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NMS-P118

CAS No. : 1262417-51-5

MCE 站：NMS-P118

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  XAV-939  |  Rucaparib  |  PJ34  |  3-Aminobenzamide  |  G007-LK  |  Dehydrocorydaline chloride  |  AG14361  |  Iniparib  |  AZD-2461  |  BGP-15  |  Fucosterol  |  JW 55  |  EB-47 dihydrochloride  |  UPF 1069  |  AZ6102  |  iRucaparib-AP6  |  ME0328  |  MN-64  |  5,?7,?4'-?Trimethoxyflavone  |  Benzamide  |  GeA-69  |  Paris saponin VII  |  PARP14 inhibitor H10  |  BYK204165  |  NU1025  |  Oroxin A

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