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MK-4827 (Niraparib)
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
货号 | CAS号 | 操作 |
---|---|---|
M127627-50mg | 1038915-60-4 | 询价 |
M127627-100mg | 1038915-60-4 | 询价 |
M127627-10mg | 1038915-60-4 | 询价 |
- 分子式 C19H20N4O
- 分子量320.39
属性
溶解性 | DMSO |
存贮条件 | 储存温度-20°C |
描述
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 |
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途