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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5 Customer Reviews

  • 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.

  • 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.

    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.

Purity & Quality Control

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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 MUHLbY5ie2ViYYPzZZk> NXL2c4ZVhjFyIN88US=> NXe1dGc6TE2VTx?= MYnpcohq[mm2czDGRWsheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzMTDuUS=> NYPUfIhCOTd|OUW1PVQ>
REF52 M2nhdWtqdmG|ZTDhd5NigQ>? MmCyglExKM7:TR?= MkXPSG1UVw>? NFLUVpNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKH5zMECgcm0> NHvyOYcyPzN7NUW5OC=>
PC3 MlLoT4lv[XOnIHHzd4F6 NW[4[JRShjFyIN88US=> M1j6fWROW09? M2rneIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTByIH7N M{TGU|E4Ozl3NUm0
SKOV-3 M2SwXGtqdmG|ZTDhd5NigQ>? NF6zRZV,OTBizszN NG[xVXBFVVOR NGnG[I5qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N MoHENVc{QTV3OUS=
L3.6p1 NIracZRMcW6jc3WgZZN{[Xl? MXH+NVAh|ryP NHGyRmdFVVOR Mo[5bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{ODBibl2= MUmxO|M6PTV7NB?=
F-G MnrRT4lv[XOnIHHzd4F6 NH\TbGZ,OTBizszN NFe5TZFFVVOR M2\kN4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzBibl2= NYLZZVZIOTd|OUW1PVQ>
MDCK NV7JVmNQU2mwYYPlJIF{e2G7 MXL+NVAh|ryP NXPiV4pXTE2VTx?= MknBbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2ODBibl2= MX6xO|M6PTV7NB?=
PC3 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXizdJJbOTBizszN NH3kbZBFVVOR NGLR[Ih{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> MVSxO|M6PTV7NB?=
REF52 NV:0eohqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUDWVWRpOTBizszN M13ZU2ROW09? MXzzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NWLzTI5tOTd|OUW1PVQ>
MDCK Mn;0RZBweHSxc3nzJIF{e2G7 M2TsV|ExKM7:TR?= MXHEUXNQ MY\pcoR2[2W|IHHwc5B1d3Orcx?= MUGxO|M6PTV7NB?=
REF52 MVzBdI9xfG:|aYOgZZN{[Xl? MUSxNEDPxE1? NXvjOVV{TE2VTx?= NGfj[lNqdmS3Y3XzJIFxd3C2b4Ppdy=> NH72PVkyPzN7NUW5OC=>
REF52 NXPRXnQ2TnWwY4Tpc44h[XO|YYm= Ml3mNVAh|ryP NEjVO4tFVVOR NVPMbG9S[myxY3vzJJNmenWvIHHu[EBHVi2|dHnteYxifGWmIH3p[5JifGmxbh?= MXGxO|M6PTV7NB?=
platelet M1[xU2Z2dmO2aX;uJIF{e2G7 NUPoRmdrOSEQvF2= NYLFd3dtTE2VTx?= M1;tXolvcGmkaYTzJJBt[XSnbHX0JIFo\3KnZ3H0bY9vKGGwZDDzdJJm[WSrbne= M2r1bFE6PzF4OECz
platelet NWfKNmFVTnWwY4Tpc44h[XO|YYm= NXvC[|NYOSEQvF2= M4nxVWROW09? NGPWfG1t\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU MlTuNVk4OTZ6MEO=
platelet MmfHSpVv[3Srb36gZZN{[Xl? MnXmNUDPxE1? NYHrbIdDTE2VTx?= M3ywdIJtd2OtczDjZYxkcXWvIH3vZoltcXqjdHnvckBidmRiZHXud4Uh\3KjboXs[UB{\WO{ZYTpc44> NVTtb4xDOTl5MU[4NFM>
4T1 M33jbmZ2dmO2aX;uJIF{e2G7 NGW5fphFVVOR MljGZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? Mo[0NVk4PDB2M{O=
MCF7 NXLmNFlDU2mwYYPlJIF{e2G7 MnW2glExKM7:TR?= NVG3[HNMTE2VTx?= NUP0eo1ncW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB2M{Cgcm0> MVOyNFM2PDd6MB?=
TamR M1z6ZmtqdmG|ZTDhd5NigQ>? M{j6[J4yOCEQvF2= NHzzd5VFVVOR MVPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxKG6P MkLUNlA{PTR5OEC=
FasR MULLbY5ie2ViYYPzZZk> NFK5dmZ,OTBizszN NUixZm5mTE2VTx?= NI[xT|ZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDF|MDDuUS=> NXjuW2p[OjB|NUS3PFA>
TamR MoKwSpVv[3Srb36gZZN{[Xl? NGXuSnYyKM7:TR?= NHjzeWJFVVOR NHnKfHZqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= NUTy[oYyOjB|NUS3PFA>
FasR M2rRe2Z2dmO2aX;uJIF{e2G7 M4HVXFEh|ryP NWLUSJFTTE2VTx?= MWTpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NYXOPGtpOjB|NUS3PFA>
endothelial cell M2K0TGtqdmG|ZTDhd5NigQ>? NYLlU3lxPDBibl2= MmXFSG1UVw>? NIO3dIZqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> NIfwZnozOTJzMkSwNi=>
endothelial cell MW\GeY5kfGmxbjDhd5NigQ>? MVq0NEBvVQ>? MUDEUXNQ M3LzfIlvcGmkaYTzJGgzVzJvaX7keYNm\CC|dILld5Mh\mmkZYKg[o9zdWG2aX;u MYmyNVIyOjRyMh?=
endothelial cell MUfBdI9xfG:|aYOgZZN{[Xl? NHrSUmE1OCCwTR?= M3viOmROW09? MlPibY5pcWKrdIOgZZBweHSxc3nz NH7tWoIzOTJzMkSwNi=>
GH3 NEnJTmhHfW6ldHnvckBie3OjeR?= MkL1N{DPxE1? NV3iZ|RyTE2VTx?= NIfNbWJqdmO{ZXHz[ZMhUUtqQ3GpJIFueGyrdIXk[S=> NYe0b2hlOjF7MkW1NVI>
GH3 MoHiSpVv[3Srb36gZZN{[Xl? NIXqeIw{KM7:TR?= MYrEUXNQ Mmm1[Y5p[W6lZYOgRmtE[S2laHHucoVtKGGldHn2bZR6 Mn7NNlE6OjV3MUK=
HUVEC MYnjfZRwfG:6aXPpeJkh[XO|YYm= NVr6NHJyhjFyIN88US=> MUHEUXNQ NGPETZFqdXCjaYLzJIVv\G:2aHXsbYFtKGOnbHygeoli[mmuaYT5 M4OxclIzODd3MEW3
HUVEC MlXWT4lv[XOnIHHzd4F6 NEXXXYY2KM7:TR?= MUPEUXNQ Mn7SbY5pcWKrdIOgSmFMKGurbnHz[UBi[3Srdnn0fS=> MkjDNlIxPzVyNUe=
HUVEC MXPGeY5kfGmxbjDhd5NigQ>? NW[wZVlJPSEQvF2= MkGwSG1UVw>? NGj3R2ZqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NFTpfZMzOjB5NUC1Oy=>
HUVEC NHnmTZZCeG:ydH;zbZMh[XO|YYm= NHLxdoU2KM7:TR?= M1;kfWROW09? NHuxZmNqdmS3Y3XzJIFxd3C2b4Ppdy=> M{fi[FIzODd3MEW3
HUVEC NE[yc3RHfW6ldHnvckBie3OjeR?= NI\Qdoc2KM7:TR?= Ml7ZSG1UVw>? NEnZZplqdXCnZHXzJIVv\G:2aHXsbYFtKGOnbHygcYloemG2aX;uJIFv\CCjbITldpMhfGinIHPlcIx2dGG{IHHjeIlvKGO7dH;zb4Vt\XSxbh?= MWCyNlA4PTB3Nx?=
HUVEC NHjET3VHfW6ldHnvckBie3OjeR?= Mnr3OUDPxE1? MX\EUXNQ MXvicI9kc3NiSGXWSWMhe3C{b4X0bY5oKG:wIHPvcIxi\2WwIFmg[4Vtew>? NGSwNYszOjB5NUC1Oy=>
human peripheral blood T cells NXXycm9tU2mwYYPlJIF{e2G7 MnTkglExKM7:TR?= NWrPTGlPTE2VTx?= MXfpcohq[mm2czDzbZRmNXOyZXPp[olkKHCqb4PwbI9zgWyjdHnvckBw\iCIQVu= MkmwNlM6OjhzOEi=
human peripheral blood T cells NEDxO4dHfW6ldHnvckBie3OjeR?= NXPHW2JYhjFyIN88US=> NFfSTVBFVVOR MknMbY1x[Wm{czDUR3IucW6mdXPl[EBVKGOnbHygcY9zeGixbH;nbYNidCClaHHu[4V{KGGwZDDhcJRmenNiYXP0bZZqfHlib3[gVohwSQ>? NWn2[nhqOjN7MkixPFg>
human peripheral blood T cells MXnGeY5kfGmxbjDhd5NigQ>? Mlj6glExKM7:TR?= NGjkVI5FVVOR MkXybY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHpCWC15MDDhcoQhVEGW NIryfJozOzl{OEG4PC=>
human peripheral blood T cells NYHibFFnTnWwY4Tpc44h[XO|YYm= NFra[ZJ,OTBizszN MWPEUXNQ M4jDc4lueGGrcoOgRY51cWenbj3k[ZBmdmSnboSgWEBk\WyuIHPvcop2\2G2aX;u MYWyN|kzQDF6OB?=

... Click to View More Cell Line Experimental Data

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', 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:[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)

Solubility (25°C)

In vitro DMSO 26 mg/mL (52.9 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
8mg/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

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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID