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-144585
    AGD-0182
    AGD-0182 is a microtubule disrupting agent. AGD-0182 is a synthetic analogue of the naturally occurring tubulin-binding molecule Dolastatin 10. AGD-0182 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.
    AGD-0182
  • HY-N0446R
    10-Methoxycamptothecin (Standard)
    10-Methoxycamptothecin (Standard) is the analytical standard of 10-Methoxycamptothecin. This product is intended for research and analytical applications. 10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and has been confirmed to possess high anti-cancer properties. 10-Methoxycamptothecin has higher cytotoxicity than 10-hydroxycamptothecin by testing antitumor activity against 2774 cell lines.
    10-Methoxycamptothecin (Standard)
  • HY-130996
    Diacetyl Agrochelin
    Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines.
    Diacetyl Agrochelin
  • HY-156516
    10NH2-11F-Camptothecin
    10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.
    10NH2-11F-Camptothecin
  • HY-14519CS
    (R)-Methotrexate-d3
    (R)-Methotrexate-d3 is the deuterium labeled (R)-Methotrexate.
    (R)-Methotrexate-d<sub>3</sub>
  • HY-178302
    TNF-α agonistic 2
    TNF-α agonistic 2 (Compound 009) is a toxic molecule. TNF-α agonistic 2 reduces the thickness of the right ear in mice. TNF-α agonistic 2 can be used as an ADC toxic molecule.
    TNF-α agonistic 2
  • HY-148231
    Dideoxy-amanitin
    Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM.
    Dideoxy-amanitin
  • HY-178226
    PBX-7016
    PBX-7016 is a Camptothecin (HY-16560) derivative. PBX-7016 can selectively inhibit Topoisomerase 1. PBX-7016 can specifically bind and degrade the cancer protein DDX5, thereby down-regulating the expression of anti-apoptotic proteins such as Survivin, Mcl-1, and XIAP, and promoting the apoptosis of cancer cells. PBX-7016 can be used to synthesis of ADCs.
    PBX-7016
  • HY-P1126
    Dolastatin 15
    Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
    Dolastatin 15
  • HY-19826
    Isofistularin-3
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
    Isofistularin-3
  • HY-13631T
    (1R,9S)-Exatecan
    (1R,9S)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    (1R,9S)-Exatecan
  • HY-157078
    Eg5-IN-2
    Eg5-IN-2 (Compound Scaffold B (4)) is an Eg5 inhibitor (IC50: < 0.5 nM). Eg5-IN-2 can be used as an ADC payload for synthesis of ADCs.
    Eg5-IN-2
  • HY-164107
    Auristatin S
    Auristatin S is an Auristatin payload with potent antitumor activity. Auristatin S attenuates bystander activity with improved off-target toxicity. Auristatin S has excellent tolerability in Karpas/KarpasBVR cell models. Auristatin S can be used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
    Auristatin S
  • HY-129356
    Seco-Duocarmycin SA
    Seco-Duocarmycin SA is a DNA alkylator. Seco-Duocarmycin SA is an antitumor antibiotic (IC50 = 10 pM). Seco-Duocarmycin SA can induce a concentration-dependent increase in apoptotic cell death. Seco-Duocarmycin SA can lead to significant cell cycle arrest in S and G2/M phases. Seco-Duocarmycin SA acts as an ADC cytotoxin for antibody-drug conjugates.
    Seco-Duocarmycin SA
  • HY-171081
    Glucocorticoid receptor agonist-6
    Glucocorticoid receptor agonist-6 (Compound A) is a Glucocorticoid receptor (GR) agonist. Glucocorticoid receptor agonist-6 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).
    Glucocorticoid receptor agonist-6
  • HY-126665A
    DMEA-PNU-159682 dichloroacetate
    DMEA-PNU-159682 (molecule D12) dichloroacetate is an ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682.
    DMEA-PNU-159682 dichloroacetate
  • HY-177285
    NVP-BQS481
    NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).
    NVP-BQS481
  • HY-N2346
    Tubulysin E
    Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis.
    Tubulysin E
  • HY-178315
    Exatecan analog 38
    Exatecan analog 38 is a camptothecin derivative with potent topoisomerase I inhibitory activity. Exatecan analog 38 can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan analog 38 can be used for cancer research.
    Exatecan analog 38
  • HY-P5748
    Bac5(1-25)
    Bac5(1-25) is an N-terminal fragment of the bovine proline-rich antimicrobial peptide Bac5.
    Bac5(1-25)
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