Antibody-drug conjugates (ADCs) represent a novel class of cancer therapeutics. Their design involves a tumor-specific antibody, a linker and a cytotoxic payload. The payload in ADCs are highly potent cytotoxins, exerting their effects on critical cellular processes required for survival. Typically, the cytotoxins used in ADCs are a 100-1000 times more potent than regular chemotherapeutics and preferably have sub-nanomolar potency. Most compounds in current clinical testing utilize either maytansine derivatives (DM1/DM4) or auristatins (MMAE/ MMAF), which are both microtubule inhibitors. These typically induce apoptosis in cells undergoing mitosis by causing cell cycle arrest at G2/M. More recent work shows that microtubule inhibitors may also disrupt non-dividing cells in interphase. Other classes of cytotoxins used in ADCs include enediynes (Calicheamicin ), duocarmycin derivatives, pyrrolobenzodiazepines (PBDs) and indolinobenzodiazepines, all of which target the minor groove of DNA, and quinoline alkaloids (SN-38), which inhibit topoisomerase. For example, the potent cytotoxic drug doxorubicin and daunorubicin may interact with DNA by intercalation.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
Cell Cycle/DNA Damage >
Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MicroRNA PARP PKC Sirtuin Protein Arginine Deiminase
GPCR/G Protein >
5-HT Receptor Adenosine Receptor Adenylate Cyclase Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR Dopamine Receptor EBI2/GPR183 Endothelin Receptor GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR MCHR1 (GPR24) Melatonin Receptor mGluR Motilin Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor Prostaglandin Receptor Protease-Activated Receptor (PAR) Ras RGS Protein Sigma Receptor Somatostatin Receptor TSH Receptor Urotensin Receptor Vasopressin Receptor Melanocortin Receptor
Immunology/Inflammation >
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JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

MC-DOXHZN hydrochloride

MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin, with acid-sensitive properties[1].

  • CAS Number: 480998-12-7
  • MF: C37H43ClN4O13
  • MW: 787.21
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Aminomethyl-10-methyl-11-fluoro camptothecin

7-Aminomethyl-10-methyl-11-fluoro camptothecin is a cytotoxin of MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (HY-132158,compound 21a). 7-Aminomethyl-10-methyl-11-fluoro camptothecin can be used for the synthesis of camptothecin antibody-drug conjugate (ADC).

  • CAS Number: 2378616-23-8
  • MF: C22H20FN3O4
  • MW: 409.41
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAD

MMAD is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugates (ADCs).

  • CAS Number: 203849-91-6
  • MF: C41H66N6O6S
  • MW: 771.064
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 906.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 501.8±34.3 °C

Methotrexate-d3

Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].

  • CAS Number: 432545-63-6
  • MF: C20H19D3N8O5
  • MW: 457.45800
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 210°C dec.
  • Flash Point: 9℃

Thailanstatin A

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC[1][2][3].

  • CAS Number: 1426953-21-0
  • MF: C28H41NO9
  • MW: 535.63
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-CBI-CDPI2

(+)-CBI-CDPI2 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI2 is an antibody drug conjugates (ADCs) toxin.

  • CAS Number: 128300-15-2
  • MF: C36H28N6O4
  • MW: 608.64500
  • Catalog: ADC Cytotoxin
  • Density: 1.64g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aniline-MPB-amino-C3-PBD

Aniline-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Aniline-MPB-amino-C3-PBD is a sequence-selective DNA minor-groove binding agent. Aniline-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity[1].

  • CAS Number: 2412923-79-4
  • MF: C42H46N8O6
  • MW: 758.86
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methotrexate disodium

Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].

  • CAS Number: 7413-34-5
  • MF: C20H20N8Na2O5
  • MW: 498.403
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 823℃
  • Melting Point: N/A
  • Flash Point: N/A

Mitomycin C

Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis.

  • CAS Number: 50-07-7
  • MF: C15H18N4O5
  • MW: 334.327
  • Catalog: Bacterial
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 532.0±60.0 °C at 760 mmHg
  • Melting Point: 360 °C
  • Flash Point: 275.5±32.9 °C

Daunorubicin

Daunorubicin is a topoisomerase II inhibitor.

  • CAS Number: 20830-81-3
  • MF: C27H29NO10
  • MW: 527.520
  • Catalog: ADC Cytotoxin
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 770.0±60.0 °C at 760 mmHg
  • Melting Point: 155ºC
  • Flash Point: 419.5±32.9 °C

Seco-DUBA hydrochloride

Seco-DUBA hydrochloride is a toxin for ADC drug SYD985[1].

  • CAS Number: 1795733-93-5
  • MF: C29H23ClN4O4.xClH
  • MW:
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Duocarmycin SA

Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM[1]. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro[2].

  • CAS Number: 130288-24-3
  • MF: C25H23N3O7
  • MW: 477.46600
  • Catalog: ADC Cytotoxin
  • Density: 1.53±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SN-38-d5

SN-38-d5 is deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].

  • CAS Number: 718612-51-2
  • MF: C22H15D5N2O5
  • MW: 397.44
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-CBI-CDPI1

(+)-CBI-CDPI1 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI1 is an antibody drug conjugates (ADCs) toxin.

  • CAS Number: 128300-14-1
  • MF: C25H20N4O3
  • MW: 424.45
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Eg5-IN-2

Eg5-IN-2 (Compound Scaffold B (4)) is an Eg5 inhibitor (IC50: < 0.5 nM). Eg5-IN-2 can be used as an ADC payload for synthesis of ADCs[1].

  • CAS Number: 1629735-05-2
  • MF: C31H38F3N5O3
  • MW: 585.66
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Antibiotic 1166C

Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity[1][2][3].

  • CAS Number: 83329-73-1
  • MF: C38H58O11
  • MW: 690.86100
  • Catalog: Fungal
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)

7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin) is a Camptothecin (HY-16560) analogue. 7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin) is a ADC cytotoxin that can be used for synthesis of ADCs, and for cancer research[1].

  • CAS Number: 2873460-17-2
  • MF: C25H24FN3O7
  • MW: 497.47
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daunorubicin citrate

Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor[1][2][4][5].

  • CAS Number: 1884557-85-0
  • MF: C33H37NO17
  • MW: 719.64
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methotrexate

Methotrexate is a folate antagonist, with median IC50 of 78 nM in in vitro assay.

  • CAS Number: 59-05-2
  • MF: C20H22N8O5
  • MW: 454.439
  • Catalog: ADC Cytotoxin
  • Density: 1.4080
  • Boiling Point: 561.26°C
  • Melting Point: 195°C
  • Flash Point: 11℃

Duostatin 5

Duostatin 5 is a cytotoxin designed based on dolastatin, can meet the requirement of serving as an effective cytotoxin in ADC, but has the advantages of fewer synthesis steps, easy operation, less difficulty in quality control and more stable chemical synthesis process[1].

  • CAS Number: 2124210-34-8
  • MF: C40H69N9O6
  • MW: 772.03
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

D8-MMAE

D8-MMAE is a deuterated labeled MMAE, a potent mitotic inhibitor.

  • CAS Number: 2070009-72-0
  • MF: C39H59D8N5O7
  • MW: 726.03
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Monomethyl auristatin E

Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

  • CAS Number: 474645-27-7
  • MF: C39H67N5O7
  • MW: 717.979
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 873.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 482.1±34.3 °C

Paclitaxel-d5

Paclitaxel D5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].

  • CAS Number: 1129540-33-5
  • MF: C47H46D5NO14
  • MW: 858.93700
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

D-AMETHOPTERIN HYDRATE

Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].

  • CAS Number: 6745-93-3
  • MF: C20H24N8O6
  • MW: 472.45500
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 195ºC (dec.)(lit.)
  • Flash Point: N/A

Fmoc-MMAE

Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC[1].

  • CAS Number: 474645-26-6
  • MF: C54H77N5O9
  • MW: 940.22
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 1036.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 580.6±34.3 °C

Calicheamicin

Calicheamicin is a cytotoxic agent that causes double-strand DNA breaks.

  • CAS Number: 108212-75-5
  • MF: C55H74IN3O21S4
  • MW: 1368.348
  • Catalog: ADC Cytotoxin
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PNU-159682

PNU-159682, a highly potent metabolite of the anthracycline nemorubicin with outstanding cytotoxicity, is a potent ADCs cytotoxin.

  • CAS Number: 202350-68-3
  • MF: C32H35NO13
  • MW: 641.619
  • Catalog: ADC Cytotoxin
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 838.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 460.9±34.3 °C

S-Me-DM4

S-Me-DM4 is a metabolite of DM4 S-methylated by intracellular enzyme. DM4 (HY-100503) is a microtubule-depolymerizing maytansinoid with strong cytotoxicity. DM4 can be used as an ADC Cytotoxin molecule[1].

  • CAS Number: 890654-03-2
  • MF: C39H56ClN3O10S
  • MW: 794.39
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NMS-P528

NMS-P528 is a Duocarmycin derivative that can be used as an ADC payload. NMS-P528 can be used to synthesize NMS-P945[1].

  • CAS Number: 1466546-45-1
  • MF: C27H28ClN3O3S
  • MW: 510.05
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulysin IM-2

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.

  • CAS Number: 1032072-50-6
  • MF: C26H42N4O6S
  • MW: 538.70
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A