Ribociclib succinate

製品コードS5188 バッチS518803

印刷

化学情報

Chemical Structure Synonyms LEE011 succinate Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C27H36N8O5
分子量 552.63 CAS No. 1374639-75-4
Solubility (25°C)* 体外 DMSO 10 mg/mL (18.09 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ribociclib (LEE011) succinate is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
in vitro

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. [2]
in vivo

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. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines
濃度 10 μM
反応時間 ~100 h
実験の流れ

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.
動物実験 動物モデル Mice bearing BE2C, NB-1643, or EBC1 xenografts
投薬量 ~200 mg/kg daily
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Internally Controlled and Dynamic Optical Measures of Functional Tumor Biology [ Anal Chem, 2023, 95(13):5661-5670] PubMed: 36952386
Overexpressed Cyclin D1 and CDK4 proteins are responsible for the resistance to CDK4/6 inhibitor in breast cancer that can be reversed by PI3K/mTOR inhibitors [ Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8] PubMed: 35982377
Genome wide CRISPR/Cas9 screen identifies the coagulation factor IX (F9) as a regulator of senescence [ Cell Death Dis, 2022, 13(2):163] PubMed: 35184131
MYC promotes tyrosine kinase inhibitor resistance in ROS1 fusion-positive lung cancer [ Mol Cancer Res, 2022, molcanres.MCR-22-0025-E.2022] PubMed: 35149545
Treatment of Retinoblastoma 1-Intact Hepatocellular Carcinoma With Cyclin-Dependent Kinase 4/6 Inhibitor Combination Therapy [ Hepatology, 2021, 74(4):1971-1993] PubMed: 33931882
Development and Characterization of Novel Endoxifen-Resistant Breast Cancer Cell Lines Highlight Numerous Differences from Tamoxifen-Resistant Models [ Mol Cancer Res, 2021, 19(6):1026-1039] PubMed: 33627502
Inhibition of CDK4/6 kinases causes production of aneuploid oocytes by inactivating the spindle assembly checkpoint and accelerating first meiotic progression [ Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044] PubMed: 33865884
Targeting WEE1 Inhibits Growth of Breast Cancer Cells That Are Resistant to Endocrine Therapy and CDK4/6 Inhibitors [ Front Oncol, 2021, 11:681530] PubMed: 34277427
Molecular targeted drugs resistance impairs double-strand break repair and sensitizes ER-positive breast cancer to PARP inhibitors [ Breast Cancer, 2021, 10.1007/s12282-021-01282-5] PubMed: 34346034
Genomic Resistance Patterns to Second-Generation Androgen Blockade in Paired Tumor Biopsies of Metastatic Castration-Resistant Prostate Cancer [ JCO Precis Oncol, 2017, 1PO.17.00140] PubMed: 32913968

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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