Ribociclib

Catalog No.S7440 Batch:S744006

Technical Data

Formula

C₂₃H₃₀N₈O

Molecular Weight

434.54

CAS No.

1211441-98-3

Solubility (25°C)*

In vitro

DMSO

22 mg/mL (50.62 mM)

Water

Insoluble

Ethanol

Insoluble

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

Clear solution

5%DMSO 1 Corn oil

1.1mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 22 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.

* <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 is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

Targets

CDK4 ^[2] (Cell-free assay)	CDK6 ^[2] (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. ^[1]

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. ^[1]

Features

Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.

Protocol (from reference)

Cell Assay:^{^[1]}	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 hours 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:^{^[1]}	Animal Models Mice bearing BE2C, NB-1643, or EBC1 xenografts. Dosages ~200 mg/kg daily Administration p.o.

Cell Assay:^{^[1]}

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 hours
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:^{^[1]}

Animal Models
Mice bearing BE2C, NB-1643, or EBC1 xenografts.
Dosages
~200 mg/kg daily
Administration
p.o.

References

Customer Product Validation

: , , Cancer Cell Int, 2017, 17:35

: Data from [Data independently produced by , , Nature, 2017, 553(7686):91-95]

: Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(22):6958-6968]

: Data from [Data independently produced by , , Cancer Res, 2016, 76(22):6723-6734]

Selleck's Ribociclib has been cited by 101 publications

Ribociclib leverages phosphodiesterase 4 inhibition in the treatment of neutrophilic inflammation and acute respiratory distress syndrome [ J Adv Res, 2024, S2090-1232(24)00119-X]	PubMed: 38548264
ERK hyperactivation serves as a unified mechanism of escape in intrinsic and acquired CDK4/6 inhibitor resistance in acral lentiginous melanoma [ Oncogene, 2024, 43(6):395-405]	PubMed: 38066089
Pharmacological inhibition of CDK4/6 impairs diffuse pleural mesothelioma 3D spheroid growth and reduces viability of cisplatin-resistant cells [ Front Oncol, 2024, 14:1418951]	PubMed: 39011477
Drug Repositioning via Graph Neural Networks: Identifying Novel JAK2 Inhibitors from FDA-Approved Drugs through Molecular Docking and Biological Validation [ Molecules, 2024, 29(6)1363]	PubMed: 38542998
Comparative biological activity of palbociclib and ribociclib in hormone receptor-positive breast cancer [ Sci Rep, 2024, 14(1):16030]	PubMed: 38992220
CDK4/6 inhibition to resensitize BRAF/EGFR inhibitor in patient-derived BRAF/PTEN-mutant colon cancer cells [ Transl Cancer Res, 2024, 13(7):3695-3703]	PubMed: 39145064
Synergistic Effects of Neratinib in Combination With Palbociclib or Miransertib in Brain Cancer Cells [ World J Oncol, 2024, 15(3):492-505]	PubMed: 38751701
The Combination of Afatinib With Dasatinib or Miransertib Results in Synergistic Growth Inhibition of Stomach Cancer Cells [ World J Oncol, 2024, 15(2):192-208]	PubMed: 38545471
Pharmacokinetics and Pharmacogenomics of Ribociclib in Black Patients with Metastatic Breast Cancer: The LEANORA study [ Res Sq, 2024, rs.3.rs-4656461]	PubMed: 39184092
p21 Prevents the Exhaustion of Cluster of Differentiation 4-Positive T Cells Within the Antitumor Immune Response Against Colorectal Cancer [ Gastroenterology, 2023, S0016-5085(23)05008-4]	PubMed: 37734420

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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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