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-129355
    Duocarmycin Analog
    Duocarmycin Analog is an analog of Duocarmycin, and used as an DNA alkylator and ADC cytotoxin.
    Duocarmycin Analog
  • 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-14519S
    Methotrexate-d3
    ≥99.0%
    Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
    Methotrexate-d<sub>3</sub>
  • HY-N7053
    Tubulysin M
    Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis.
    Tubulysin M
  • HY-14648G
    Dexamethasone (GMP)
    Dexamethasone (Hexadecadrol) (GMP) is Dexamethasone (HY-14648) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dexamethasone is an agonist of glucocorticoid receptor.
    Dexamethasone (GMP)
  • 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-156174
    E104
    E104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs.
    E104
  • 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-160177
    Glucocorticoid receptor agonist-3
    98.46%
    Glucocorticoid receptor agonist-3 (Preparation 6) is a glucocorticoid receptor agonist.
    Glucocorticoid receptor agonist-3
  • HY-145397S
    (4-NH2)-Exatecan-d5
    (4-NH2)-Exatecan-d5 is a deuterated labeled (4-NH2)-Exatecan. (4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (4-NH2)-Exatecan-d5
  • HY-156849
    Exatecan-methylacetamide-OH
    Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6).
    Exatecan-methylacetamide-OH
  • HY-128873
    Duocarmycin GA
    Duocarmycin GA is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-agent resistant cell lines.
    Duocarmycin GA
  • 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-156225
    MMAF-OtBu
    MMAF-OtBu (Example 2) is a modified MMAF (HY-15579 ). MMAF-OtBu can be used for synthesis of ADCs.
    MMAF-OtBu
  • 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-15584B
    Taltobulin hydrochloride
    98.34%
    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)
Cat. No. Product Name / Synonyms Application Reactivity

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