品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S83040-5mg	99%	￥792.00元	>10	-	-	-
源葉(MedMol)	S83040-10mg	99%	￥960.00元	>10	-	-	-
源葉(MedMol)	S83040-50mg	99%	￥3600.00元	>10	-	-	-
源葉(MedMol)	S83040-100mg	99%	￥5200.00元	>10	-	-	-

產(chǎn)品介紹

Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

產(chǎn)品描述： Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

靶點： CDK4:10 nM (IC50);CDK6:39 nM (IC50);CDK

體外研究：
Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively

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 Ribociclib (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<0.0001), although growth resumed post-treatment

參考文獻：
1. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. 2. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.

溶解性： Soluble in DMSO、H2O

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.752 ml	8.762 ml	17.524 ml
5 mM	0.35 ml	1.752 ml	3.505 ml
10 mM	0.175 ml	0.876 ml	1.752 ml
50 mM	0.035 ml	0.175 ml	0.35 ml

注意：

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參考文獻

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LEE011 (succinate hydrate) 99%

LEE011 (succinate hydrate)