產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg
CAS	199986-75-9
別名	CVT 313;NG 26;CVT313;NG26;NG-26
化學(xué)名	2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol
分子式	C20H28N6O3
分子量	400.47
溶解度	≥ 20 mg/mL in DMSO, ≥ 51.1 mg/mL in EtOH with gentle warming
儲存條件	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

產(chǎn)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].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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