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.