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Ribociclib succinate hydrate

Name: Ribociclib succinate hydrate
Brand: TargetMol
SKU: T15731
Rating: 4.5 (1 reviews)

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Catalog No. T15731Cas No. 1374639-79-8

Alias LEE011 succinate hydrate

Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Ribociclib succinate hydrate

😃Good

Catalog No. T15731Alias LEE011 succinate hydrateCas No. 1374639-79-8

Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	Inquiry	1-2 weeks	1-2 weeks
50 mg	Inquiry	1-2 weeks	1-2 weeks
100 mg	Inquiry	1-2 weeks	1-2 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
Targets&IC50	CDK4:10 nM, CDK6:39 nM
In vitro	Ribociclib succinate hydrate treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition causes 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. Treatment with Ribociclib obviously 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. Treating a panel of 17 neuroblastoma cell lines with Ribociclib across a four-log dose range (10 to 10,000 nM) [2].
In vivo	Treatment with Ribociclib (LEE011; 200 mg/kg) or vehicle control for 21 days significantly delayed tumor growth in CB17 immunodeficient mice bearing BE2C or NB-1643 (MYCN amplified, sensitive in vitro) xenografts, with both groups showing a marked growth inhibition (p<0.0001); however, tumor growth resumed after the treatment period. This study also included EBC1 (non-amplified, resistant in vitro) xenografts in the treatment regimen. The daily dosing of Ribociclib was well tolerated across all xenograft models, with no observed weight loss or signs of toxicity [2].
Synonyms	LEE011 succinate hydrate

Chemical Properties

Molecular Weight	570.651
Formula	C₂₇H₃₈N₈O₆
Cas No.	1374639-79-8
Smiles	O.OC(=O)CCC(O)=O.CN(C)C(=O)c1cc2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n1C1CCCC1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 19 mg/mL (33.3 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (2.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7524 mL	8.7619 mL	17.5238 mL	87.6192 mL
5 mM	0.3505 mL	1.7524 mL	3.5048 mL	17.5238 mL
10 mM	0.1752 mL	0.8762 mL	1.7524 mL	8.7619 mL
20 mM	0.0876 mL	0.4381 mL	0.8762 mL	4.3810 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc