Home > Products > Cell Cycle > CDK > LEE-011

LEE-011

(CAS No:1211441-98-3)

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

CAS No:1211441-98-3

Molecular Weight(MW):434.54

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

Price and large packaging, please e-mail consultation:info@SuperLan-chem.com

QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1211441-98-3
Molecular formula(MF)	C₂₃H₃₀N₈O
Molecular Weight(MW):	434.54
Alias

Solubility

In vitro	DMSO	7 mg/mL (16.1 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo

Biological Activity

Description

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. 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 ^[1]
(Cell-free assay)

CDK6 ^[1]
(Cell-free assay)

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 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		IC50ï¼10000 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		IC50ï¼10000 nM	25810375
Rh30	Growth Inhibition Assay		72 h		IC50ï¼10000 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 Î¼M	24 h		decreases the proportion of cells in S phase	25028469
449	Growth Inhibition Assay	3.33 Î¼M	24 h		decreases the proportion of cells in S phase	25028469
LP3	Growth Inhibition Assay	3.33 Î¼M	24 h		decreases the proportion of cells in S phase	25028469
LP6	Growth Inhibition Assay	3.33 Î¼M	24 h		decreases the proportion of cells in S phase	25028469
LP8	Growth Inhibition Assay	3.33 Î¼M	24 h		decreases the proportion of cells in S phase	25028469
LPS141	Growth Inhibition Assay	3.33 Î¼M	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	IC50ï¼10000 nM	24045179
NB16	Growth Inhibition Assay		24 h	DMSO	IC50ï¼10000 nM	24045179
RPE1	Growth Inhibition Assay		24 h	DMSO	IC50ï¼10000 nM	24045179

... Click to View More Cell Line Experimental Data

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]