AT7519,CDK抑制剂

AT7519 (订货以英文为准)

编号:A127001
CAS号:844442-38-2
分子式:C16H17N5O2CL2
分子量:382.24
货号 品牌 包装 目录价 您的价格 库存 数量 购买
A127001-25mg 阿拉丁 25mg ¥2059.90
A127001-5mg 阿拉丁 5mg ¥520.90
A127001-100mg 阿拉丁 100mg ¥6385.90
产品名称 AT7519
中文名称 AT7519,CDK抑制剂
CAS号 844442-38-2
分子式(M.F.) C16H17N5O2CL2
分子量(M.W.) 382.24
储存条件 -20°C储存
溶解性Soluble in DMSO (10 mg/ml) at 25°C, water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25°C.
存贮条件储存温度-20°C
应用A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6.
产品介绍AT7519是多种CDK抑制剂,作用于CDK1, 2, 4, 6和9时,IC50为10-210 nM,对CDK3作用效果稍弱,对CDK7几乎没有抑制活性。Phase 2。
备注AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. Phase 1.
生化机理AT7519 is a novel small molecule effective as a multi-cyclin-dependent kinase inhibitor for Cdk1/cyclin B (IC50 = 210 nM), Cdk2/Cyclin A (IC50 = 47 nM), Cdk3/Cyclin E (IC50 = 360 nM), Cdk4/Cyclin D1 (IC50 = 100 nM), Cdk5/p35 (IC50 = 13 nM) and Cdk6/Cyclin D3 (IC50 = 170 nM). AT7519 is an ATP competitive Cdk inhibitor with a Ki value of 38 nM for Cdk1. AT7519 is inactive against all non-Cdk kinases with the exception of GSK3β (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription.
别名N-(4-哌啶基)-4-(2,6-二氯苯甲酰氨基)-1H-吡唑-3-甲酰胺;AT 7519;AT-7519;4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide;N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide
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