PF-573228
Catalog No.S2013
Molecular Weight(MW): 491.49
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.
6 Customer Reviews
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OVISE cells were incubated for 25 hr at the indicated concentrations of the FAK inhibitors. Immunoblots were performed to assess inhibition of auto-phosphorylation by the FAK inhibitors.
PLoS One 2014 9(2), e88588. PF-573228 purchased from Selleck.
Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Focal adhesion kinase (FAK) inhibitor PF-573228. PF-573228 was applied on NCI-H460 and COR-L23, both derived from large cell lung carcinoma. Hence, it acted similarly showing strong inhibitory potential in both cell lines by suppressing the growth of 50% of cells between 4 and 7 礛.
2014 Dr.Milica Pesic from Institute for Biological Research. PF-573228 purchased from Selleck.
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FAK inhibition blunted the increased migration induced by PGC1α depletion. G361 cells were subjected to 24 h transwell migration assays in the presence of DMSO or various doses of FAK inhibitor PF-573228. Images represent three pictures captured with scale bar representing 100 μm.
Nature, 2016, 537(7620):422-429.. PF-573228 purchased from Selleck.
(b) Using PF-573228 at a concentration range of 0.01–10 μM for 24 hours decreased phosphorylated FAK expression in a time-dependent manner, and there was a 70% inhibition rate at the range of 5–10 μM.
Sci Rep, 2017, 7:43146. PF-573228 purchased from Selleck.
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Effect of PF-228 (namely PF-573228) on EC actin stress fiber formation and FAK localization after thrombin. Confluent human pulmonary artery EC were pretreated with PF-228 (10 μM, 30 min) or vehicle and then stimulated with thrombin (1 U/ml, 5 min) or vehicle. (A) Immunofluorescent imaging of cells stained for F-actin (red) and FAK (green) was performed and representative images are shown. Increased actin stress fiber formation after thrombin with co-localization of FAK at the ends of stress fibers are noted (small and large arrows, respectively). (B) Quantification of actin stress fibers was performed separately and is expressed as a percentage of the total area imaged. (n=3 representative images from separate experiments for each experimental condition, *p < .05 compared to each other condition). (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article.)
Vascul Pharmacol, 2018, doi:10.1016/j.vph.2018.06.017. PF-573228 purchased from Selleck.
a. Gelatin degradation by NCI-H460/R and COR-L23 cells treated with DOX, PF-573228, WZ811 and their combinations for 24 h. Images were captured using a 20× objective on a fluorescence microscope and representative examples are presented on the left part of the panel. At least 100 cells were analyzed per experiment. All experiments were performed at least three times. Merged channels show fluorescent gelatin (green), actin (red) and nuclei (blue) staining; dark areas represent spots of degraded gelatin. Scale bar = 100 μm. Corresponding histograms for each cell line are presented in the right part of the panel showing percentages of degraded gelatin areas relative to the cell volume. Each bar represents mean value ± S.E. * indicates p < 0.05 compared to untreated control cells; # indicates p < 0.05 compared to cells treated with PF-573228; $ indicates p < 0.05 compared to cells treated with WZ811.
Cell Oncol (Dordr), 2017, 40(1):47-62.. PF-573228 purchased from Selleck.
Purity & Quality Control
Choose Selective FAK Inhibitors
Biological Activity
| Description | PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. [1] |
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| Cell Data |
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| In vivo | Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice [2]. |
Protocol
| Kinase Assay: |
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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 |
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Solubility (25°C)
| In vitro | DMSO | 26 mg/mL (52.9 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+2% Tween 80+30% PEG 300+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 491.49 |
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| Formula | C22H20F3N5O3S |
| CAS No. | 869288-64-2 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
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Question 1:
Would you please let me know the detail of how to dissolve PF-573228 (Catalog No.S2013) for in vivo study (oral administration)?
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Answer:
PF-573228 in 30% PEG400+0.5% Tween80+ 5% Propylene glycol at 30mg/ml is a suspension. If you will use the compound for oral gavage, this suspension is fine for it.
