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Ribociclib(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。
Ribociclib(LEE011)图片
CAS NO:1211441-98-3
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)434.54
FormulaC23H30N8O
CAS No.1211441-98-3 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 7 mg/mL (16.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILESO=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C
Synonyms

LEE 011; Ribociclib; LEE011; LEE-011; trade name: Kisqali

Chemical Name: 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

Exact Mass: 434.25426

实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: Ribociclib (formerly also known as LEE011, NVP-LEE011; trade name: Kisqali) is a potent, orally available and highly specific inhibitor of CDK4/6 (cyclin-dependent kinase) with IC50s of 10 nM and 39 nM, respectively. As of March 2017, Ribociclib was approved by FDA to treat postmenopausal women with a type of advanced breast cancer. Ribociclib functions via decreasing in phosphorylated RB and FOXM1. When tested with 17 human neuroblastoma cell lines, 12 of them were sensitive to Ribociclibtreatment with mean IC50=306±68 NM. Treatment with Ribociclib could dramatically decrease cell growth via arresting cell cycle G0-G1. In 12 of 17 human neuroblastoma-derived cell lines, treatment with LEE011 could significantly reduce cell proliferation.


Cell Assay: 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 are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once.

In VivoLEE011 (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.
Animal modelMice bearing BE2C, NB-1643, or EBC1 xenografts.
Formulation & DosageDissolved in 0.5% methylcellulose; 200 mg/kg daily; p.o.
ReferencesClin Cancer Res. 2013 Nov 15;19(22):6173-82.