Name | ERCC1-XPF-IN-1 |
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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 | |
Target |
IC50: 0.49 μM (ERCC1-XPF)[1] |
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. |
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]. |
References |
Molecular Formula | C28H32ClN5O2 |
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Molecular Weight | 506.04 |