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• 产品描述： Ribociclib (LEE011) succinate (Kisqali) 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. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. 2. Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182. 3. Antonio Marra, Giuseppe Curigliano. NPJ Breast Cancer. 2019 Aug 29;5:27.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C;充氩

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.81 ml	9.048 ml	18.095 ml
  5 mM	0.362 ml	1.81 ml	3.619 ml
  10 mM	0.181 ml	0.905 ml	1.81 ml
  50 mM	0.036 ml	0.181 ml	0.362 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *