Home Cell Cycle CDK inhibitor Ribociclib For research use only.

Ribociclib

Synonyms: LEE011

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

Ribociclib Chemical Structure

Ribociclib Chemical Structure

CAS: 1211441-98-3

Selleck's Ribociclib has been cited by 87 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DFSP105 Growth Inhibition Assay 24 h GI50=276 nM 25852058
Myoblast Growth Inhibition Assay 72 h IC50=1035 nM 25810375
IMRS Growth Inhibition Assay 72 h IC50=873 nM 25810375
SKNAS Growth Inhibition Assay 72 h IC50＞10000 nM 25810375
Rh28 Growth Inhibition Assay 72 h IC50=845 nM 25810375
Rh41 Growth Inhibition Assay 72 h IC50=7187 nM 25810375
CW9019 Growth Inhibition Assay 72 h IC50=9912 nM 25810375
Rh5 Growth Inhibition Assay 72 h IC50＞10000 nM 25810375
Rh30 Growth Inhibition Assay 72 h IC50＞10000 nM 25810375
778 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
449 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
LP3 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
LP6 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
LP8 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
LPS141 Growth Inhibition Assay 72 h inhibits cell growth dose dependently 25028469
778 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
449 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
LP3 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
LP6 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
LP8 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
LPS141 Growth Inhibition Assay 3.33 μM 24 h decreases the proportion of cells in S phase 25028469
IMR5 Growth Inhibition Assay 24 h DMSO IC50=126 nM 24045179
BE2C Growth Inhibition Assay 24 h DMSO IC50=134 nM 24045179
1643 Growth Inhibition Assay 24 h DMSO IC50=147 nM 24045179
SKNSH Growth Inhibition Assay 24 h DMSO IC50=148 nM 24045179
SY5Y Growth Inhibition Assay 24 h DMSO IC50=154 nM 24045179
NGP Growth Inhibition Assay 24 h DMSO IC50=175 nM 24045179
KELLY Growth Inhibition Assay 24 h DMSO IC50=220 nM 24045179
CHP134 Growth Inhibition Assay 24 h DMSO IC50=273 nM 24045179
NLF Growth Inhibition Assay 24 h DMSO IC50=328 nM 24045179
LAN5 Growth Inhibition Assay 24 h DMSO IC50=429 nM 24045179
NB69 Growth Inhibition Assay 24 h DMSO IC50=738 nM 24045179
SKNDZ Growth Inhibition Assay 24 h DMSO IC50=801 nM 24045179
NBSD Growth Inhibition Assay 24 h DMSO IC50=1900 nM 24045179
SKNF1 Growth Inhibition Assay 24 h DMSO IC50=3500 nM 24045179
EBC1 Growth Inhibition Assay 24 h DMSO IC50=6400 nM 24045179
SKNAS Growth Inhibition Assay 24 h DMSO IC50＞10000 nM 24045179
NB16 Growth Inhibition Assay 24 h DMSO IC50＞10000 nM 24045179
RPE1 Growth Inhibition Assay 24 h DMSO IC50＞10000 nM 24045179
Sf21 Function assay 10 mins Inhibition of recombinant human full length N-terminal GST-tagged CDK4/Cyclin-D3 co-expressed in baculovirus infected sf21 cells using Rb substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.013 μM. 29518312
Sf21 Function assay 10 mins Inhibition of recombinant human full length C-terminal 6His-tagged CDK9/Cyclin-T1 co-expressed in baculovirus infected sf21 cells using PDKtide substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.197 μM. 29518312
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.2862 μM. 29407975
SEM Antiproliferative assay 72 hrs Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.4605 μM. 29407975
KOPN8 Antiproliferative assay 72 hrs Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.5008 μM. 29407975
NCI-H1299 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 5.46 μM. 29518312
T47D Growth inhibition assay 72 hrs Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 6.227 μM. 28651979
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 6.23 μM. 29518312
H1299 Growth inhibition assay 72 hrs Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 7.637 μM. 28651979
KOPN8 Apoptosis assay 0.5 uM 3 hrs Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM after 3 hrs by Western blot analysis 29407975
KOPN8 Apoptosis assay 0.5 uM 24 hrs Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM pre-treated with NAC for 1 hr and measured after 24 hrs by Western blot analysis 29407975
Hep3B Cell cycle assay 24 hrs Cell cycle arrest in human Hep3B cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
HepG2 Cell cycle assay 24 hrs Cell cycle arrest in human HepG2 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
A549 Cell cycle assay 24 hrs Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
NCI-H460 Cell cycle assay 24 hrs Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
T47D Cell cycle assay 24 hrs Cell cycle arrest in human T47D cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
MDA-MB-231 Cell cycle assay 24 hrs Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry 29518312
Fluc-labeled 4T1 Antitumor assay 130 mg/kg 18 days Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as reduction in tumor weight at 130 mg/kg, ip administered daily for 18 days measured after 8 to 25 days 29518312
T47D Cell cycle assay 24 hrs Induction of cell cycle arrest in human T47D cells assessed as increase in G0/G1 phase accumulation incubated for 24 hrs by flow cytometry 28651979
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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.
Features Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets
CDK4 [2]
(Cell-free assay)		 CDK6 [2]
(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. [1]
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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP 29789630
Growth inhibition assay Cell viability 26390342
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. [1]
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
NCT06075758 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis February 9 2024 --
NCT05996107 Recruiting Breast Cancer University of Michigan Rogel Cancer Center January 2024 Phase 1
NCT05843253 Not yet recruiting High Grade Glioma|Diffuse Intrinsic Pontine Glioma|Anaplastic Astrocytoma|Glioblastoma|Glioblastoma Multiforme|Diffuse Midline Glioma H3 K27M-Mutant|Metastatic Brain Tumor|WHO Grade III Glioma|WHO Grade IV Glioma Nationwide Children''s Hospital|Novartis January 15 2024 Phase 2

Chemical lnformation & Solubility

Molecular Weight 434.54 Formula

C23H30N8O
CAS No. 1211441-98-3 SDF Download Ribociclib SDF
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 8 mg/mL ( (18.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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