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PF-573228

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Catalog No. T2001Cas No. 869288-64-2
Alias PF 573228

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

PF-573228

PF-573228

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Purity: 99.51%
Catalog No. T2001Alias PF 573228Cas No. 869288-64-2
PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$45In StockIn Stock
10 mg$72In StockIn Stock
25 mg$138In StockIn Stock
50 mg$228In StockIn Stock
100 mg$366In StockIn Stock
500 mg$718-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.51%
Color:White
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Product Introduction

Bioactivity
Description
PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.
Targets&IC50
FAK:4 nM
In vivo
PF 573228 (IC50=30-500 nM) inhibited FAK Tyr397 phosphorylation in REF52 cells, PC3 cells, SKOV-3 cells, and L3.6p1 and F-G, MDCK cells.PF 573228 (1 μM) inhibited FAK phosphorylation but did not inhibit cell growth or induce apoptosis.
Kinase Assay
Affinity determination: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model.
Cell Research
Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted.(Only for Reference)
SynonymsPF 573228
Chemical Properties
Molecular Weight491.49
FormulaC22H20F3N5O3S
Cas No.869288-64-2
SmilesCS(=O)(=O)c1cccc(CNc2nc(Nc3ccc4NC(=O)CCc4c3)ncc2C(F)(F)F)c1
Relative Density.1.459
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (50.87 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.07 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 mM2.0346 mL10.1731 mL20.3463 mL101.7315 mL
5 mM0.4069 mL2.0346 mL4.0693 mL20.3463 mL
10 mM0.2035 mL1.0173 mL2.0346 mL10.1731 mL
20 mM0.1017 mL0.5087 mL1.0173 mL5.0866 mL
50 mM0.0407 mL0.2035 mL0.4069 mL2.0346 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:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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