LEE011

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LEE011

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1211441-98-3
包装:	2mg, 5mg, 10mg, 25mg

包装与价格：

产品名称

Ribociclib

产品介绍

Ribociclib (LEE011) 是一种高度特异性的 CDK4/6 抑制剂，IC₅₀ 值分别为 10 nM 和 39 nM，对 cyclin B/CDK1 复合体的活性低于其 1000 倍。

细胞实验
细胞系	MYCN amplified neuroblastoma cell lines
方法	Pharmacologic growth inhibition LEE011 was provided by Novartis pharmaceuticals. A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, was plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system (ACEA Biosciences) and treated 24 hours later with a four-log dose range of inhibitor or with a DMSO control. Cell indexes were monitored continuously for ~100 hours, and IC50 values were determined as follows: Growth curves were generated by plotting the cell index as a function of time and were 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 post-treatment was then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas were normalized to the DMSO control, and the resulting data were analyzed using a non-linear log inhibitor vs. normalized response function (Graphpad). All experiments were repeated at least once.
浓度	0~10μM
处理时间	96h

动物实验
动物模型	BE2C, NB-1643, or EBC1 cell line-derived xenografts of CB17 SCID–/– mice
配制	0.5 % methylcellulose
剂量	200 mg/kg
给药处理	oral

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.3013 mL	11.5064 mL	23.0128 mL
5 mM	0.4603 mL	2.3013 mL	4.6026 mL
10 mM	0.2301 mL	1.1506 mL	2.3013 mL