Ribociclib succinate (Synonyms: LEE011 succinate)

Name: Ribociclib succinate
Brand: MedChemExpress
SKU: HY-15777B
Rating: 5.0 (60 reviews)

Cat. No.: HY-15777B Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Ribociclib succinate (LEE011 succinate) is a highly specific 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 succinate Chemical Structure

CAS No. : 1374639-75-4

Size	Price	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 84	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	USD 348	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 624	In-stock	Estimated Time of Arrival: December 31
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Based on 60 publication(s) in Google Scholar

Other Forms of Ribociclib succinate:

55 Publications Citing Use of MCE Ribociclib succinate

: Ribociclib succinate 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 succinate 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 succinate 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 succinate 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 succinate 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK4

10 nM (IC₅₀)

CDK6

39 nM (IC₅₀)

In Vitro

Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC₅₀=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC₅₀ of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G₀/G₁ phase of the cell cycle. This G₀/G₁ arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively^[2].

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

In Vivo

CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment^[2].

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

Clinical Trial

Molecular Weight

552.63

Formula

C₂₇H₃₆N₈O₅

CAS No.

1374639-75-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 9.38 mg/mL (16.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 4.17 mg/mL (7.55 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8095 mL	9.0476 mL	18.0953 mL
5 mM	0.3619 mL	1.8095 mL	3.6191 mL
10 mM	0.1810 mL	0.9048 mL	1.8095 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 3.12 mg/mL (5.65 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Protocol 2

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 15.15 mg/mL (27.41 mM); Clear solution; Need ultrasonic

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (280 KB) SDS (788 KB)

COA (251 KB) LCMS (93 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]

Cell Assay ^[2]	Cells are grown for 24 hours in 35 mm plates, treated with 500 nM Ribociclib for 6 days, and then fixed and stained overnight. Cells are then imaged for SA-β-gal using an Axio Observer D.1 phase contrast microscope. The percentage of SA-β-gal positive cells is determined by counting the number of positive cells present in three separate microscope frames, and then normalizing to the control. To assess apoptotic activity, cells are plated in triplicate in 96 well plates, treated with Ribociclib, and assayed for caspase 3/7 activation 16 hours after treatment with Caspase-Glo 3/7. Cells treated with SN-38 are used as a positive control^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] The BE2C, NB-1643, or EBC1 cell line-derived xenografts are implanted subcutaneously into the right flank of CB17 SCID^-/- mice. Animals bearing engrafted tumors of 200-600 mm³ are then randomized to oral treatment with 200 mg/kg Ribociclib in 0.5 % methylcellulose (n=10) or vehicle (n=10) daily for a total of 21 days. Tumor burden is determined periodically throughout treatment according to the formula (π/6)×d², where d represents the mean tumor diameter obtained by caliper measurement. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

H₂O / DMSO	1 mM	1.8095 mL	9.0476 mL	18.0953 mL	45.2382 mL
H₂O / DMSO	5 mM	0.3619 mL	1.8095 mL	3.6191 mL	9.0476 mL
DMSO	10 mM	0.1810 mL	0.9048 mL	1.8095 mL	4.5238 mL
DMSO	15 mM	0.1206 mL	0.6032 mL	1.2064 mL	3.0159 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Ribociclib succinate 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:

Ribociclib1374639-75-4LEE011LEE 011LEE-011CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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Ribociclib succinate (Synonyms: LEE011 succinate)

Customer Review

Other Forms of Ribociclib succinate:

Ribociclib succinate Related Antibodies

55 Publications Citing Use of MCE Ribociclib succinate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ribociclib succinate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ribociclib succinate Related Classifications

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