LEE011 (hydrochloride)

99.80%

LEE011 (hydrochloride)

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品牌：源叶(MedMol)

产品编号：S82374 一键复制产品信息

CAS号：1211443-80-9

分子式：C₂₃H₃₁ClN₈O

分子量：470.9982

别名：LEE011hydrochloride; LEE011 (hydrochloride); 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide hydrochloride; LEE011 hydrochloride;

货号	规格	价格	上海	北京	珠海	重庆	武汉
S82374-5mg	99.80%	￥390.00 S82374-5mg ￥390.00 现货	289 >10	-	-	-	-
S82374-10mg	99.80%	￥692.00 S82374-10mg ￥692.00 现货	149 >10	-	-	-	-
S82374-50mg促销	99.80%	￥1870.00 ￥1490.00 S82374-50mg ￥1490.00 现货	35 >10	-	-	-	-
S82374-100mg促销	99.80%	￥3110.00 ￥2480.00 S82374-100mg ￥2480.00 现货	22 >10	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

Ribociclib (LEE011) hydrochloride 是一种高度特异性的针对 CDK4 和 CDK6 的双重抑制剂，对应的IC50值分别为10 nM和39 nM

靶点：

CDK4(Cell-free assay):10 nM; CDK6(Cell-free assay):39 nM;CDK

体外研究：

LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence.

体内研究：

LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity.

细胞实验：

Cell lines: BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines Concentrations: 10 μM Incubation Time: ~100 h Method: A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data ar

动物实验：

Animal Models: Mice bearing BE2C, NB-1643, or EBC1 xenografts Dosages: ~200 mg/kg daily Administration: p.o.

参考文献：

1. Todd VanArsdale, 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, 19(22), 6173-6182.

溶解性：

Soluble in DMSO、H2O、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.123 ml	10.616 ml	21.232 ml
5 mM	0.425 ml	2.123 ml	4.246 ml
10 mM	0.212 ml	1.062 ml	2.123 ml
50 mM	0.042 ml	0.212 ml	0.425 ml