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

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-129589
    Thailanstatin A
    99.71%
    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.
    Thailanstatin A
  • HY-128915
    Duocarmycin DM free base
    98.04%
    Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.
    Duocarmycin DM free base
  • HY-12522
    PF-06380101
    99.47%
    PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
    PF-06380101
  • HY-145449
    CC-885-CH2-PEG1-NH-CH3
    99.22%
    CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC).
    CC-885-CH2-PEG1-NH-CH3
  • HY-15583
    Auristatin F
    99.44%
    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
  • HY-114936
    Piericidin A
    ≥99.0%
    Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.
    Piericidin A
  • 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.
    Ansamitocin P-3
  • HY-15580
    Dolastatin 10
    98.11%
    Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.
    Dolastatin 10
  • HY-19474
    Maytansinol
    99.84%
    Maytansinol (Ansamitocin P-0) is a derivative of Maytansine. Maytansinol can inhibit tubulin polymerization and induce apoptosis. Maytansinol has antitumor activity. Maytansinol can be used in cancer drug research.
    Maytansinol
  • HY-13704S
    SN-38-d3
    99.07%
    SN-38-d3 is the 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].
    SN-38-d<sub>3</sub>
  • HY-101160
    SG2057
    98.67%
    SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.
    SG2057
  • HY-148424
    PBD dimer-2
    98.03%
    PBD dimer-2 (compound 2c) is a C8-linked pyrrolobenzodiazepine dimer. PBD dimer-2 can span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. PBD dimer-2 can be used as a payload for antibody–agent conjugates (ADCs), and it can be used for the research of cancer.
    PBD dimer-2
  • HY-13061
    Daun02
    98.72%
    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.
    Daun02
  • HY-125586
    β-Amanitin
    β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
    β-Amanitin
  • HY-42487B
    (R)-Exatecan Intermediate 1
    (R)-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.
    (R)-Exatecan Intermediate 1
  • HY-148185
    T01-1
    98.80%
    T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity.
    T01-1
  • HY-15579AS
    MMAF-d8 hydrochloride
    99.70%
    MMAF-d8 (hydrochloride)e is a deuterated form of MMAF hydrochloride, which is a microtubule disrupting agent.
    MMAF-d<sub>8</sub> hydrochloride
  • HY-19791
    N-Acetyl-Calicheamicin
    99.39%
    N-Acetyl-Calicheamicin (N-Acetyl-Calicheamicin γ), an enediyne anti-tumor antibiotic, is an ADC cytotoxin. N-Acetyl-Calicheamicin can induce DNA damage, and can be used in the synthesis of ADC.
    N-Acetyl-Calicheamicin
  • HY-79256
    MMAF-OMe
    99.62%
    MMAF-Ome, an antitubulin agent, is also an ADC cytotoxin. MMAF-Ome inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively.
    MMAF-OMe
  • HY-144880
    SC209
    99.52%
    SC209, an ADC cytotoxin extracted from patent WO2021247798, is used in synthesis of anti-EGFR antibody-drug conjugate ADC. SC209 is a metabolite of STRO-002.
    SC209
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