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.

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In DMSO USD 190 In stock
USD 147 In stock
USD 570 In stock
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Cited by 33 Publications

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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 MkD3T4lv[XOnIHHzd4F6 MX;+NVAh|ryP NYXNOVdOTE2VTx?= Ml[2bY5pcWKrdIOgSmFMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMUGgcm0> NYLXcmRYOTd|OUW1PVQ>
REF52 NV3jXGFFU2mwYYPlJIF{e2G7 MYr+NVAh|ryP NEjW[3ZFVVOR NYrwfGYycW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iC-MUCwJI5O MmXKNVc{QTV3OUS=
PC3 MnjkT4lv[XOnIHHzd4F6 MUn+NVAh|ryP MXnEUXNQ NI\KVppqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDFyMDDuUS=> MXixO|M6PTV7NB?=
SKOV-3 NXTYc4JjU2mwYYPlJIF{e2G7 NVjxRYxlhjFyIN88US=> NGS3PJFFVVOR M2W0XIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= NFfYSWkyPzN7NUW5OC=>
L3.6p1 Mm[5T4lv[XOnIHHzd4F6 M4rBWZ4yOCEQvF2= M2\RTWROW09? NIPORlRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDNyMDDuUS=> MYmxO|M6PTV7NB?=
F-G M3TOPGtqdmG|ZTDhd5NigQ>? NFn4OZN,OTBizszN M4i5UmROW09? MYnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxKG6P M{HwclE4Ozl3NUm0
MDCK MXPLbY5ie2ViYYPzZZk> NHHTUHZ,OTBizszN NXTvR|h{TE2VTx?= M1;KcolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTByIH7N M3G4WFE4Ozl3NUm0
PC3 NFLIbZVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPIO2wyOCEQvF2= MX;EUXNQ NXX1V4VKe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> MVGxO|M6PTV7NB?=
REF52 M3TVSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{XKPFExKM7:TR?= MYjEUXNQ MkDDd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NHnDcIoyPzN7NUW5OC=>
MDCK MmrpRZBweHSxc3nzJIF{e2G7 NWWzd5JqOTBizszN MoDjSG1UVw>? MVXpcoR2[2W|IHHwc5B1d3Orcx?= NIO4fYoyPzN7NUW5OC=>
REF52 NFvCXmlCeG:ydH;zbZMh[XO|YYm= MkP3NVAh|ryP NELwcJdFVVOR NYTmfnhncW6mdXPld{BieG:ydH;zbZM> NFPhWmYyPzN7NUW5OC=>
REF52 NYK2bIRLTnWwY4Tpc44h[XO|YYm= NWDlcZYyOTBizszN M4DadmROW09? MkfnZoxw[2u|IIPldpVuKGGwZDDGUk1{fGmvdXzheIVlKG2rZ4LheIlwdg>? NGTKZZgyPzN7NUW5OC=>
platelet M4jye2Z2dmO2aX;uJIF{e2G7 M3LvVFEh|ryP NFnDbpdFVVOR NGHEco5qdmirYnn0d{BxdGG2ZXzleEBi\2e{ZXfheIlwdiCjbnSgd5Bz\WGmaX7n MYOxPVcyPjhyMx?=
platelet M1\kR2Z2dmO2aX;uJIF{e2G7 Ml3jNUDPxE1? MkW3SG1UVw>? NYnIdWgxdGWjZIOgeI8hcW6qaXLpeIlwdiCxZjDQRWsh[W6mIFHLWC=> NVq5dmR6OTl5MU[4NFM>
platelet M{G5e2Z2dmO2aX;uJIF{e2G7 NHrzbXkyKM7:TR?= M1;oNGROW09? M3HnNIJtd2OtczDjZYxkcXWvIH3vZoltcXqjdHnvckBidmRiZHXud4Uh\3KjboXs[UB{\WO{ZYTpc44> MXKxPVcyPjhyMx?=
4T1 NXjpRWZyTnWwY4Tpc44h[XO|YYm= M1;P[mROW09? Mn7uZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? M33r[FE6PzRyNEOz
MCF7 M133[2tqdmG|ZTDhd5NigQ>? MV\+NVAh|ryP NVHYTHplTE2VTx?= NUHBUopVcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB2M{Cgcm0> NXvyUlRDOjB|NUS3PFA>
TamR MV\LbY5ie2ViYYPzZZk> MoD2glExKM7:TR?= M2TiOWROW09? M3OyNIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= MXOyNFM2PDd6MB?=
FasR NILvbHFMcW6jc3WgZZN{[Xl? MkjsglExKM7:TR?= NWHIbJZSTE2VTx?= NIjHPIlqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDF|MDDuUS=> NYGwUYpyOjB|NUS3PFA>
TamR Mn7OSpVv[3Srb36gZZN{[Xl? NV20VXBEOSEQvF2= MkjkSG1UVw>? MYLpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MlzsNlA{PTR5OEC=
FasR M3fZTWZ2dmO2aX;uJIF{e2G7 MUCxJO69VQ>? MoK1SG1UVw>? M3ey[4lvcGmkaYTzJINmdGxibXnndoF1cW:w NHzNPIszODN3NEe4NC=>
endothelial cell MXXLbY5ie2ViYYPzZZk> M4LT[lQxKG6P M2fTTGROW09? MVTpcohq[mm2czDINm8zNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKE[DSx?= NETHOo0zOTJzMkSwNi=>
endothelial cell Mlq0SpVv[3Srb36gZZN{[Xl? M2DNXlQxKG6P NFrnV2ZFVVOR M1zjTolvcGmkaYTzJGgzVzJvaX7keYNm\CC|dILld5Mh\mmkZYKg[o9zdWG2aX;u NEnpUFQzOTJzMkSwNi=>
endothelial cell MXPBdI9xfG:|aYOgZZN{[Xl? MYi0NEBvVQ>? MXnEUXNQ NX;pR2NJcW6qaXLpeJMh[XCxcITvd4l{ NY\Vd4JGOjF{MUK0NFI>
GH3 MVHGeY5kfGmxbjDhd5NigQ>? MlPWN{DPxE1? NHr6fY5FVVOR M2TyS4lv[3KnYYPld{BKUyiFYTmgZY1xdGm2dXTl M3qyeFIyQTJ3NUGy
GH3 M{Pwe2Z2dmO2aX;uJIF{e2G7 NHzPe24{KM7:TR?= Ml;vSG1UVw>? MmH1[Y5p[W6lZYOgRmtE[S2laHHucoVtKGGldHn2bZR6 NIfBWHkzOTl{NUWxNi=>
HUVEC MV3jfZRwfG:6aXPpeJkh[XO|YYm= MXH+NVAh|ryP NET1NIpFVVOR MnzubY1x[Wm{czDlcoRwfGinbHnhcEBk\WyuII\pZYJqdGm2eR?= NGnFNJYzOjB5NUC1Oy=>
HUVEC NIPpVmJMcW6jc3WgZZN{[Xl? NH\lclc2KM7:TR?= NFjNcXZFVVOR NX7WO2xVcW6qaXLpeJMhTkGNIHvpcoF{\SCjY4Tpeol1gQ>? MmfPNlIxPzVyNUe=
HUVEC MkW1SpVv[3Srb36gZZN{[Xl? M3K5cFUh|ryP NGLScINFVVOR MYfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mk\3NlIxPzVyNUe=
HUVEC M4G1cmFxd3C2b4Ppd{Bie3OjeR?= NYHoR3dYPSEQvF2= NFXadoNFVVOR MVfpcoR2[2W|IHHwc5B1d3Orcx?= M2XOfFIzODd3MEW3
HUVEC NX7adoY4TnWwY4Tpc44h[XO|YYm= NXn4TWs3PSEQvF2= MmGzSG1UVw>? Ml[zbY1x\WSnczDlcoRwfGinbHnhcEBk\WyuIH3p[5JifGmxbjDhcoQh[Wy2ZYLzJJRp\SClZXzseYxieiCjY4TpckBkgXSxc3vlcIV1d25? NED4WJozOjB5NUC1Oy=>
HUVEC Mn;1SpVv[3Srb36gZZN{[Xl? M1z0OFUh|ryP MYjEUXNQ NXHCUHN3[myxY3vzJGhWXkWFIIPwdo92fGmwZzDvckBkd2yuYXflckBKKGenbIO= NUL5cW9WOjJyN{WwOVc>
human peripheral blood T cells MX\LbY5ie2ViYYPzZZk> MorFglExKM7:TR?= NGfoPGhFVVOR NHPi[lRqdmirYnn0d{B{cXSnLYPw[YNq\mmlIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> MnP5NlM6OjhzOEi=
human peripheral blood T cells M3G2d2Z2dmO2aX;uJIF{e2G7 M3\hSp4yOCEQvF2= NWrKb5M4TE2VTx?= NEHMb5ZqdXCjaYLzJHREWi2rbnT1Z4VlKFRiY3XscEBud3KyaH;sc4dq[2GuIHPoZY5o\XNiYX7kJIFtfGW{czDhZ5Rqfmm2eTDv[kBTcG:D NHXOUmwzOzl{OEG4PC=>
human peripheral blood T cells M2Xq[2Z2dmO2aX;uJIF{e2G7 NF\idYh,OTBizszN NVTiNY4yTE2VTx?= M4jhWIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBbSVBvN{CgZY5lKEyDVB?= MV:yN|kzQDF6OB?=
human peripheral blood T cells M16xRmZ2dmO2aX;uJIF{e2G7 NX;WTWpDhjFyIN88US=> MXXEUXNQ NVzsWZRrcW2yYXnyd{BCdnSrZ3XuMYRmeGWwZHXueEBVKGOnbHygZ49vcnWpYYTpc44> NYSwfZIxOjN7MkixPFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1; 

PubMed: 30761269     


(D) On the third day, PF-573228-treated cells were harvested and subjected to Western blot analysis for cyclin B1. Cyclin B1 levels were much higher in A549 cells with 1 μM PF-573228 or without PF-573228 treatment than in the cells treated with higher concentrations of PF-573228. (E) After 10 μM PF-573228 treatment, cyclin B1 levels declined markedly in H460 cells. (F) PF-573228 administration slightly reduced cyclin B1 levels in H1299 cells. 

p-FAK / FAK ; 

PubMed: 30761269     


FAK expression levels and FAK activity, as measured by the phosphorylation of FAK at tyrosine 576 and 577, were quantified by Western blot analysis after treatment of lung cancer cells with PF-573228 for 3 days.

Lamin A / Lamin C; 

PubMed: 30761269     


(B) The cells treated with 10 μM PF-573228 exhibited a decrease in p-FAK levels. Lamin A and lamin C expression levels were much lower in A549 cells exposed to 10 μM PF-573228. 

30761269
Immunofluorescence
FAK / F-actin; 

PubMed: 30761269     


(B) The cells were stained with phalloidin to visualize F-actin (red) and a FAK antibody to visualize the FAK distribution (green). In cells without PF-573228 administration, FAK translocated to focal adhesions at the tips of actin stress fibers, and the focal adhesions were relatively large. When cells were exposed to 10 μM PF-573228, FAK translocation to focal adhesions was reduced, and the sizes of the focal adhesions were smaller. Nuclei in cells treated with PF-573228 were deformed, as visualized with DAPI staining, whereas most nuclei in cells without PF-573228 treatment were oval shaped. 

Emerin; 

PubMed: 30761269     


(A) After PF-573228 treatment of A549 cells, the cells were fixed and stained with phalloidin to label F-actin (red) and an antibody against emerin (green) to outline the nuclear shape. Cells treated with PF-573228 were extremely large and had deformed nuclei, whereas mostly oval-like nuclei were present in the cells without PF-573228 treatment. 

30761269
Growth inhibition assay
Cell viability; 

PubMed: 30761269     


Three different types of lung cancer cells, (A) A549 lung adenocarcinoma and (B) H460, and (C) H1299 large cell carcinoma, were selected for the PF-573228 administration regimen. Cell growth curves of the three lung cancer cell lines treated with various doses of PF-573228 for 4 days were established. The administration of PF-573228 at 10 μM to the lung cancer cells effectively suppressed cell growth in vitro, as proliferative activity totally ceased in the cells exposed to 10 μM PF-573228.

30761269
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]

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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
Cell Research:

[1]

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  • 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]

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  • 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.

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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