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Bystander activity

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6

Inhibitors & Agonists

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Fluorescent Dye

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-164729
    FZ-AD005

    		Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis Cancer
    FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
    FZ-AD005
  • HY-163099
    P5(PEG24)-VC-PAB-Exatecan

    		Drug-Linker Conjugates for ADC Topoisomerase Apoptosis Cancer
    P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
    P5(PEG24)-VC-PAB-Exatecan
  • HY-176976
    Exatecan-mpGNNG

    		Drug-Linker Conjugates for ADC Cancer
    Exatecan-mpGNNG (Compound 10a) is the linker-payload component of an antibody-drug conjugate (ADC). Exatecan-mpGNNG is composed of Exatecan (HY-13631), a potent topoisomerase I inhibitor, and the linker .
    Exatecan-mpGNNG
  • HY-164107
    Auristatin S

    		ADC Payload Microtubule/Tubulin Cancer
    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-126218
    HSV-TK substrate

    		HSV Cancer
    HSV-TK substrate is a substrate for HSV-TK, and induces multi-log cytotoxicity in HSV-TK-expressing and bystander cells. HSV-TK substrate shows antitumor activity .
    HSV-TK substrate
  • HY-182623
    WB214

    		MDM-2/p53 Cancer
    WB214 is an MDM2 and GSPT1 degrader with human MDM2 Ki >10 μM. WB214 induces a neo-interaction between MDM2 and the cereblon E3 ligase complex, triggering MDM2 ubiquitination, proteasomal degradation, and bystander p53 degradation, and does not bind MDM2’s p53 binding region. WB214 induces GSPT1 degradation, and exhibits anti-proliferative activity in leukemia cells. WB214 can be used for the research of leukemia .
    WB214

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