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PF-431396

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Catalog No. T2314Cas No. 717906-29-1

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

PF-431396

PF-431396

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Purity: 99.82%
Catalog No. T2314Cas No. 717906-29-1
PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$50In StockIn Stock
10 mg$74In StockIn Stock
25 mg$148In StockIn Stock
50 mg$261In StockIn Stock
100 mg$447In StockIn Stock
200 mg$659In Stock-
1 mL x 10 mM (in DMSO)$59In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.82%
Color:Yellow
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Product Introduction

Bioactivity
Description
PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).
Targets&IC50
FAK:2 nM, PYK2:11 nM
In vitro
PF-431396 consistently inhibits protein tyrosine kinase phosphorylation under both calcium deficiency and the presence of Ca/W-7. It also blocks tyrosine phosphorylation of Pyk2 and FAK induced by anti-Ig- and aggregated LFA-1 in A20 cells, thereby inhibiting B cell proliferation.
Kinase Assay
In Vitro Kinase Assays and Selectivity Screening : To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel.
Chemical Properties
Molecular Weight506.5
FormulaC22H21F3N6O3S
Cas No.717906-29-1
SmilesCN(c1ccccc1CNc1nc(Nc2ccc3NC(=O)Cc3c2)ncc1C(F)(F)F)S(C)(=O)=O
Relative Density.1.506 g/cm3
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25.3 mg/mL (49.95 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.95 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
1mg5mg10mg50mg
1 mM1.9743 mL9.8717 mL19.7433 mL98.7167 mL
5 mM0.3949 mL1.9743 mL3.9487 mL19.7433 mL
10 mM0.1974 mL0.9872 mL1.9743 mL9.8717 mL
20 mM0.0987 mL0.4936 mL0.9872 mL4.9358 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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