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CVT-313
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CVT-313图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
CVT-313 (Cdk2 Inhibitor III) 是一种有效的、选择性的、可逆的、ATP 竞争性的 CDK2 抑制剂,IC50 为 0.5 μM。 CVT-313 抑制 CDC5L 磷酸化。

Cell lines

Human DLBCL cells

Preparation method

The solubility of this compound in DMSO is >20 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

25 μM, 24 hr

Applications

CVT-313 inhibited cdk2 in several human DLBCL cells. Incubation of DLBCL cells with 25 μM CVT-313 reduced phosphorylation of endogenous Rb on Thr821. CVT-313 (48 and 72 hr) induced cell apoptosis in human DLBCL cells in a time-dependent manner. CVT-313 treatment did not result in cell cycle arrest at 20 hr or at 48 hr. Treatment of LY3, LY8 cells and LY18 cells with CVT-313 led to parallel changes in XIAP and Mcl-1 mRNA levels. In normal and tumor human/murine cell lines, CVT-313 inhibited cell proliferation with the IC50 ranged from 1.25 to 20 μM. CVT-313 (12.5 μM, 18 h) induced cell arrest at the G1/S and G2/M boundary. In nonsynchronized MRC-5 cells, treatment with CVT-313 (6.25 μM) for 36 h induced a 2 N DNA content. Treatment with CVT-313 (6.25 μM) for 4 or 8 h after serum stimulation inhibited Rb hyperphosphorylation.

Animal models

Injured rat carotid artery model of restenosis

Dosage form

0.75 and 0.25 mg/kg

Application

In the injured rat carotid artery model of restenosis, lower doses of CVT-313 (0.75 and 0.25 mg/kg) were less efficacious, reducing mean neointimal area by about 30%, whereas the lowest dose tested (0.025 mg/kg) did not achieve any significant reduction in neointimal area. Treatment with CVT-313 for 14 days blocked restenosis in the rat carotid model.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

CVT-313 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) with IC50 value of 0.5 μM [1].
CDK2 is a serine/threonine kinase that is essential for the G1-S phase during cell division. CDK2 is an important target for prevention of aberrant cell proliferation [1].
In MRC-5 cells, CVT-313 inhibited Rb hyperphosphorylation in a time-dependant way and the cell cycle was arrested at the G1/S phase. Also, CVT-313 inhibited the growth of mouse, rat and human cells with IC50 values from 1.25 to 20 mM [1]. In human diffuse large B-cell lymphoma (DLBCL) cells, CVT-313 reduced CDK2-mediated phosphorylation of the retinoblastoma gene product (Rb) on T821. Also, CVT-313 reduced the anti-apoptotic factor Myeloid cell leukemia-1 (Mcl-1) and induced apoptosis [2].
In the injured rat carotid artery model of restenosis, CVT-313 (1.25 mg/kg) reduced neointima formation by 80%. Moreover, Treatment animals with CVT-313, the neointimal areas were inhibited by at least 70%. These suggested that CDK2 was an antiproliferative target and CVT-313 is an ideal candidate for the treatment of proliferative diseases [1].
References:
[1]. Brooks EE, Gray NS, Joly A, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem, 1997, 272(46): 29207-29211.
[2]. Faber AC, Chiles TC. Inhibition of cyclin-dependent kinase-2 induces apoptosis in human diffuse large B-cell lymphomas. Cell Cycle, 2007, 6(23): 2982-2989.