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-15583
    Auristatin F
    99.58%
    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-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-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.
    SN-38-d<sub>3</sub>
  • 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-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-15579A
    MMAF hydrochloride
    99.93%
    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.
    MMAF hydrochloride
  • 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-148185
    T01-1
    99.87%
    T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity.
    T01-1
  • 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.
    Ansamitocin P-3
  • 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-156617
    Cyclopropaneacetamide-Exatecan
    99.60%
    Cyclopropaneacetamide-Exatecan is an Exatecan (HY-13631) analogue and an ADC Cytotoxin. Cyclopropaneacetamide-Exatecan can be used to synthesize ADC molecules for cancer research.
    Cyclopropaneacetamide-Exatecan
  • HY-13631J
    (1R,9R)-Exatecan mesylate
    99.94%
    (1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research.
    (1R,9R)-Exatecan mesylate
  • HY-42487B
    (R)-Exatecan Intermediate 1
    99.95%
    (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-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-101160
    SG2057
    99.93%
    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-164285
    MYX1715
    99.14%
    MYX1715 is an inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. MYX1715 inhibits the proliferation of LU0884 and LU2511 with IC50 values of 44 nM and 9 nM. MYX1715 exhibits antitumor efficacy against neuroblastoma and gastric cancer in mouse models. MYX1715 can be used as ADC toxin.
    MYX1715
  • HY-B0015R
    Paclitaxel (Standard)
    Paclitaxel (Standard) is the analytical standard of Paclitaxel. This product is intended for research and analytical applications. 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.
    Paclitaxel (Standard)
  • 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-107769
    Duocarmycin TM
    99.82%
    Duocarmycin TM (CBI-TMI) is a potent antitumor antibiotic. Duocarmycin TM induces a sequence-selective alkylation of duplex DNA.
    Duocarmycin TM
  • 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
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