MK-4827 (Niraparib)-分析测试百科网

溶解性	DMSO
存贮条件	储存温度-20°C

产品介绍	MK-4827(Niraparib)是高活性PARP1/PARP2抑制剂，IC50分别为3.8 nM/2.1 nM，在BRCA-1和BRCA-2突变型肿瘤细胞中具有很好的活性，比对PARP3，V-PARP和Tank1的抑制性高330倍以上。
备注	MK-4827 is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Phase 3.
生化机理	MK-4827 is a potent, selective, PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively. MK-4827 possesses potential antineoplastic activity. In a whole cell assay, MK-4827 prevented PARP activity with an EC50 of 4 nM, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. MK-4827 induces selective synthetic lethality in homologous recombination (HR) repair deficient tumors with BRCA1/2 loss and tumor cell lines with non-BRCA-related HR defects, supporting clinical utility in sporadic tumors. MK-4827 reveals good pharmacokinetic properties and is currently in phase I clin. trials. The phase I clinical trials for MK-4827 is ongoing in the treatment of solid tumors.
别名	2-[4-((3S)-3-哌啶基)苯基]-2H-吲唑-7-甲酰胺;Niraparib;MK 4827;MK4827;2-[4-((3S)-3-Piperidinyl)phenyl]-2H-indazole-7-carboxamide