.
Bioactivity: DC1-Sme is an antibody conjugate of phosphate
prodrug ofcytotoxic DNA alkylators for the targeted treatment of
cancer.
Bioactivity: Fmoc-Phe-Lys(Boc)-PAB-PNP is an linker used in
theADCsynthesis of antibody-drug conjugates (ADCs).
Bioactivity: Fmoc-Val-Cit-PAB is a linker for
antibody-drug-conjugation(ADC).
Bioactivity: Fmoc-Val-Cit-PAB-PNP is a peptide prodrug linker,
is a linkerfor antibody-drug-conjugation (ADC).
Bioactivity: MC-Val-Cit-PAB is a cathepsin cleavable that isADC
linkerused for making antibody-drug conjugate. FDA approved
drugssuch as brentuximab vedotin use this linker.
Bioactivity: Mc-Val-Cit-PABC-PNP is a cathepsin cleavable
usedADC linkerin the synthesis of antibody-drug conjugates
(ADCs).
(Ac)Phe-Lys(Alloc)-PABC-PNP Cat. No.: HY-20560
6-Maleimidohexanoic acid N-hydroxysuccinimide ester (EMCS) Cat.
No.: HY-78961
6-Quinoxalinecarboxylic acid, 2,3-bis(bromomethyl)- Cat.
No.: HY-21210
DC1 Cat. No.: HY-112899
DC1-SMe Cat. No.: HY-112898
Fmoc-Phe-Lys(Boc)-PAB-PNP Cat. No.: HY-114430
Fmoc-Val-Cit-PAB Cat. No.: HY-19318
Fmoc-Val-Cit-PAB-PNP Cat. No.: HY-41189
MC-Val-Cit-PAB Cat. No.: HY-78738
Mc-Val-Cit-PABC-PNPCat. No.: HY-20336
https://www.MedChemExpress.com/Targets/ADC
Linker.htmlhttps://www.MedChemExpress.com/_ac_phe-lys_alloc_-pabc-pnp.htmlhttps://www.MedChemExpress.com/6-maleimidohexanoic-acid-n-hydroxysuccinimide-ester.htmlhttps://www.MedChemExpress.com/6-Quinoxalinecarboxylic-acid,-2,3-bis_bromomethyl_-.htmlhttps://www.MedChemExpress.com/DC1.htmlhttps://www.MedChemExpress.com/DC1-SMe.htmlhttps://www.MedChemExpress.com/Fmoc-Phe-Lys_Boc_-PAB-PNP.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB-PNP.htmlhttps://www.MedChemExpress.com/MC-Val-Cit-PAB.htmlhttps://www.MedChemExpress.com/Mc-Val-Cit-PABC-PNP.html
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Purity: 99.64%Clinical Data: No Development ReportedSize: 100
mg, 500 mg, 1 g
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg
Bioactivity: UAA crosslinker 1 act as substrates for pylRS/tRNA
pair thatenable its incorporation into a target protein.
Bioactivity: Val-cit-PAB-OH is a peptide prodrug linker.
10 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
UAA crosslinker 1 Cat. No.: HY-111434
Val-cit-PAB-OH Cat. No.: HY-12362
https://www.MedChemExpress.com/UAA_crosslinker_1.htmlhttps://www.MedChemExpress.com/Val-cit-PAB-OH.html
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www.MedChemExpress.com 11
Drug-Linker Conjugates for ADC
Drug-Linker Conjugates for Antibody Drug Conjugates
(ADC)comprise of an active cytotoxic drug and an appropriate
linker. TheDrug-Linker Conjugates can expand the utility of
monoclonalantibody (mAbs) and improve their potency and
effectiveness. Thesite-specific conjugations of Drug-Linker to an
antibody may involvegenetic engineering of the mAb to introduce
discrete, availablecysteines or non-natural amino acids with an
orthogonally-reactivefunctional group handle. These site-specific
approaches not onlyincrease the homogeneity of ADCs but also enable
novelbio-orthogonal chemistries that utilize reactive moieties
other thanthiol or amine. The cytotoxic drug, monomethyl auristatin
E (MMAE),
is conjugated to the three trastuzumab variants using a protease
cleavable linker and shows in vivo therapeuticefficacy.
https://www.MedChemExpress.com/Targets/Antibody-drug
Conjugate.html
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Purity: 97.23%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 10mM
x 1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.57%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 98.89%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.43%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 98.07%Clinical Data: No Development ReportedSize: 1 mg,
5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 1
mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 100
mg, 250 mg, 500 mg
Purity: 96.50%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Drug-Linker Conjugates for ADC Inhibitors & Modulators
Bioactivity: Acetylene-linker-Val-Cit-PABC-MMAE consists the
ADCs linker(Acetylene-linker-Val-Cit-PABC) and potent tubulin
inhibitor(MMAE), Acetylene-linker-Val-Cit-PABC-MMAE is an antibody
drugconjugate.
Bioactivity: AcLys-PABC-VC-Aur0101 is a cleavable anti-CXCR4
drug-linker.conjugates for ADC
Bioactivity: AmPEG6C2-Aur0131 is a non-cleavable anti-CXCR4
drug-linker.conjugates for ADC
Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin
inhibitor, isa toxin payload in antibody drug conjugate. IC50
Value: N/ATarget: tubulin; ADCs For comparison purposes, the ADC
A1-mc-MMAD and/or A1 -vc-MMAD were used. The linker payload,mc-MMAD
(6-maleimidocaproyl-monomethylauristatin-D) was…
Bioactivity: DBCO-(PEG)3-VC-PAB-MMAE is made by MMAE conjugated
toDBCO-(PEG)3-vc-PAB linker. Monomethyl auristatin E (MMAE),
apotent tubulin inhibitor, is a toxin payload in antibody
drugconjugate.
Bioactivity: Deruxtecan, a toxin and linker moiety of DS-8201,
is adrug-linker conjugate for antibody-drug conjugate
(ADC)extracted from patent WO2017002776A1, compound 1.
Bioactivity: Fmoc-Val-Cit-PAB-MMAE consists the ADCs
linker(Fmoc-Val-Cit-PAB) and potent tubulin inhibitor
(MMAE),Fmoc-Val-Cit-PAB-MMAE is an antibody drug conjugate.
Bioactivity: MAL-di-EG-Val-Cit-PAB-MMAE consists the ADCs
linker(MAL-di-EG-Val-Cit-PAB) and potent inhibitor
(MMAE),tubulinMAL-di-EG-Val-Cit-PAB-MMAE is an antibody drug
conjugate.
Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin
inhibitor, isa toxin payload in antibody drug conjugate; Mc-MMAD is
aprotective group (maleimidocaproyl) -conjugated MMAD. IC50Value:
Target: tubulin; ADCs For comparison purposes, the ADCA1 -mc-MMAD
and/or A1 -vc-MMAD were used. The linkerpayload,…
Bioactivity: Mc-MMAE is a protective group
(maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE), which
is a potent tubulininhibitor, is a toxin payload in antibody drug
conjugate (
).ADC
12 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) Cat. No.:
HY-19812
AcLys-PABC-VC-Aur0101 Cat. No.: HY-111554
AmPEG6C2-Aur0131 Cat. No.: HY-111555
Cys-mcMMAD Cat. No.: HY-15750
DBCO-(PEG)3-VC-PAB-MMAE Cat. No.: HY-111012
Deruxtecan Cat. No.: HY-13631E
Fmoc-Val-Cit-PAB-MMAE Cat. No.: HY-19811
MAL-di-EG-Val-Cit-PAB-MMAE Cat. No.: HY-100567
Mc-MMAD Cat. No.: HY-15740
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat. No.:
HY-15741
https://www.MedChemExpress.com/Targets/Drug-Linker Conjugates
for
ADC.htmlhttps://www.MedChemExpress.com/Acetylene-linker-Val-Cit-PABC-MMAE.htmlhttps://www.MedChemExpress.com/AcLys-PABC-VC-Aur0101.htmlhttps://www.MedChemExpress.com/AmPEG6C2-Aur0131.htmlhttps://www.MedChemExpress.com/cys-mcmmad.htmlhttps://www.MedChemExpress.com/DBCO-_PEG_3-VC-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Deruxtecan_analog.htmlhttps://www.MedChemExpress.com/Fmoc-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/MAL-di-EG-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Mc-MMAD.htmlhttps://www.MedChemExpress.com/Mc-MMAE.html
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www.MedChemExpress.com 13
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg,
5 mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg, 100 mg
Purity: 95.58%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.54%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg
Purity: 99.18%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg,
5 mg, 10 mg
Purity: 99.58%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Bioactivity: Mc-MMAF is a protective group-conjugated MMAF. MMAF
is a morepotent drug than Monomethyl auristatin E (MMAE), but
ischarged and relatively membrane-impermeable, is a potenttubulin
inhibitor, is a toxin payload in antibody drugconjugate. Target:
MMAF is a new auristatin derivative with a…
Bioactivity: mDPR-Val-Cit-PAB-MMAE consists the ADCs
linker(mDPR-Val-Cit-PAB) and potent tubulin inhibitor
(MMAE),mDPR-Val-Cit-PAB-MMAE is an antibody drug conjugate.
Bioactivity: N3-PEG3-vc-PAB-MMAE is a withdrug-linker conjugate
for ADCpotent antitumor activity by using the anti-mitotic
agent,monomethyl auristatin E (MMAE), linked via the
peptideN3-PEG3-vc-PAB.
Bioactivity: NAMPT inhibitor-linker 1 is a drug-linker
conjugates for ,ADCcomposed of an inhibitor as a payload, and a
linker.NAMPTADC-3 consists of an NAMPT inhibitor-linker 1 and
ananti-c-Kit monoclonal antibody, exihibits potent activityagainst
c-Kit expressing cell lines such as GIST-T1 and…
Bioactivity: NAMPT inhibitor-linker 2 is a drug-linker
conjugates for ,ADCcomposed of an inhibitor as a payload, and a
linker.NAMPTADC-4 consists of an NAMPT inhibitor-linker 2 and
ananti-c-Kit monoclonal antibody, exihibits potent activityagainst
c-Kit expressing cell lines such as GIST-T1 and…
Bioactivity: SMCC-DM1 is DM1 with a reactive linker SMCC to make
antibodydrug conjugate. DM1 (mertansine), a
thiol-containingmaytansinoid, is a potent microtubule-disrupting
agent.
Bioactivity: SPDB-DM4 is a by using thedrug-linker conjugate for
ADCmaytansinebased payload (DM4) via a SPDB linker,
exhibitingpotent anti-tumor activity.
Bioactivity: ST8154AA1 is a part of antibody drug conjugates (
)ADCscharged with inhibitor by a linker, shows
antitumorHDACactivity .[1]
Bioactivity: ST8155AA1 is a part of antibody drug conjugates (
)ADCscharged with inhibitor by a linker, shows
antitumorHDACactivity .[1]
Bioactivity: sulfo-SPDB-DM4 is a by using thedrug-linker
conjugate for ADCmaytansinebased payload (DM4) via the sulfo-SPDB
linker.
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat. No.:
HY-15578
mDPR-Val-Cit-PAB-MMAE Cat. No.: HY-19813
N3-PEG3-vc-PAB-MMAE Cat. No.: HY-100874
NAMPT inhibitor-linker 1 Cat. No.: HY-112615
NAMPT inhibitor-linker 2 Cat. No.: HY-112616
SMCC-DM1 (DM1-SMCC) Cat. No.: HY-101070
SPDB-DM4 Cat. No.: HY-12460
ST8154AA1 Cat. No.: HY-112805
ST8155AA1 Cat. No.: HY-112806
sulfo-SPDB-DM4 Cat. No.: HY-101141
https://www.MedChemExpress.com/McMMAF.htmlhttps://www.MedChemExpress.com/mDPR-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/N3-PEG3-vc-PAB-MMAE.htmlhttps://www.MedChemExpress.com/NAMPT_inhibitor-linker_1.htmlhttps://www.MedChemExpress.com/NAMPT_inhibitor-linker_2.htmlhttps://www.MedChemExpress.com/SMCC-DM1.htmlhttps://www.MedChemExpress.com/SPDB-DM4.htmlhttps://www.MedChemExpress.com/st8154aa1.htmlhttps://www.MedChemExpress.com/st8155aa1.htmlhttps://www.MedChemExpress.com/sulfo-SPDB-DM4.html
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Purity: 99.89%Clinical Data: Phase 2Size: 10mM x 1mL in
DMSO,
1 mg, 5 mg, 10 mg, 50 mg, 100 mg
Purity: >98%Clinical Data: No Development ReportedSize: 10mM
x 1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: 99.83%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Purity: >98%Clinical Data: No Development ReportedSize: 250
mg, 500 mg
Purity: 97.87%Clinical Data: No Development ReportedSize: 10mM x
1mL in DMSO,
1 mg, 5 mg, 10 mg
Bioactivity: SuO-Val-Cit-PAB-MMAE is a bydrug-linker conjugate
for ADCusing the anti-mitotic agent, monomethyl auristatin E
(MMAE),linked via the peptide SuO-Val-Cit-PAB.
Bioactivity: SW-163D-AcLysValCit-PABC-DMAE is a Drug-Linker
Conjugates for which consists of a natural bis-intercalator,
SW-163D,ADC
conjugated via an AcLysValCitPABC-DMAE linker .[1]
Bioactivity: Val-Cit-PAB-MMAE is a by usingdrug-linker conjugate
for ADCthe anti-mitotic agent, monomethyl auristatin E (MMAE),
linkedvia the peptide Val-Cit-PAB.
Bioactivity: Vc-MMAD consists the ADCs linker(Val-Cit) and
potent tubulininhibitor (MMAD), Vc-MMAD is an antibody drug
conjugate. IC50Valu: N/A Target: tubulin; ADCs Monomethyl
auristatin D(MMAD), a potent tubulin inhibitor, is a toxin payload
andantibody drug conjugate. For comparison purposes, the ADC
A1…
Bioactivity: VcMMAE is a with potentdrug-linker conjugate for
ADCantitumor activity by using the anti-mitotic agent,
monomethylauristatin E (MMAE), linked via the lysosomally
cleavabledipeptide, valine-citrulline (vc).
14 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
SuO-Val-Cit-PAB-MMAE Cat. No.: HY-100566
SW-163D-AcLysValCit-PABC-DMAE Cat. No.: HY-114325
Val-Cit-PAB-MMAE Cat. No.: HY-100374
Vc-MMAD Cat. No.: HY-15742
VcMMAE (mc-vc-PAB-MMAE) Cat. No.: HY-15575
https://www.MedChemExpress.com/SuO-Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/SW-163D-AcLysValCit-PABC-DMAE.htmlhttps://www.MedChemExpress.com/Val-Cit-PAB-MMAE.htmlhttps://www.MedChemExpress.com/Vc-MMAD.htmlhttps://www.MedChemExpress.com/VcMMAE.html
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www.MedChemExpress.com 15
PROTAC-linker Conjugate for PACPROTAC-linker for PROTAC-antibody
Conjugate
PROTAC-linker Conjugate for PAC comprises an antibody
conjugatedvia a linker to a PROTAC. The PROTAC-Antibody Conjugate
(PAC)molecules comprise an antibody conjugated via a linker (L1) to
aPROTAC, wherein the PROTAC comprises an ubiquitin E3 ligasebinding
groug (“E3LB”), a linker (“L2”) and a protein binding group(“PB”).
To obtain a PAC having potent efficacy and a desirabletherapeutic
index, the following components are provided. 1.Antibody (Ab): The
antibody portion of a PAC can target a cell thatexpresses an
antigen whereby the antigen specific PAC is
deliveredintracellularly to the target cell, typically through
endocytosis WhilePACs that comprise an antibody directed to an
antigen that is not
found on the cell surface may result in less specific
intracellular delivery of the PROTAC portion into the cell, the
PACmay still undergo pinocytosis. 2. Linkers (L1): A“linker” (L1)
is a bifunctional or multifunctional moiety that can be usedto link
one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC.
In some embodiments, PACs can beprepared using a L1 having reactive
functionalities for covalently attaching to the PROTAC and to the
antibody. 3.PROTAC(D).
https://www.MedChemExpress.com/Targets/PROTAC-linker Conjugate
for PAC.html
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Purity: >98%Clinical Data: No Development ReportedSize: 5 mg,
10 mg
PROTAC-linker Conjugate for PAC Inhibitors & Modulators
Bioactivity: PAC comprises an antibody conjugated via a linker
to a. PAC extracts from patent WO2017201449A1, compoundPROTAC
LP2. PAC is a more marked ( )estrogen receptor-alpha ERαdegrader
compared to PROTAC (without Ab).
16 Tel: 609-228-6898 Fax: 609-228-5909 Email:
[email protected]
PAC Cat. No.: HY-112100
https://www.MedChemExpress.com/Targets/PROTAC-linker Conjugate for
PAC.htmlhttps://www.MedChemExpress.com/PAC.html