Home Cell Cycle CDK inhibitor Ribociclib succinate For research use only.

Ribociclib succinate

Synonyms: LEE011 succinate

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

Ribociclib succinate Chemical Structure

Ribociclib succinate Chemical Structure

CAS: 1374639-75-4

Selleck's Ribociclib succinate has been cited by 10 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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Biological Activity

Description Ribociclib (LEE011) succinate is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Targets
CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)
10 nM 39 nM
In vitro
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]
Cell Research 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 are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once.
In Vivo
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]
Animal Research Animal Models Mice bearing BE2C, NB-1643, or EBC1 xenografts
Dosages ~200 mg/kg daily
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03056833 Completed Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Carcinoma Ronald Buckanovich|University of Pittsburgh June 10 2017 Phase 1
NCT02934568 Recruiting Continued Access to Study Treatment(s) Cancers With a Mass Bulky Tumor Nodule Lump Advanced Cancer Advanced Solid Tumors Advanced Solid Malignancies Novartis Pharmaceuticals|Novartis December 15 2016 Phase 2
NCT02734615 Terminated Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 14 2016 Phase 1
NCT02431481 Completed Normal Renal Function|Impaired Renal Function Novartis Pharmaceuticals|Novartis October 23 2015 Phase 1
NCT02292550 Completed Non-small Cell Lung Cancer Novartis Pharmaceuticals|Novartis May 14 2015 Phase 1

Chemical lnformation & Solubility

Molecular Weight 552.63 Formula

C27H36N8O5
CAS No. 1374639-75-4 SDF --
Smiles CN(C)C(=O)C1=CC2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2[N]1C5CCCC5.OC(=O)CCC(O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 13 mg/mL ( (23.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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