Ribociclib hydrochloride

Catalog No.S5187 Batch:S518702

Technical Data

Formula

C₂₃H₃₁ClN₈O

Molecular Weight

471

CAS No.

1211443-80-9

Solubility (25°C)*

In vitro

DMSO

94 mg/mL (199.57 mM)

Water

94 mg/mL (199.57 mM)

Ethanol

94 mg/mL (199.57 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.39mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 7.8 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 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.7mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 94 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Ribociclib (LEE011) hydrochloride 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.

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.

References

Selleck's Ribociclib hydrochloride has been cited by 13 publications

SLC7A11 protects luminal A breast cancer cells against ferroptosis induced by CDK4/6 inhibitors [ Redox Biol, 2024, 76:103304]	PubMed: 39153252
Overexpression of COL11A1 confers tamoxifen resistance in breast cancer [ NPJ Breast Cancer, 2024, 10(1):38]	PubMed: 38806505
Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer [ Cancer Res, 2023, 83(1):141-157]	PubMed: 36346366
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

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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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