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Ribociclib (LEE011) CDK4/6 inhibitor

Name: Ribociclib (LEE011)
SKU: S7440
Availability: InStock
Rating: 5 (112 reviews)

Cat.No.S7440

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

Chemical Structure

Molecular Weight: 434.54

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	434.54	Formula	C₂₃H₃₀N₈O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1211441-98-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LEE011			Smiles	CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

Solubility

In vitro
Batch:

DMSO : 8 mg/mL (18.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (2.53mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets/IC₅₀/Ki	CDK4 ^[2] (Cell-free assay) 10 nM CDK6 ^[2] (Cell-free assay) 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/24045179/ [2] https://pubmed.ncbi.nlm.nih.gov/31482107/

Applications

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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	May 30 2024	Phase 2
NCT06075758	Recruiting	Breast Cancer	Novartis Pharmaceuticals\|Novartis	March 7 2024	--
NCT05996107	Recruiting	Breast Cancer	University of Michigan Rogel Cancer Center	February 27 2024	Phase 1

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