物质信息
ID:73018
名称和标识
IUPAC传统名
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-1,3-benzodiazole-4-carboxamide
别名
VeliparibABT-888
IUPAC标准名
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-1,3-benzodiazole-4-carboxamide
数据登录号
CAS号
化合物性质
产品相关信息
成盐信息
Free Base
理化性质
溶解度
DMSO
安全信息
保存条件
-20°C
药理学性质
作用靶点
PARP
描述信息
Research Area
Description
Cancer
Protocol
Kinase Assay [1]
In vitro PARP assays
PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.
Cell Assay []
Animal Study [1]
Animal Models
NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
Formulation
Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
Doses
~25 mg/kg
Administration
Orally administered
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参考文献
• Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.
• Clark CC, et al. Mol Cancer Ther, 2012 Jul 9.
• Horton TM, et al. ASCO Annual Meeting, 2007, Abs 9528.
• Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737.
• Horton TM, et al. 2007 ASCO Annual Meeting, Abstract 9528.
• Liu X, et al. Mol Cancer Res, 2009, 7(10), 1686-1692.
• Penning TD, et al, J Med Chem, 2009, 52(2), 514-523.
• Albert JM, et al, Clin Cancer Res, 2007, 13(10), 3033-3042.
• Palma JP, et al. Clin Cancer Res, 2009, 15(23), 7277-7290.
• Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.