Ribociclib (Synonyms: LEE011)

Name: Ribociclib
Brand: MedChemExpress
SKU: HY-15777
Rating: 5.0 (59 reviews)

Cat. No.: HY-15777 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

For research use only. We do not sell to patients.

Ribociclib Chemical Structure

CAS No. : 1211441-98-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 59 publication(s) in Google Scholar

Other Forms of Ribociclib:

54 Publications Citing Use of MCE Ribociclib

: Ribociclib purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22. [Abstract]; Head-to-head comparison of the effect of PD 0332991 and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

: Ribociclib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM for 72 h.

: Ribociclib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

: Ribociclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]; Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

: Ribociclib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]; Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK4

10 nM (IC₅₀)

CDK6

39 nM (IC₅₀)

In Vitro

Ribociclib (500 nM; 6 days) inhibits the growth of neuroblastoma cell lines BE2C and IMR5^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:	Neuroblastoma cell lines BE2C and IMR5
Concentration:	10 nM、100 nM、250 nM、500 nM、750 nM、1 μM and 5 μM
Incubation Time:	6 days
Result:	Down-regulated FOXM1 protein expression level.

In Vivo

Ribociclib (200 mg/kg; p.o.; 21 days) delays tumor growth in CB17-immunodeficient BE2C or 1643 xenograft mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB17 immunodeficient BE2C or 1643 xenograft mice^[2]
Dosage:	200 mg/kg
Administration:	p.o.; Once a day for 21 days
Result:	Reduced RB phosphorylation significantly.

Clinical Trial

Molecular Weight

434.54

Formula

C₂₃H₃₀N₈O

CAS No.

1211441-98-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 6.25 mg/mL (14.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3013 mL	11.5064 mL	23.0128 mL
5 mM	0.4603 mL	2.3013 mL	4.6026 mL
10 mM	0.2301 mL	1.1506 mL	2.3013 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 1 mg/mL (2.30 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.30 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.89 mg/mL (2.05 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.89 mg/mL (2.05 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.89 mg/mL (2.05 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) RP-HPLC (1150 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)

References

[1]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. [Content Brief]

[2]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3013 mL	11.5064 mL	23.0128 mL	57.5321 mL
	5 mM	0.4603 mL	2.3013 mL	4.6026 mL	11.5064 mL
	10 mM	0.2301 mL	1.1506 mL	2.3013 mL	5.7532 mL

Ribociclib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ribociclib1211441-98-3LEE011LEE 011LEE-011CDKCyclin dependent kinaseInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Ribociclib (Synonyms: LEE011)

Customer Review

Other Forms of Ribociclib:

Ribociclib Related Antibodies

54 Publications Citing Use of MCE Ribociclib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ribociclib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ribociclib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

Request for HNMR Report