PF-573228

Catalog No.S2013

PF-573228 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 570 In stock
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Cited by 8 Publications

6 Customer Reviews

  • 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.

  • 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.

  • 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.
Targets
FAK [1]
(Cell-free assay)
4 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 MnO1T4lv[XOnIHHzd4F6 NFPNeHV,OTBizszN MXrEUXNQ M4X1dYlvcGmkaYTzJGZCUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGxJI5O M2rVOlE4Ozl3NUm0
REF52 MnP2T4lv[XOnIHHzd4F6 NW[2XpdMhjFyIN88US=> NE[4TYxFVVOR MWHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJJ4yODBibl2= M{PTflE4Ozl3NUm0
PC3 NWXiPYpIU2mwYYPlJIF{e2G7 Mm\BglExKM7:TR?= NEnNVJZFVVOR NVLKTHV2cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzMECgcm0> NWf5WHo3OTd|OUW1PVQ>
SKOV-3 M{HTNGtqdmG|ZTDhd5NigQ>? NYrFNGFzhjFyIN88US=> NIWxZllFVVOR MU\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxKG6P MX2xO|M6PTV7NB?=
L3.6p1 NGTicXZMcW6jc3WgZZN{[Xl? MVr+NVAh|ryP M3W5TmROW09? M{nqcolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzByIH7N MVixO|M6PTV7NB?=
F-G M1e2WmtqdmG|ZTDhd5NigQ>? NF;V[3F,OTBizszN MYXEUXNQ NYXacIlYcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MDDuUS=> M4f3elE4Ozl3NUm0
MDCK M3L4U2tqdmG|ZTDhd5NigQ>? MV\+NVAh|ryP MX7EUXNQ NUfiO3UxcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MECgcm0> MlPvNVc{QTV3OUS=
PC3 NX2xNmJmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX2xNEDPxE1? NFrQW3ZFVVOR NVnZVnlie2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NXizOldYOTd|OUW1PVQ>
REF52 NUDWfmRkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3P3OVExKM7:TR?= NGK5bIVFVVOR MUTzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MXixO|M6PTV7NB?=
MDCK MV\BdI9xfG:|aYOgZZN{[Xl? NXzkXpRLOTBizszN NWTq[pJxTE2VTx?= M2fWdIlv\HWlZYOgZZBweHSxc3nz NHHLZpoyPzN7NUW5OC=>
REF52 NYPOcY5kSXCxcITvd4l{KGG|c3H5 MVmxNEDPxE1? M{PS[WROW09? NHzvXlVqdmS3Y3XzJIFxd3C2b4Ppdy=> Mm\NNVc{QTV3OUS=
REF52 Ml;hSpVv[3Srb36gZZN{[Xl? NFvSN|QyOCEQvF2= NI[0NYpFVVOR M1nBZ4Jtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? NELufm4yPzN7NUW5OC=>
platelet M4H1dWZ2dmO2aX;uJIF{e2G7 NVLBUms1OSEQvF2= MVjEUXNQ MnHkbY5pcWKrdIOgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIIPwdoVi\GmwZx?= MlfWNVk4OTZ6MEO=
platelet M1WyUWZ2dmO2aX;uJIF{e2G7 MXSxJO69VQ>? Mn;TSG1UVw>? MXrs[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW M{HGbFE6PzF4OECz
platelet MkjuSpVv[3Srb36gZZN{[Xl? MnjTNUDPxE1? NF;3SmVFVVOR NYrTNHhI[myxY3vzJINidGOrdX2gcY9jcWyrenH0bY9vKGGwZDDk[Y5{\SCpcnHueYxmKHOnY4LleIlwdg>? MVyxPVcyPjhyMx?=
4T1 Mn3ZSpVv[3Srb36gZZN{[Xl? MVvEUXNQ NFq1O2Fi[m:uaYPo[ZMhfGinIHnueIVz[WO2aX;uJIJmfHenZX6g{tI{KGmwdHXndolvKGGwZDDU{tJTNUmL MkfZNVk4PDB2M{O=
MCF7 NUDKZWc{U2mwYYPlJIF{e2G7 NYS5U3R7hjFyIN88US=> NV\vT|NNTE2VTx?= NEXJN29qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDR|MDDuUS=> M{\4OVIxOzV2N{iw
TamR MnzFT4lv[XOnIHHzd4F6 NGnwdVl,OTBizszN NUewRmNlTE2VTx?= MlLJbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MXKyNFM2PDd6MB?=
FasR M2POdGtqdmG|ZTDhd5NigQ>? MYH+NVAh|ryP Mm\wSG1UVw>? M1zuWolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N NFXWc2UzODN3NEe4NC=>
TamR NHWwUZVHfW6ldHnvckBie3OjeR?= M32zfFEh|ryP M2n5XGROW09? MXvpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NIHBdFEzODN3NEe4NC=>
FasR NFLwWndHfW6ldHnvckBie3OjeR?= M2rkTlEh|ryP M4i3XWROW09? MlfTbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NVPkO29ZOjB|NUS3PFA>
endothelial cell NH3OU4VMcW6jc3WgZZN{[Xl? M17VdVQxKG6P NYTQcG5KTE2VTx?= NEH5XFFqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MVqyNVIyOjRyMh?=
endothelial cell MonqSpVv[3Srb36gZZN{[Xl? NFvqTHo1OCCwTR?= NYjDelloTE2VTx?= MUHpcohq[mm2czDINm8zNWmwZIXj[YQhe3S{ZYPzJIZq[mW{IH\vdo1ifGmxbh?= M3\EbVIyOjF{NECy
endothelial cell MWPBdI9xfG:|aYOgZZN{[Xl? NEPTWZQ1OCCwTR?= NGPVOWRFVVOR NF;EOItqdmirYnn0d{BieG:ydH;zbZM> M{W2ZVIyOjF{NECy
GH3 MVnGeY5kfGmxbjDhd5NigQ>? NIH0NVU{KM7:TR?= M1uyVmROW09? NYPtXoJbcW6lcnXhd4V{KEmNKFPhLUBidXCuaYT1[IU> MUmyNVkzPTVzMh?=
GH3 MoOySpVv[3Srb36gZZN{[Xl? NEDyRmw{KM7:TR?= NUHZ[IdRTE2VTx?= MoHG[Y5p[W6lZYOgRmtE[S2laHHucoVtKGGldHn2bZR6 MnPUNlE6OjV3MUK=
HUVEC MnTEZ5l1d3SxeHnjbZR6KGG|c3H5 MUn+NVAh|ryP NHn6ZmVFVVOR M2DJdolueGGrcoOg[Y5ld3SqZXzpZYwh[2WubDD2bYFjcWyrdIm= NXHYPYQ{OjJyN{WwOVc>
HUVEC MmPuT4lv[XOnIHHzd4F6 NGq4SIU2KM7:TR?= NUH6OmVmTE2VTx?= MUXpcohq[mm2czDGRWshc2mwYYPlJIFkfGm4aYT5 MmWxNlIxPzVyNUe=
HUVEC MYjGeY5kfGmxbjDhd5NigQ>? NXe1WlZvPSEQvF2= M2ni[2ROW09? M1j1UYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M3:4R|IzODd3MEW3
HUVEC NX;ZU|V5SXCxcITvd4l{KGG|c3H5 NFX6UFE2KM7:TR?= M{jlSWROW09? NHTHV3dqdmS3Y3XzJIFxd3C2b4Ppdy=> M1ewdFIzODd3MEW3
HUVEC MmnjSpVv[3Srb36gZZN{[Xl? M{P2cVUh|ryP M3n0e2ROW09? NHvP[Y5qdXCnZHXzJIVv\G:2aHXsbYFtKGOnbHygcYloemG2aX;uJIFv\CCjbITldpMhfGinIHPlcIx2dGG{IHHjeIlvKGO7dH;zb4Vt\XSxbh?= MkKzNlIxPzVyNUe=
HUVEC NXK3VJRvTnWwY4Tpc44h[XO|YYm= MlnmOUDPxE1? MXHEUXNQ NVX2PXd6[myxY3vzJGhWXkWFIIPwdo92fGmwZzDvckBkd2yuYXflckBKKGenbIO= MX[yNlA4PTB3Nx?=
human peripheral blood T cells M33DO2tqdmG|ZTDhd5NigQ>? NVm0UWlOhjFyIN88US=> M{n1XWROW09? NGXUR4RqdmirYnn0d{B{cXSnLYPw[YNq\mmlIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> M3;KeVI{QTJ6MUi4
human peripheral blood T cells M2LlNmZ2dmO2aX;uJIF{e2G7 NELrWXp,OTBizszN NYLESpBJTE2VTx?= NXjzXY5qcW2yYXnyd{BVS1JvaX7keYNm\CCWIHPlcIwhdW:{cHjvcI9ocWOjbDDjbIFv\2W|IHHu[EBidHSncoOgZYN1cX[rdImgc4YhWmixQR?= MmexNlM6OjhzOEi=
human peripheral blood T cells MojOSpVv[3Srb36gZZN{[Xl? NULrOnRyhjFyIN88US=> M1jldmROW09? NFr6WZhqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhYkGSLUewJIFv\CCOQWS= M{LuNVI{QTJ6MUi4
human peripheral blood T cells M1rCc2Z2dmO2aX;uJIF{e2G7 NIjNZlR,OTBizszN MXHEUXNQ NXXNOnRycW2yYXnyd{BCdnSrZ3XuMYRmeGWwZHXueEBVKGOnbHygZ49vcnWpYYTpc44> NHXEclEzOzl{OEG4PC=>

... Click to View More Cell Line Experimental Data

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:

[1]

+ Expand

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
Cell Research:

[1]

+ Expand
  • Cell lines: REF52 or PC3 cells
  • Concentrations: ~10 μM
  • Incubation Time: 3 days
  • Method:

    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)
Animal Research:

[2]

+ Expand
  • Animal Models: Ctrl-MT and MFCKO-MT mice
  • Formulation: --
  • Dosages: 5 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL (52.9 mM)
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
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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • 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)?

  • 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.

FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID