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 |
MK-4827( 尼拉帕尼)
MK-4827 (Niraparib) (订货以英文为准)
编号:M127627
CAS号:1038915-60-4
分子式:C19H20N4O
分子量:320.39
产品名称 | MK-4827 (Niraparib) |
中文名称 | MK-4827( 尼拉帕尼) |
CAS号 | 1038915-60-4 |
分子式(M.F.) | C19H20N4O |
分子量(M.W.) | 320.39 |
储存条件 | -20°C储存 |
标识符号 | https://www.aladdin-e.com/images/ghs/ghs08.jpg |
信号词 | Danger |
危害声明 | H360 |
警示性声明 | P201-P308 + P313 |
个人防护设备 | Eyeshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges |
RTECS | TU5570250 |
WGK德国 | 3 |
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