产品属性：
产品名称 | 规格 | CAS号 | 型号 |
AT7519 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg | 844442-38-2 | EY-Y0165163 |
Cas No.844442-38-2
别名
化学名 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide
分子式 C16H17Cl2N5O2
分子量 382.24
溶解度 ≥ 9.55mg/mL in DMSO with gentle warming, ≥ 3.99 mg/mL in EtOH with ultrasonic
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
AT7519 is a small-molecule inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 210, 47, 100, 13, 170 and <10 nM for CDK1, CDK2, CDK4, CDK5, CDK6 and CDK9, respectively [1].
AT7519 showed no inhibition activity against CDK3, 7 and other non-CDK kinases. It inhibited CDK1 in an ATP- competitive manner with Ki value of 38 nM. AT7519 potently inhibited the proliferation of various human tumor cell lines and this activity is cell cycle related. AT7519 was also effective in cell lines with p53 mutants or suppression, suggesting that the anti-proliferation efficacy is p53-independent. In HCT116 cells, 24 h-treatment of AT7519 resulted in a remarkable induction of G0-G1 and G2-M cell cycle arrest. Besides that, AT7519 at concentrations relating to IC50 induced cell apoptosis (24 h) in HCT116, A2780 and HT29 cells with 52%, 3% and 94% survival, respectively. Moreover, in HCT116 tumor-bearing mice, 10 mg/kg AT7519 with intraperitoneal injection caused inhibition of NPM phosphorylation and induced apoptosis [1, 2].
References:
[1] Squires M S, Feltell R E, Wallis N G, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Molecular cancer therapeutics, 2009, 8(2): 324-332.
[2] Wyatt P G, Woodhead A J, Berdini V, et al. Identification of N-(4-Piperidinyl)-4-(2, 6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design†. Journal of medicinal chemistry, 2008, 51(16): 4986-4999.
关键字： 844442-38-2;C16H17Cl2N5O2;AT7519;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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