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-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.
    Taltobulin
  • HY-14573
    SJG-136
    99.47%
    SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.
    SJG-136
  • 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-107769
    Duocarmycin TM
    98.04%
    Duocarmycin TM (CBI-TMI) is a potent antitumor antibiotic. Duocarmycin TM induces a sequence-selective alkylation of duplex DNA.
    Duocarmycin TM
  • 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-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-156856
    FL118-14-Propanol
    98.69%
    FL118-14-Propanol is a FL118 derivative. FL118-14-Propanol synthesized ADC molecule has good anti-tumor effect in mice.
    FL118-14-Propanol
  • 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-101160
    SG2057
    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-13631AG
    Exatecan (mesylate) (GMP)
    Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan 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) (GMP)
  • HY-148185
    T01-1
    98.80%
    T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity.
    T01-1
  • HY-148819A
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) hydrochloride 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.
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
  • 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-B0018
    Docetaxal
    99.54%
    Docetaxal (10-Acetyl docetaxel) is an analog of Docetaxel (HY-B0011), with anticancer activity. Docetaxel is a microtubule disassembly inhibitor, with antimitotic activity.
    Docetaxal
  • HY-12456
    Duocarmycin SA
    99.55%
    Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
    Duocarmycin SA
  • HY-156617
    Cyclopropaneacetamide-Exatecan
    Cyclopropaneacetamide-Exatecan (Compound 2-A) is an ADC Cytotoxin and an Exatecan analogue. Cyclopropaneacetamide-Exatecan can be used in the synthesis of ADC such as anti-B7H3 antibody-Exatecan analogue conjugate (compound ADC-2).
    Cyclopropaneacetamide-Exatecan
  • 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
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