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-15162A
    MMAE-d8
    99.29%
    MMAE-d8 is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
    MMAE-d<sub>8</sub>
  • HY-13580
    Budesonide
    99.75%
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
    Budesonide
  • HY-19609
    Calicheamicin
    98.28%
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor. Calicheamicin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Calicheamicin
  • HY-13631DS
    Dxd-d5
    98.84%
    Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
    Dxd-d<sub>5</sub>
  • HY-14648A
    Dexamethasone acetate
    99.84%
    Dexamethasone acetate (Dexamethasone 21-acetate) 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 acetate
  • HY-W021377
    Exatecan Intermediate 2
    99.99%
    Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
    Exatecan Intermediate 2
  • HY-14519A
    Methotrexate disodium
    99.71%
    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, 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).
    Methotrexate disodium
  • HY-101161
    SG3199
    98.94%
    SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).
    SG3199
  • HY-16700
    PNU-159682
    98.25%
    PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
    PNU-159682
  • HY-145397
    (4-NH2)-Exatecan
    99.93%
    (4-NH2)-Exatecan, a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs) (US20200306243A1, compound A).
    (4-NH2)-Exatecan
  • HY-16261
    Aldoxorubicin
    Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
    Aldoxorubicin
  • HY-15142R
    Doxorubicin (hydrochloride) (Standard)
    Doxorubicin hydrochloride (Standard) is the analytical standard of Doxorubicin hydrochloride. This product is intended for research and analytical applications. Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.
    Doxorubicin (hydrochloride) (Standard)
  • HY-15582
    Auristatin E
    99.82%
    Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids.
    Auristatin E
  • HY-44369
    Exatecan Intermediate 6
    98.92%
    Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 6
  • HY-128915
    Duocarmycin DM free base
    99.69%
    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-B0154
    Fluticasone (propionate)
    99.82%
    Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity.
    Fluticasone (propionate)
  • HY-132180A
    Seco-DUBA
    98.08%
    Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs).
    Seco-DUBA
  • 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-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-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
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