化学信息：
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化学名
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2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
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简称
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MK4827
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别名
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Niraparib, MK 4827, MK-4827, Niraparib hydrochloride
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中文名
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N/A
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化学式
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C19H20N4O
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分子量
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320.39
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CAS号
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1038915-60-4
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO34mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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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.
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信号通路
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Cell Cycle; DNA Damage
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靶点
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PARP1
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PARP2
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－
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－
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－
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IC50
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3.8nM
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2.1nM
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－
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－
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－
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体外研究
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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.
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体内研究
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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.
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Jones P, et al. J Med Chem. 2009 Nov 26, 52(22), 7170-85.
2. Wang L, et al. Invest New Drugs. 2012 Dec, 30(6), 2113-20.
包装清单：
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产品编号
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产品名称
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包装
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SC6682-10mM
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MK4827 (RARP抑制剂)
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10mM×0.2ml
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SC6682-5mg
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MK4827 (RARP抑制剂)
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5mg
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SC6682-25mg
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MK4827 (RARP抑制剂)
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25mg
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—
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说明书
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1份
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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。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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