基本信息

产品描述

CVT-313是有效的CDK2抑制剂，在体外的IC50值为0.5 μM。它对其他非相关的、依赖于ATP的丝氨酸/苏氨酸激酶没有作用。

靶点（IC50 & Targe）

CDK1,4.2μM

CDK2,0.5μM

CDK4,215μM

体外研究

In cells exposed to CVT-313, hyperphosphorylation of the retinoblastoma gene product is inhibited, and progression through the cell cycle is arrested at the G1/S boundary. The growth of mouse, rat, and human cells in culture is also inhibited by CVT-313 with the IC50 for growth arrest ranging from 1.25 to 20 μM. CVT-313 inhibits Rb hyperphosphorylation[1].

细胞实验

Cell lines: MRC-5 cells

Concentrations: 12.5 μM

Incubation Time: 24 h

Method: --

(Only for Reference)

动物实验

Animal Models: Rat carotid artery model of restenosis

Formulation: saline

Dosages: 0.025, 0.25, 0.75, 1.25 mg/kg

Administration: intraluminal

(Only for Reference)

参考文献

[1] Brooks EE, et al. J Biol Chem. 1997, 272(46):29207-11.

安全信息

图形或危害标志
提示语	Danger
危险说明	H315 H317 H318 H334 H335 H341 H361 H370 H413
防范说明	P201 P202 P260 P264 P270 P271 P272 P273 P280 P302+P352 P304+P340 P305+P351+P338 P310 P321 P362 P405

产品说明

一般描述

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ ~1.25-20 µM) in vitro and prevent neointima formation in vivo.
A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC₅₀ = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC₅₀ >1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC₅₀ = ~1.25-20 µM) in vitro and prevent neointima formation in vivo.

包装

1, 5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
Cdk2/A, Cdk2/E
Target IC₅₀: 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1
Reversible: yes
Cell permeable: yes
Product competes with ATP.

警告

Toxicity: Carcinogenic / Teratogenic (D)

重悬

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Bhattacharjee, R.N., et al. 2001. Mol. Cell. Biol.21, 5417.
Brooks, E.E., et al. 1997. J. Biol. Chem.272, 29207.

法律信息

Sold under license of U.S. Patents 6,617,331 and 6,803,371.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息