產(chǎn)品目錄

規(guī)格	10 mM * 1 mL in DMSO2mg5mg10mg25mg50mg100mg
CAS	920113-03-7
別名	N/A
化學(xué)名	2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one;hydrochloride
分子式	C21H20ClNO5.HCl
分子量	438.3
溶解度	Soluble in DMSO
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：

P276-00 is a novel inhibitor for CDK-1, CDK4 and CDK9 with IC50 of 79 nM, 63 nM and 20 nM, respectively [1].

CDK (cyclin-dependent kinase) plays an important role in cell cycle progression via promoting the G1/S cell cycle transition. Many studies have shown that more CDKs are overexpressed in cancer cells than in normal cells, which explain the reason of cancer cells divide uncontrollably[2]. The overexpression of CDK1/4/6 contributes to the phosphorylation of retinoblastoma protein (RB) via binding to CCND1 and results in the release of E2F transcription of genes required for cell cycle progression [3].

P276-00 is a novel inhibitor of CDK (cyclin-dependent kinase) with the ability of arresting the cells in G1/S phase transcription. When tested with NSCLC cell lines, P276-00 showed high ability of inhibiting cell proliferate thus decreased the colony forming potential via blocking cell cycle [4]. In head and neck squamous carcinoma cell line (FaDu, Detroits-562, SCC-25), treated with P276-00 for 12 hours could significantly inhibit cell ability with IC50 value ranging from 0.8 to 1.7 uM for different cell lines via decreasing the expression of CCND1[2].

In SCID mice model with H460 xenograft, treatment of P276-00 could down regulate the expression of CDK1 thus induced tumor regression [4]. When tested with HNSCC tumor xenograft mouse model, P276-00 treatment showed anti-cancer ability with a 48% tumor growth inhibition [2].

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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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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