NMS-P118

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP19322CAS No. ：1262417-51-5Purity：98%

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CAS No.	1262417-51-5	Cat. No.	BCP19322
Name	NMS-P118
Synonyms
SMILES
Chemical Name
Formula	C20H24F3N3O2	M. Wt	395.42
Purity	98%	Storage	Store at 4-8°C
Description	InVitro: 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. InVivo: NMS-P118 is a potent (KD = 0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (KD = 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.