化学信息：
| 化学名 | 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide |
|
| 简称 | MK4827 | |
| 别名 |
Niraparib, MK 4827, MK-4827, Niraparib hydrochloride |
|
| 中文名 | N/A | |
| 化学式 | C19H20N4O | |
| 分子量 | 320.39 | |
| CAS号 | 1038915-60-4 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO34mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.56ml DMSO，或者每3.2mg加入1ml DMSO，配制成10mM溶液。SC6682-10mM用DMSO配制。 |
生物信息：
| 产品描述 | MK-4827 (Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8nM/2.1nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1. | ||||
| 信号通路 | Cell Cycle; DNA Damage | ||||
| 靶点 | PARP1 | PARP2 | － | － | － |
| IC50 | 3.8nM | 2.1nM | － | － | － |
| 体外研究 | MK-4827 displays excellent PARP 1 and 2 inhibition with IC(50)=3.8 and 2.1nM, respectively, and in a whole cell assay, it inhibits PARP activity with EC(50)=4nM and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100nM range. | ||||
| 体内研究 | MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement of radiation response is observed in clinically relevant radiation-dose fractionation schedules. The therapeutic window during which time MK-4827 interacts with radiation lasts for several hours. These biological attributes make translation of this therapeutic combination treatment feasible for translation to the treatment of a variety of human cancers. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SC6682-10mM | MK4827 (RARP抑制剂) | 10mM×0.2ml |
| SC6682-5mg | MK4827 (RARP抑制剂) | 5mg |
| SC6682-25mg | MK4827 (RARP抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
