Ribociclib (LEE011) 瑞博西尼；瑞博西利；瑞博西林；瑞波西利

目录号 M2218 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

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。

别名：Ribociclib

其他规格数量报价？

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。

Ribociclib (LEE011) (200 mg/kg/day，口服)引起小鼠中的BE2C或者1643细胞显著的生长延迟。

	数据来源	Bio Pharma (2018). Figure 5. LEE011
	方法	qRT-PCR
	细胞系/动物模型	MDCKII-ABCB1, MDCKII-ABCG2, or MDCKII-parent cells
	浓度	12 and 20 μM
	处理时间	72 h
	实验结果	The ABCB1 and ABCG2 expression rate was assessed using the ΔΔCt method, and we observed no significant change in the transporter-encoding gene studied, as demonstrated in Figure 5D.

体外实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

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

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。

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