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CAS No.: 902135-91-5

AT7519 HCl Catalog No. CSN16210

Synonyms: AT7519 (hydrochloride)

AT7519 HCl is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM and less potent to CDK3 and little active to CDK7.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CDK1

IC50:10-210nM CDK2

IC50:10-210nM CDK4

IC50:10-210nM Cdk6

IC50:10-210nM Cdk9

IC50:10-210nM 更多
描述The CDKs (cyclin dependent kinases), as direct regulators of specific phases of the cell cycle, can control cellular proliferation and transcription with their activating cyclin partners and subunit inhibitors. Thus, the inhibition of CDKs can be assessed with monitoring the phosphorylation state of specific substrates. For example, decreased phosphorylation of the CDK1 substrate PP1 (T320) and the CDK2 substrates Rb (T821) and NPM (T199) can indicated the inhibition of the CDKs. Decreased phosphorylation of pSer5 and pSer2 of RNA pol II CTD would indicate inhibition of CDKs 7 and 9, respectively. AT7519 Hydrochloride is the hydrochloride form of AT7519. AT7519 is a pan-CDKs inhibitor with IC50 values of 47, 13, <10nM for CDK2/CyclinA, CDK5/p35 and CDK9/CyclinT, and modest activity against CDK1/CyclinB, CDK3/CyclinE, CDK4/CyclinD1 and CDK6/CyclinD3 with IC50 values of 210, 360, 100 and 170nM, respectively (measured by in vitro kinase assays) . Treatment with 0.05-1uM AT7519 for 24 h was sufficient to inhibit phosphorylation of the CDK1 substrate PP1 (T320) and the CDK2 substrates Rb (T821) and NPM (T199) in HCT116 cells. AT7519 on concentration of 0.5uM induced rapid dephosphorylation at both RNA pol II CTD at both the serine 2 and serine 5 sites. AT7519 showed antiproliferative activity and apoptosis-induction in a panel of human tumor cell lines, including ovarian carcinoma, lung carcinoma, breast carcinoma, uterine sarcoma, leukemia and lymphoma, with IC50 values ranging from 40 to 940nM. AT7519 with concentration of 250-1000nM can induce G0-G1 and G2-M cell cycle blockade in HCT116 cells. Intraperitoneal or intravenous administration of 9.1mg/kg AT7519 twice a day for 9 consecutive days achieved completely tumor regression on day 15 in HCT116 tumor xenografts . Phase 2 studies of AT7519 treatment for mantle cell lymphoma and chronic lymphocytic leukemia have been completed (see in https://www.clinicaltrials.gov/).
动物研究
剂量
Mice: 32 mg/kg^[3] (i.v.), 5 mg/kg^[2] (i.v.); 10 mg/kg^[2] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 32 mg/kg^[3] (i.v.), 5 mg/kg^[2] (i.v.); 10 mg/kg^[2] (i.p.)
给药途径	i.v., i.p.

[1] Santo L, Vallet S, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.
[2] Squires MS, Feltell RE, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3883 mL
- 11.9416 mL
- 23.8831 mL
- 5 mM
- 0.4777 mL
- 2.3883 mL
- 4.7766 mL
- 10 mM
- 0.2388 mL
- 1.1942 mL
- 2.3883 mL

技术信息

CAS号

902135-91-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H18Cl3N5O2

运输

蓝冰

分子量

418.71

别名

AT7519 (hydrochloride)

溶解度

DMSO	500.0 mg/mL (1194.2 mM) warming
Water	70.0 mg/mL (167.2 mM) warming

动物实验配方

0.5% CMC-Na

48 mg/mL

suspension

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靶点	Description	IC50
CDK1		IC50:10-210nM
CDK2		IC50:10-210nM
CDK4		IC50:10-210nM
Cdk6		IC50:10-210nM
Cdk9		IC50:10-210nM

AT7519 HCl Catalog No. CSN16210

靶点选择性

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