| Description |
ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells[1].
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| Related Catalog |
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| Target |
IC50: 0.49 μM (ERCC1-XPF)[1]
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| In Vitro |
ERCC1-XPF-IN-1 (compound B7) (2 μM; 0-24 hours) significantly inhibits the removal of CPDs in UV-irradiated HCT-116 cells[1]. ERCC1-XPF-IN-1 (5-20 μM; 72 hours) exhibits approximately 95% of the HCT116 cells survived at 5 μM[1]. ERCC1-XPF-IN-1 (2 and 4 μM; 72 hours) significantly sensitizes HCT 116 cells to cyclophosphamide[1]. Cell Cytotoxicity Assay Cell Line: HCT-116[1] Concentration: 5, 10, 15 and 20 μM Incubation Time: 72 hours Result: Exhibited approximately 95% of the HCT116 cells survived at 5 μM.
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| In Vivo |
ERCC1-XPF-IN-1 has a moderate rate of metabolism in human liver microsomes, with log D value of 2.01 at pH 7.4 and an efflux ratio ≥ 43.39[1].
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| References |
[1]. Elmenoufy AH, Gentile F, Jay D, et al. Design, synthesis and in vitro cell-free/cell-based biological evaluations of novel ERCC1-XPF inhibitors targeting DNA repair pathway. Eur J Med Chem. 2020;204:112658.
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