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Abemaciclib methanesulfonate

🥰Excellent
Catalog No. T3111Cas No. 1231930-82-7
Alias LY2835219 mesylate, LY2835219 (methanesulfonate), LY2835219, abemaciclib mesylate

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Abemaciclib methanesulfonate

Abemaciclib methanesulfonate

🥰Excellent
Purity: 99.44%
Catalog No. T3111Alias LY2835219 mesylate, LY2835219 (methanesulfonate), LY2835219, abemaciclib mesylateCas No. 1231930-82-7
Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$50In StockIn Stock
10 mg$72In StockIn Stock
25 mg$86In StockIn Stock
50 mg$98In StockIn Stock
100 mg$126In StockIn Stock
200 mg$157In StockIn Stock
1 mL x 10 mM (in DMSO)$67In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.44%
Color:Yellow
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Product Introduction

Bioactivity
Description
Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
Targets&IC50
CDK6:10 nM, GSK-3β:192 nM, PIM1:50 nM, PIM2:3400 nM, HIPK2:31 nM, CDK1-cyclinB1:1627 nM, CK2:117 nM, FLT3 (D835Y):403 nM, JNK3:389 nM, CDK2-CyclinE:504 nM, CDK9-CyclinT1:57 nM, DRAK1:659 nM, CDK5-p35:287 nM, CDK7-CyclinH-MAT1:3910 nM, CDK4:2 nM, DYRK2:61 nM, FLT3:3960 nM, CDK5-p25:355 nM
In vitro
In subcutaneous and intracranial glioma models (U87 mg), MsOH treatment results in LY2835219 inhibiting tumor growth in a dose-dependent manner.
In vivo
In retinoblastoma, LY2835219 inhibits cancer cell growth by specifically targeting and inhibiting CDK4 and CDK6, leading to cell cycle arrest at the G1 phase and suppression of DNA synthesis.
Kinase Assay
Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.
Cell Research
LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.
SynonymsLY2835219 mesylate, LY2835219 (methanesulfonate), LY2835219, abemaciclib mesylate
Chemical Properties
Molecular Weight602.7
FormulaC27H32F2N8·CH4O3S
Cas No.1231930-82-7
SmilesCS(O)(=O)=O.CCN1CCN(Cc2ccc(Nc3ncc(F)c(n3)-c3cc(F)c4nc(C)n(C(C)C)c4c3)nc2)CC1
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 45 mg/mL (74.66 mM), Sonication is recommended.
DMSO: 9.62 mg/mL (15.96 mM), Sonication is recommended.
Ethanol: 23 mg/mL (38.16 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.66 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/Ethanol/H2O
1mg5mg10mg50mg
1 mM1.6592 mL8.2960 mL16.5920 mL82.9600 mL
5 mM0.3318 mL1.6592 mL3.3184 mL16.5920 mL
10 mM0.1659 mL0.8296 mL1.6592 mL8.2960 mL
Ethanol/H2O
1mg5mg10mg50mg
20 mM0.0830 mL0.4148 mL0.8296 mL4.1480 mL
H2O
1mg5mg10mg50mg
50 mM0.0332 mL0.1659 mL0.3318 mL1.6592 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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