1. Antibody-drug Conjugate/ADC Related
  2. 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 (127):

Cat. No. Product Name Effect Purity
  • 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-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-15162
    Monomethyl auristatin E 99.92%
    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-14519
    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-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-145148
    Hemiasterlin derivative-1
    Hemiasterlin derivative-1 is a hemiasterlin derivative. Hemiasterlin derivative-1 can be used for the synthesis of the Antibody-drug conjugate (ADC)[1].
  • HY-78933
    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].
  • HY-15142A
    Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy[1][2]. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM[3].
  • HY-16560
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
  • HY-13631D
    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  • HY-19610
    α-Amanitin 99.79%
    α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
  • HY-19792
    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC)[1][2].
  • HY-13062
    Daunorubicin hydrochloride 99.37%
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin hydrochloride inhibits DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.
  • HY-15162A
    D8-MMAE 99.29%
    D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
  • HY-16261
    Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  • HY-19609
    Calicheamicin 98.28%
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor[1].
  • HY-12454
    DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
  • HY-15584
    Taltobulin 99.90%
    Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis[1].
  • HY-15579A
    MMAF hydrochloride 99.52%
    MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A[1][2][3].
  • HY-16700
    PNU-159682, a metabolite of the anthracycline nemorubicin, is a highly potent DNA topoisomerase I inhibitor with excellent cytotoxicity[1]. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis[2]. PNU-159682 can be used in EDV-nanocell technology to overcome drug resistance[3].