NMS-P118是可口服的高选择性PARP-1抑制剂，用于癌症治疗，在HeLa细胞中的IC50值为0.04 μM。

NMS-P118 is a potent, selective and orally available Inhibitor of PARP-1 for cancer therapy.

NMS-P118 proved to be a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles and high efficacy in vivo both as a single agent and in combination with Temozolomide in MDA-MB-436 and Capan-1 xenograft models, respectively. Cocrystal structures of 20by with both PARP-1 and PARP-2 catalytic domain proteins allowed rationalization of the observed selectivity.

1262417-51-5

C20H24F3N3O2

395.426

DMSO:16 mg/mL (40.46 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years