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 (89):

Cat. No. Product Name Effect Purity
  • HY-15142
    Doxorubicin hydrochloride 99.47%
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2]. Doxorubicin hydrochloride inhibits human DNA topoisomerase I with an IC50 of 0.8 μM[3].
  • HY-B0015
    Paclitaxel 99.97%
    Paclitaxel (Taxol) 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-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-14519
    Methotrexate 99.85%
    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-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-133571
    Aminohexylgeldanamycin
    Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activity[1].
  • HY-133541
    Glucopiericidin A
    Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2].
  • HY-133537
    Hygrolidin
    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].
  • HY-16560
    Camptothecin 98.62%
    Camptothecin (Campathecin) is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.
  • HY-13704
    SN-38 99.46%
    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.
  • HY-13062
    Daunorubicin Hydrochloride 99.37%
    Daunorubicin Hydrochloride (Daunomycin Hydrochloride; RP 13057 Hydrochloride; Rubidomycin Hydrochloride) is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin Hydrochloride (Daunomycin Hydrochloride; RP 13057 Hydrochloride; Rubidomycin Hydrochloride) inhibites DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.
  • HY-19792
    Mertansine 99.80%
    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-16261
    Aldoxorubicin
    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-13631D
    Dxd 98.20%
    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-19609
    Calicheamicin 98.44%
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor[1].
  • 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-15579A
    MMAF Hydrochloride 99.89%
    MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A[1][2][3].
  • HY-13061
    Daun02 98.05%
    Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
  • 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-15739
    Ansamitocin P-3 >98.0%
    Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.