1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. ADC Cytotoxin

ADC Payload

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147408
    Rezetecán
    99.60%
    Rezetecán (SHR9265) is a topoisomerase I inhibitor. In addition, Rezetecán can be used to synthesize Trastuzumab rezetecan, an antineoplastic agent. Rezetecán can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
    Rezetecán
  • HY-145674
    HDP 30.1699
    99.13%
    HDP 30.1699, the derivative of α-Amanitin, shows considerable cross-links. The cysteine residues of the anti-HER2 THIOMAB antibody are used for conjugation of the cysteine reactive linker–Amanitin compound, HDP 30.1699, with a cleavable linker by maleimide chemistry.
    HDP 30.1699
  • HY-147179
    INX-SM-56
    99.47%
    INX-SM-56 is a cytotoxin that can be used for the synthesis of anti-VISTA antibody agent conjugate. VISTA: V-region Immunoglobulin-containing Suppressor of T cell Activation.
    INX-SM-56
  • HY-43565B
    Exatecan intermediate 10
    99.92%
    Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM (0.975 μg/mL) for use in cancer research.
    Exatecan intermediate 10
  • HY-15583S
    Auristatin F-d8
    99.82%
    Auristatin F-d8 is deuterium labeled Auristatin F (HY-15583). Auristatin F is a potent cytotoxin in antibo-conjugated agents and an analogue of MMAF. Auristatin F is a potent microtubule inhibitor and vascular damaging agent (VDA). Auristatin F inhibits cell division by preventing tubulin aggregation.Auristatin F can be used in antibody-drug conjugates (ADC) .
    Auristatin F-d<sub>8</sub>
  • HY-15584A
    Taltobulin trifluoroacetate
    99.08%
    Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
    Taltobulin trifluoroacetate
  • HY-W021377C
    Exatecan Intermediate 4 dihydrochloride
    99.92%
    Exatecan Intermediate 4 dihydrochloride (Compound 14f) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
    Exatecan Intermediate 4 dihydrochloride
  • HY-402091
    SJG-136 intermediate-1
    99.95%
    SJG-136 intermediate-1 (compound 19) is an intermediate for synthesizing SJG-136. SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA.
    SJG-136 intermediate-1
  • HY-78932
    Dap-NE
    Dap-NE is an intermediate reagent in the synthesis of the ADC toxin Monomethyl auristatin E (HY-15162).
    Dap-NE
  • HY-42487A
    (rac)-Exatecan Intermediate 1
    99.84%
    (rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer.
    (rac)-Exatecan Intermediate 1
  • HY-13631P
    Exatecan mesylate dihydrate
    Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Exatecan mesylate dihydrate
  • HY-15582G
    Auristatin E (GMP)
    Auristatin E (GMP) is Auristatin E (HY-15582) produced by using GMP guidelines. Auristatin E is a tubulin polymerization inhibitor.
    Auristatin E (GMP)
  • HY-12455
    Duocarmycin A
    Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
    Duocarmycin A
  • HY-16261C
    Aldoxorubicin hydrochloride
    Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
    Aldoxorubicin hydrochloride
  • HY-100861
    C-11
    C-11 is a tubulin inhibitor and acts as an ADC cytotoxin, displays cytotoxicity for carcinoma cell lines.
    C-11
  • 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).
    DGN462
  • HY-145609
    Debotansine
    Debotansine is a immunomodulator and antineoplastic.
    Debotansine
  • 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.
    DC1
  • 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 agent conjugates (ADCs) toxin.
    (+)-CBI-CDPI1
  • 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.
    DM3-SMe
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