ERCC1-XPF-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ERCC1-XPF-IN-1 

ERCC1-XPF-IN-1 是一种有效且具有高亲和力的 ERCC1-XPF 抑制剂,IC50 为 0.49 μM。ERCC1-XPF-IN-1 通过抑制 CPDs 的去除、以及环磷酰胺对结直肠癌细胞的毒性,增强了 UV 辐射的细胞毒性作用,抑制 DNA 修复。

ERCC1-XPF-IN-1

ERCC1-XPF-IN-1 Chemical Structure

CAS No. : 2411584-25-1

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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[1].

IC50 & Target

IC50: 0.49 μM (ERCC1-XPF)[1]

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

506.04

Formula

C28H32ClN5O2

CAS 号

2411584-25-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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