NMS-P515 是有效的、口服有效的、立体定向的PARP-1 的抑制剂，Kd 值为16 nM，IC50 值为 27 nM (Hela 细胞中)。有抗肿瘤活性。
CAS：1262395-13-0
分子式：C21H29N3O2
分子量：355.47
纯度：98%
存储：Store at -20°C

Background:

NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity[1]. PARP-1|16 nM (Kd)|PARP-1|27 nM (IC50, in Hela cells)

NMS-P515 (80 mg/kg, orally daily for 12 days) exhibits potent antitumor activity in mouse models based pancreatic cancer[1]. Animal Model: Subcutaneously implanted Capan-1 pancreatic (BRCA2-mutated) mouse xenografts[1].

[1]. Papeo G, et al. Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515. ACS Med Chem Lett. 2019 Mar 13;10(4):534-538.