NMS-P118

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Chemical Structure| 1262417-51-5 同义名 : -
CAS号 : 1262417-51-5
货号 : A743839
分子式 : C20H24F3N3O2
纯度 : 98+%
分子量 : 395.42
MDL号 : MFCD30533610
存储条件：

Pure form

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • PARP1

    PARP1, Kd:0.009 μM

  • PARP1

    PARP1, Kd:0.009 μM
描述 NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor for cancer therapy with an IC50 of 0.04 μM in HeLa cell.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
HeLa cells Function assay 30 mins Inhibition of PARP1 in human HeLa cells assessed as reduction of H2O2-induced PAR formation preincubated for 30 mins followed by H2O2 addition measured after 15 mins by immunocytochemical analysis, IC50=0.04 μM 26222319
MDA-MB-436 cells Cytotoxicity assay 10 to 14 days Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining, IC50=0.14 μM 26222319
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.29mL

5.06mL

2.53mL
参考文献

[1]Papeo G, Posteri H, et al. Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl] -6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. J Med Chem. 2015 Sep 10;58(17):6875-98.