产品
编 号：F752238
分子式：C28H32ClN5O2
分子量：506.04
分子式：C28H32ClN5O2
分子量：506.04
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CAS No: 2411584-25-1
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
ERCC1-XPF-IN-1 (compound B7) (2 μM; 0-24 hours) significantly inhibits the removal of CPDs in UV-irradiated HCT-116 cells.ERCC1-XPF-IN-1 (5-20 μM; 72 hours) exhibits approximately 95% of the HCT116 cells survived at 5 μM.ERCC1-XPF-IN-1 (2 and 4 μM; 72 hours) significantly sensitizes HCT 116 cells to cyclophosphamide.
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.
体内研究：
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.
体外研究：
ERCC1-XPF-IN-1 (compound B7) (2 μM; 0-24 hours) significantly inhibits the removal of CPDs in UV-irradiated HCT-116 cells.ERCC1-XPF-IN-1 (5-20 μM; 72 hours) exhibits approximately 95% of the HCT116 cells survived at 5 μM.ERCC1-XPF-IN-1 (2 and 4 μM; 72 hours) significantly sensitizes HCT 116 cells to cyclophosphamide.
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