2. Antibody-drug Conjugate/ADC Related
  3. ADC Cytotoxin

ADC Cytotoxin

ADC cytotoxins (also known as payloads) are cytotoxic agents that induce target cell death in Antibody Drug Conjugates (ADCs). An ADC is a targeted agent composed with a monoclonal antibody, a linker and a cytotoxin. The cytotoxin is the most important component as it determines the potency to kill cancer cells of an ADC.

There are many cytotoxins which are currently being used such as Calicheamicins, Duocarmycins, Pyrrolobenzodiazepines (PBDs), Camptothecins, Daunorubicins/Doxorubicins, Auristatins and Maytansinoids. They can be divided in two classes based on their mechanism of action, DNA damaging agents and tubulin inhibitors. Among them Calicheamicins, Duocarmycins and PBDs are DNA minor grove binders, Camptothecins and Daunorubicins/Doxorubicins are topoisomerase inhibitors, which are DNA damaging agents. Auristatins and Maytansinoids are tubulin inhibitors. Except for the listed cytotoxins, there are numbers of traditional cytotoxic agents with similar mechanisms of killing cancer cells and can also be used in the development of ADCs.

ADC Cytotoxin Related Products (150):

Cat. No. Product Name Effect Purity
  • HY-15162
    Monomethyl auristatin E 99.94%
    Monomethyl auristatin E (MMAE; SGD-1010) 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.
  • HY-15142
    Doxorubicin hydrochloride
    Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2][3].
  • HY-14519
    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].
  • HY-B0015
    Paclitaxel 99.97%
    Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].
  • HY-13704
    SN-38 99.80%
    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].
  • HY-148870
    Maytansinoid B
    Maytansinoid B is a kind of ADC Cytotoxin. Maytansinoid B can be used to conjugates with antibodies to form Antibody-Drug Conjugates (ADCs). Maytansinoids are known as antimitotic agents, binding to tubulin and inhibiting microtubule assembly. Maytansinoids induces G2/M arrest in the cell cycle to induce apoptosis[1][2].
  • HY-148818
    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].
  • HY-148819
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro[1].
  • HY-101150
    DGN462
    DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1].
  • HY-147281
    BAY 1135626
    BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–drug conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].
  • HY-101150A
    sulfo-DGN462 sodium
    sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML)[1].
  • HY-112899
    DC1
    DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
  • HY-129589
    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].
  • HY-130996
    Diacetyl Agrochelin
    Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines[1].
  • HY-130080
    DM3
    DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs)[1].
  • HY-14519A
    Methotrexate disodium 99.71%
    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].
  • HY-14519CS
    (R)-Methotrexate-d3
    (R)-Methotrexate-d3 is the deuterium labeled (R)-Methotrexate[1].
  • HY-128880
    (+)-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.
  • HY-130081
    DM3-SMe
    DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM[1][2].
  • HY-148231
    Dideoxy-amanitin
    Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM[1].