LEE011 (Ribociclib) Selectivity & Specificity

Target Selectivity of LEE011 (Ribociclib)

Key Target	IC₅₀	Description	Reference
PDE4A	0.25 nM	HTRF reagents	PMC11331181
CDK4/cyclinD1	2 nM	In vitro CDK4/cyclinD1 activity assay (γ-33P radioactivity assay)	PMC12865202
PDE4C	4.4 nM	HTRF reagents	PMC11331181
PDE4B	4.94 nM	HTRF reagents	PMC11331181
PDE4D	10 nM	HTRF reagents	PMC11331181
Cyclin D1–CDK4, CyclinD1/2/3–CDK6, Cyclin B–CDK1, Cyclin A/E–CDK2	10 nM	IC50 inhibition assay	PMC5652078
CDK4	10 nM	preclinical drug-exposure experiments	PMC7912842
CDK4/CDK6	10 nM	--	PMC6647725
CDK6	39 nM	preclinical drug-exposure experiments	PMC7912842
cyclin D–CDK4/6 complexes	40 nM	half maximal inhibition (IC50) assay	PMC5652078
CDK2	0.07 µM	CDK2 analysis kit from [Vendor] Bioscience	PMC11678221
CaMKII δ	153 nM	In vitro CaMKII δ activity assay against a peptide substrate (γ-33P radioactivity assay)	PMC12865202

Check the LEE011 (Ribociclib) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Cell-free Assays (IC₅₀/K_i) for LEE011 (Ribociclib)

Key Target	IC₅₀ (Cell-free)	Description	Reference
CaMKII δ	153 nM	In vitro CaMKII δ activity assay against a peptide substrate (γ-33P radioactivity assay)	Download PDF
CDK4/cyclinD1	2 nM	In vitro CDK4/cyclinD1 activity assay (γ-33P radioactivity assay)	Download PDF
CDK2	0.07 µM	CDK2 analysis kit from [Vendor] Bioscience	Download PDF
PDE4A	0.25 ± 0.03 lM	HTRF reagents	PMC11331181
PDE4B	4.94 ± 0.07 lM	HTRF reagents	PMC11331181
PDE4C	4.40 ± 0.06 lM	HTRF reagents	PMC11331181
PDE4D	>10 lM	HTRF reagents	PMC11331181
cyclin D–CDK4/6 complexes	<40 nM	half maximal inhibition (IC50) assay	PMC5652078
Cyclin D1–CDK4, CyclinD1/2/3–CDK6, Cyclin B–CDK1, Cyclin A/E–CDK2	10 nmol/L (Cyclin D1–CDK4), 39 nmol/L (CyclinD1/2/3–CDK6), 1	IC50 inhibition assay	PMC5652078
CDK4	10 nmol/L	enzymatic assays	Download PDF
CDK6	39 nmol/L	enzymatic assays	Download PDF
CDK4	10 nM	Activity measurement	Download PDF
CDK6	39 nM	Activity measurement	Download PDF

Cell-based Assay (IC₅₀) for LEE011 (Ribociclib)

Cell Type	IC₅₀ (Cell-based)	Description	Reference
SK-N-BE(2)C cells	2 μM	Confluency analysis	Download PDF
OATP1B1	25.9 µM	Transport activity quantified by spectrofluorometry and normalized to total protein.	Download PDF
Oatp1b2	19.2 µM	Transport activity quantified by spectrofluorometry and normalized to total protein.	Download PDF
OATP1B3	42.9 µM	Transport activity quantified by spectrofluorometry and normalized to total protein.	Download PDF
SF8628	2.973 μM	CellTiter 96 AQueous One Solution Cell Proliferation Assay	Download PDF
SF7761	0.575 μM	CellTiter 96 AQueous One Solution Cell Proliferation Assay	Download PDF
SU-DIPG17	0.019 μM	CellTiter 96 AQueous One Solution Cell Proliferation Assay	Download PDF
HJSD-DIPG007	1.746 μM	CellTiter 96 AQueous One Solution Cell Proliferation Assay	Download PDF
Parental MCF-7	0.2 µM	CCK-8 cell growth assay, LDH cytotoxicity assay	PMC12738774
Parental T47D	0.2 µM	CCK-8 cell growth assay, LDH cytotoxicity assay	PMC12738774
Ribociclib-resistant MCF-7	>0.8 µM	CCK-8 cell growth assay, LDH cytotoxicity assay	PMC12738774
Ribociclib-resistant T47D	>0.8 µM	CCK-8 cell growth assay, LDH cytotoxicity assay	PMC12738774
MDA-MB-231	11μM	MTT assay	Download PDF
MCF-7	20μM	MTT assay	Download PDF
MCF-7	36.45 μM	Cell Counting Kit-8 (CCK-8) assay	PMC11583401
MCF-7	28.24 μM	Cell Counting Kit-8 (CCK-8) assay	PMC11583401
MDA-MB-231	47.71 μM	Cell Counting Kit-8 (CCK-8) assay	PMC11583401
MDA-MB-231	35.95 μM	Cell Counting Kit-8 (CCK-8) assay	PMC11583401
Human neutrophils	0.83 ± 0.04 lM	Spectrophotometric monitoring of cytochrome c reduction	PMC11331181
Human neutrophils	3.26 ± 0.07 lM	HTRF reagents	PMC11331181
A549	45.56 mM (6 h), 15.98 mM (24 h), 4.796 mM (48 h), 2.104 mM (	Cell Counting Kit 8 (CCK-8)	Download PDF
PC9	38.6 mM (6 h), 23.37 mM (24 h), 12.34 mM (48 h), 6.165 mM (7	Cell Counting Kit 8 (CCK-8)	Download PDF
T47D-p16	20-fold higher than MOCK control cells	Cell proliferation measured by crystal violet staining after 6 days.	Download PDF
MCF7-p16	17-fold higher than MOCK control cells	Cell proliferation measured by crystal violet staining after 6 days.	Download PDF
T47D-cyclin D1	3- to 5-fold higher than MOCK control cells	Cell proliferation measured by crystal violet staining after 6 days.	Download PDF
MCF7-cyclin D1	2- to 3-fold higher than MOCK control cells	Cell proliferation measured by crystal violet staining after 6 days.	Download PDF
U937	3.7 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
HL60	0.5 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
NB4	2.6 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
MV4-11	2.1 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
K562	13.1 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
CCRF	8.6 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary ALL cells (Patient 1)	2.14 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary ALL cells (Patient 2)	1.73 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary ALL cells (Patient 3)	14.68 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary ALL cells (Patient 4)	2.68 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary ALL cells (Patient 5)	11.52 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary AML cells (Patient 1)	2.54 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary AML cells (Patient 2)	8.46 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary AML cells (Patient 3)	1.94 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary AML cells (Patient 4)	5.04 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
primary AML cells (Patient 5)	2.98 µM	CCK8 Kit, calculated by Graph Prism software	Download PDF
Rb WT MCF-7	6 ± 0.5 μg/ml (48h), 4 ± 0.3 μg/ml (72h)	MTT assay	Download PDF
Rb KD MCF-7	17 ± 1.2 μg/ml (48h), 6 ± 0.4 μg/ml (72h)	MTT assay	Download PDF
BT-549	3.2 μg/ml (48h), 12.7 μg/ml (72h)	MTT assay	Download PDF

Size	Price	Qty
5mg	USD 197
25mg	USD 590
100mg	USD 997

Target Selectivity of LEE011 (Ribociclib)

Cell-free Assays (IC50/Ki) for LEE011 (Ribociclib)

Cell-based Assay (IC50) for LEE011 (Ribociclib)

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Cell-free Assays (IC₅₀/K_i) for LEE011 (Ribociclib)

Cell-based Assay (IC₅₀) for LEE011 (Ribociclib)