1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. ADC Payload

ADC Cytotoxin

ADC 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 payload. The payload is the most important component as it determines the potency to kill cancer cells of an ADC.

There are many payloads 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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14519R
    Methotrexate (Standard)
    Methotrexate (Standard) is the analytical standard of Methotrexate. This product is intended for research and analytical applications. 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).
    Methotrexate (Standard)
  • HY-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
    99.73%
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader (MZ 1 (HY-107425) analog) and PEG-based linker. PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can be used for the research of HER2-positive breast cancer.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-160885A
    NH2-Gly-PAB-Exatecan-D-glucuronic acid formic
    99.34%
    NH2-Gly-PAB-Exatecan-D-glucuronic acid formic (Compound 8) is the formic salt form of H2N-Gly-PAB-Exatecan-D-glucuronic acid. H2N-Gly-PAB-Exatecan-D-glucuronic acid formic is an intermediate, which reacts with NHS group to form drug-linker conjugate for ADC, Mal-Gly-PAB-Exatecan-D-glucuronic acid (HY-153179).
    NH2-Gly-PAB-Exatecan-D-glucuronic acid formic
  • 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-148818
    S-Me-DM4
    99.94%
    S-Me-DM4 is a metabolite of DM4 S-methylated by intracellular enzyme. DM4 (HY-100503) is a microtubule-depolymerizing maytansinoid with strong cytotoxicity. DM4 can be used as an ADC Cytotoxin molecule.
    S-Me-DM4
  • HY-19474
    Maytansinol
    99.49%
    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-15995
    Tubulysin A
    99.56%
    Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin.
    Tubulysin A
  • HY-144880
    SC209
    98.99%
    SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules.
    SC209
  • HY-156856S
    FL118-14-Propanol-d5
    FL118-14-Propanol-d5 is the deuterium labeled FL118-14-Propanol (HY-156856). FL118-14-Propanol is a FL118 derivative. FL118-14-Propanol synthesized ADC molecule has good anti-tumor effect in mice.
    FL118-14-Propanol-d<sub>5</sub>
  • HY-15580
    Dolastatin 10
    98.34%
    Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.
    Dolastatin 10
  • HY-117371
    Hemiasterlin
    99.90%
    Hemiasterlin ((-)-Hemiasterlin) is an antimitotic marine natural product with potent anticancer effects. Hemiasterlin can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
    Hemiasterlin
  • HY-400708
    (R)-Benzyl 2-cyclopropyl-2-hydroxyacetate
    99.08%
    (R)-Benzyl 2-cyclopropyl-2-hydroxyacetate can be used in the synthesis of pyrrolidines, a relevant molecule for ADC applications.
    (R)-Benzyl 2-cyclopropyl-2-hydroxyacetate
  • HY-126663
    N-Me-L-Ala-maytansinol
    99.89%
    N-Me-L-Ala-maytansinol is a hydrophobic, cell permeable payload used for making antibody-drug conjugate (ADC).
    N-Me-L-Ala-maytansinol
  • HY-78933
    Fmoc-MMAE
    99.35%
    Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC.
    Fmoc-MMAE
  • HY-43564
    Exatecan Intermediate 5
    99.98%
    Exatecan Intermediate 5 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 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 5
  • HY-19791
    N-Acetyl-Calicheamicin
    99.94%
    N-Acetyl-Calicheamicin (N-Acetyl-Calicheamicin γ), an enediyne anti-tumor antibiotic, is an ADC cytotoxin. N-Acetyl-Calicheamicin can induce DNA damage, and can be used in the synthesis of ADC.
    N-Acetyl-Calicheamicin
  • HY-128914
    Tubulysin
    99.60%
    Tubulysin is a microtubule destabilizer that binds to the β-tubulin peptide site adjacent to the vinca alkaloid binding site and inhibits tubulin polymerization. Tubulysin induces apoptosis and exhibits antiproliferative activity against a variety of human cancer cells, including multidrug-resistant strains. Tubulysin can be conjugated to antibodies via a disulfide-containing quaternary ammonium linker for ADC synthesis. Tubulysin is applicable to tumor-related research.
    Tubulysin
  • HY-145149
    Duostatin 5
    99.76%
    Duostatin 5 is a ADC Cytotoxin designed based on MMAF (HY-15579) and can be used to synthesize ADCs. The preparation of Duostatin 5 has the advantages of fewer synthetic steps, simple operation, less difficulty in quality control, and more stable chemical synthesis process. Duostatin 5 can be linked to the antibody targeting 5T4 (ZV05) by cross-linking with interchain cysteines through a disubstituted C-Lock linker. Duostatin 5 is a click chemistry reagent. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-driven alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups[1][2].
    Duostatin 5
  • 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-156174
    E104
    99.38%
    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
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