Ribociclib succinate

Catalog No.S5188 Batch:S518801

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Technical Data

Formula

C27H36N8O5

Molecular Weight 552.63 CAS No. 1374639-75-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.95 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

Protocol (from reference)

Cell Assay:

[2]

  • 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.

Animal Study:

[2]

  • Animal Models

    Mice bearing BE2C, NB-1643, or EBC1 xenografts

  • Dosages

    ~200 mg/kg daily

  • Administration

    p.o.

Selleck's Ribociclib succinate has been cited by 10 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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