Niraparib (MK-4827)
商品编号:
TS0095
备注:
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详细介绍
l 基本信息 |
产品名称 | 尼拉帕尼(Niraparib (MK-4827)) |
一般描述 | Niraparib(尼拉帕尼) is an orally bioavailable inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and -2), with antineoplastic activity. |
别 称 | 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide |
纯 度 | ≥98.0%(HPLC) | CAS NO. | 1038915-60-4 |
分子式 | C19H20N4O | 分子量 | 320.39 |
适用范围 | 生物试剂,适用于细胞培养等 |
l 理化信息 |
外 观 | 固体 |
溶解性(25℃) | DMSO | ≥50mg/mL |
乙醇 | ≥50mg/mL |
水 | Insoluble |
l 生物学信息 |
生物活性/药理作用 | Niraparib is an orally bioavailable inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and
-2), with antineoplastic activity. Upon administration, niraparib binds to and inhibits the activity of PARP-1 and -2, thereby inhibiting PARP-1 and
-2-mediated DNA repair, enhancing the accumulation of DNA strand breaks, promoting genomic instability and resulting in apoptosis. The PARP family of proteins catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks. Niraparib 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. |
l 存储 |
存储温度 | -20℃ |
l 注意事项及免责声明 |
本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。 |
l 参考文献 |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |