NMS-P118是一种有效的，口服可用的，高选择性的PARP-1抑制剂，在HeLa细胞中的IC₅₀值为0.04 μM。

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

Solid

PARP-1 9 nM (Kd) PARP-2 1390 nM (Kd)

NMS-P118 is found to be less myelotoxic in vitro than olaparib (now marketed as Lynparza), a dual PARP-1/-2 inhibitor. NMS-P118 proves to be metabolically stable, it modestly inhibites two cytochrome P450 family members (CYP-2B6 IC50: 8.15 μM; CYP-2D6 IC50: 9.51 μM) out of eight isoforms tested. Its ability in hampering the proliferation of bone marrow cells is from 5 to > 60 times lower then olaparib according to the species. has not independently confirmed the accuracy of these methods. They are for reference only.

NMS-P118 is a potent (K D =0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (K D =1.39 μM). NMS-P118 possesses excellent pharmacokinetic profile and nearly complete oral bioavailability both in mice and rats. It proved to be highly efficacious in vivo both as single agent in MDA-MB-436 human breast cancer tumors and in combination with temozolomide in CAPAN-1 human pancreatic tumors growing as xenografts in the mouse. The compound is well tolerated at highly efficacious doses and is endowed with an excellent ADME profile. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Papeo G, 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

In Vitro: DMSO : 16 mg/mL (40.46 mM; Need ultrasonic and warming)配制储备液