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抑制劑描述：

產(chǎn)品名稱：LEE011

產(chǎn)品別名：7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

英文別名：LEE 011;LEE-011;Ribociclib;LEE011

靶點(diǎn)：CDK

CAS：1211441-98-3

純度：>98%

外觀：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：

LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

溶解性：DMSO：7 mg/mL (16.1 mM)

體外研究：

LEE011是一種CDK4/CDK6的雙重抑制劑，能夠顯著抑制17種神經(jīng)細(xì)胞瘤中的12種的生長，平均IC50值是307 nM。對(duì)神經(jīng)細(xì)胞瘤的抑制主要是抑制細(xì)胞的生長，受到G1細(xì)胞周期阻滯和細(xì)胞衰老的調(diào)控。

體內(nèi)研究：CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with LEE011 (200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p.

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