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-15142A
    Doxorubicin
    Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
    Doxorubicin
  • HY-112898
    DC1SMe
    ≥98.0%
    DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. 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.
    DC1SMe
  • HY-13062A
    Daunorubicin
    Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin
  • HY-129355
    Duocarmycin Analog
    Duocarmycin Analog is an analog of Duocarmycin, and used as an DNA alkylator and ADC cytotoxin.
    Duocarmycin Analog
  • HY-16560S
    Camptothecin-d5
    99.61%
    Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
    Camptothecin-d<sub>5</sub>
  • HY-160179
    Glucocorticoid receptor agonist-4
    99.80%
    Glucocorticoid receptor agonist-4 (Compound Preparation 5) is a glucocorticoid receptor agonist that can be conjugated to TNF-α antibodies for the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-4
  • HY-160097
    AXC-666
    99.75%
    AXC-666, an immune agonist, is a Imiquimod (HY-B0180) derivative. AXC-666 can be used for the synthesis of antibody-drug conjugate (ADC).
    AXC-666
  • HY-160177
    Glucocorticoid receptor agonist-3
    98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
  • HY-100503
    Maytansinoid DM4
    Maytansinoid DM4 is a thiol-containing maytansine derivative with highly potent cytotoxicity. Maytansinoid DM4 can be used as a cytotoxic moiety of ADC.
    Maytansinoid DM4
  • HY-103688
    N-Ac-γ-Calicheamicin-AcBut-NHS ester
    AcBut-N-Ac-γ-Calicheamicin is an ADC cytotoxic payload that induces cell cycle arrest and apoptosis by causing DNA double-strand breaks. AcBut-N-Ac-γ-Calicheamicin is primarily used in the synthesis of antibody-drug conjugates (ADC) and holds promise for research in the field of cancer, including acute lymphoblastic leukemia (ALL) and other hematological malignancies.
    N-Ac-γ-Calicheamicin-AcBut-NHS ester
  • HY-14648S5
    Dexamethasone-d3-1
    98.02%
    Dexamethasone-d3-1 (Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
    Dexamethasone-d<sub>3</sub>-1
  • HY-133571
    Aminohexylgeldanamycin
    99.56%
    Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.
    Aminohexylgeldanamycin
  • HY-126708
    Luisol A
    ≥99.0%
    Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, is an anthraquinone antibiotic analog.
    Luisol A
  • HY-100504
    S-methyl DM1
    99.58%
    S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects.
    S-methyl DM1
  • HY-160473
    TAM557
    TAM557 is a cytotoxic tubulysin compound that can be used in enzymatic conjugation reactions.
    TAM557
  • HY-132162
    7-MAD-MDCPT
    98.00%
    7-MAD-MDCPT, a Camptothecin analog, is a toxin payload in antibody drug conjugates (ADCs).
    7-MAD-MDCPT
  • HY-15584B
    Taltobulin hydrochloride
    99.34%
    Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
    Taltobulin hydrochloride
  • HY-B0015S1
    Paclitaxel-d5 (benzoyloxy)
    98.12%
    Paclitaxel-d5 (benzoyloxy) is the deuterium labeled Paclitaxel. 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[1][2].
    Paclitaxel-d<sub>5</sub> (benzoyloxy)
  • 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
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