产品属性：
产品名称 | 规格 | CAS号 | 型号 |
AT7519 Hydrochloride | 5mg 10mg 50mg 100mg | 902135-91-5 | EY-Y0165128 |
Cas No.902135-91-5
别名 AT 7519 Hydrochloride;AT-7519 Hydrochloride
化学名 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide;hydrochloride
分子式 C16H18Cl3N5O2
分子量 418.71
溶解度 ≥ 43.3 mg/mL in DMSO with ultrasonic, ≥ 8.82 mg/mL in EtOH with ultrasonic, ≥ 29.93 mg/mL in H2O
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：
IC50: AT7519 showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines.
Cyclin-dependent kinases (CDK) play a central role in the growth, division, and death of eukaryotic cell. This crucial role in cell cycle progression and their deregulation in several human cancers make them attractive therapeutic oncology targets. Series of CDK inhibitors was developed, among which, AT7519 is in early-phase clinical development currently.
In vitro: AT7519 showed potent antiproliferative activity (40-940 nmol/L)in a panel of human tumor cells, and the mechanism of action was shown to be consistent with the inhibition of CDK1 and CDK2. Cell cycle arrest caused by AT7519 followed by apoptosis in human tumor cells and inhibited tumor growth in human tumor xenograft models [1].
In vivo: Tumor regression was observed following twice daily dosing of AT7519 in the HCT116 and HT29 colon cancer xenograft models. The authors show that these effects are linked to inhibition of CDKs in vivo and that AT7519 induces tumor cell apoptosis [1].
Clinical trial: A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Electrocardiogram review suggested a dose-dependent increase in QTc and recruitment was discontinued without establishing a maximum tolerated dose. 4 patients with stable disease for >6 months and one had a prolonged partial response. Pharmacokinetic profile indicated modest interpatient variation with linear exposure at increased doses. AT7519 elicited clinical and PD activity resulting from CDK inhibition at doses below the appearance of DLT of QTc prolongation [2].
References:
[1] Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT.Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009;8(2):324-32.
[2] Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, Dragovich T, Adams J, Lock V, Smith DM, Von Hoff D, Calvert H. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Ann Oncol. 2011;22(9):2137-43.
关键字： 902135-91-5;C16H18Cl3N5O2;AT7519 Hydrochloride;
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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