[S(R)]-N-[(1R)-1-[2-(二苯基膦)苯基]乙基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[2-(二环己基膦)苯基](5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[3,5-二叔丁基-4-甲氧基苯基][2-(二环己基膦)苯基]甲基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(1S)-1-[2-(二环己基膦)苯基]乙基]-N-甲基-2-叔丁基亚磺酰胺
[S(R)]-N-[(1S)-1-[2-(9-蒽基)苯基]-2-(二苯基膦)乙基]-N-甲基-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[2-(二苯基膦)苯基]苯基甲基]-N-甲基-2-叔丁基亚磺酰胺
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 |