PF-573228

Catalog No.S2013

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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PF-573228 Chemical Structure

PF-573228 Chemical Structure
Molecular Weight: 491.49

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

Related Compound Libraries

PF-573228 is available in the following compound libraries:

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A431NFXhd4RMcW6jc3WgZZN{[Xl?NHnmPI9,OTBizszNMo\zSG1UVw>?MoLZbY5pcWKrdIOgSmFMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMUGgcm0>NX\iTHl7OTd|OUW1PVQ>
REF52MYnLbY5ie2ViYYPzZZk>M3vEcJ4yOCEQvF2=MVjEUXNQNELOVWlqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKH5zMECgcm0>NHzDcXUyPzN7NUW5OC=>
PC3MXvLbY5ie2ViYYPzZZk>NHPhSmp,OTBizszNNVLabXF{TE2VTx?=MlHSbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kAyODBibl2=Mn7ONVc{QTV3OUS=
SKOV-3NHe1bWFMcW6jc3WgZZN{[Xl?M3HDWp4yOCEQvF2=MnfCSG1UVw>?NUDzdXFzcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=>MXexO|M6PTV7NB?=
L3.6p1M3fz[2tqdmG|ZTDhd5NigQ>?NH\aZ2h,OTBizszNNFq4[GhFVVORNHjSXHJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDNyMDDuUS=>MmDPNVc{QTV3OUS=
F-GMlL2T4lv[XOnIHHzd4F6NIr2OYx,OTBizszNNHL3OXpFVVORMVfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxKG6PMYSxO|M6PTV7NB?=
MDCKMlj5T4lv[XOnIHHzd4F6NWjQNWFChjFyIN88US=>NU\B[m03TE2VTx?=NGP3VnFqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=>NVfrbJhWOTd|OUW1PVQ>
PC3MlvES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NGj3emEyOCEQvF2=MYDEUXNQMoW4d4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6=MWmxO|M6PTV7NB?=
REF52M2njSmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7MnfWNVAh|ryPM4fJ[2ROW09?MoPTd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6=NW\XOmFwOTd|OUW1PVQ>
MDCKMX;BdI9xfG:|aYOgZZN{[Xl?MWixNEDPxE1?MX7EUXNQMorubY5lfWOnczDhdI9xfG:|aYO=NWDPUotkOTd|OUW1PVQ>
REF52MlK4RZBweHSxc3nzJIF{e2G7M1vPVFExKM7:TR?=NHT4R29FVVORMm\mbY5lfWOnczDhdI9xfG:|aYO=NV\SeZRXOTd|OUW1PVQ>
REF52NVjSNZFiTnWwY4Tpc44h[XO|YYm=MXGxNEDPxE1?M{L5XmROW09?M3nOSoJtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25?M1:3OFE4Ozl3NUm0
plateletM1zle2Z2dmO2aX;uJIF{e2G7MnLONUDPxE1?MYLEUXNQMY\pcohq[mm2czDwcIF1\WyndDDh[4dz\WejdHnvckBidmRic4Dy[YFlcW6pMmDYNVk4OTZ6MEO=
plateletNHm5VXZHfW6ldHnvckBie3OjeR?=NVXTbYFlOSEQvF2=NYX1[3RuTE2VTx?=M4TOXYxm[WS|IITvJIlvcGmkaYTpc44hd2ZiUFHLJIFv\CCDS2S=NF;5ZlQyQTdzNkiwNy=>
plateletM{nPdmZ2dmO2aX;uJIF{e2G7NYK0cmVXOSEQvF2=NHS2SmZFVVORMnn2Zoxw[2u|IHPhcINqfW1ibX;ibYxqgmG2aX;uJIFv\CCmZX7z[UBoemGwdXzlJJNm[3KndHnvci=>M3jhfVE6PzF4OECz
4T1MYPGeY5kfGmxbjDhd5NigQ>?NF;FdJFFVVORMlz3ZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>?NIDMXHkyQTd2MESzNy=>
MCF7MXXLbY5ie2ViYYPzZZk>NVvqNZY4hjFyIN88US=>M{H0WGROW09?NHX1OFZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDR|MDDuUS=>MYmyNFM2PDd6MB?=
TamRNUnZPIdiU2mwYYPlJIF{e2G7MYf+NVAh|ryPNXLwdm1ITE2VTx?=MnHUbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?=M4rSXVIxOzV2N{iw
FasRM{fWbmtqdmG|ZTDhd5NigQ>?NWH3[o4yhjFyIN88US=>MmH1SG1UVw>?M{PTdIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7NNHzn[|kzODN3NEe4NC=>
TamRNY\GZXc4TnWwY4Tpc44h[XO|YYm=NXTyZ4pzOSEQvF2=NI\3UldFVVORNEPIRXZqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?=MWGyNFM2PDd6MB?=
FasRNFPVc5JHfW6ldHnvckBie3OjeR?=MWCxJO69VQ>?NULZN5RVTE2VTx?=MmrnbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25?MnO5NlA{PTR5OEC=
endothelial cellMXfLbY5ie2ViYYPzZZk>M{X5fFQxKG6PM2q5O2ROW09?NFv2eYpqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=>MXuyNVIyOjRyMh?=
endothelial cellM2fWUWZ2dmO2aX;uJIF{e2G7MYW0NEBvVQ>?MoLSSG1UVw>?M4exU4lvcGmkaYTzJGgzVzJvaX7keYNm\CC|dILld5Mh\mmkZYKg[o9zdWG2aX;uM3q3UFIyOjF{NECy
endothelial cellMYTBdI9xfG:|aYOgZZN{[Xl?NFvze401OCCwTR?=MkDzSG1UVw>?NYfnclhFcW6qaXLpeJMh[XCxcITvd4l{NWf4NWNUOjF{MUK0NFI>
GH3M{XmbmZ2dmO2aX;uJIF{e2G7NE\5bWE{KM7:TR?=MljqSG1UVw>?NH;zNWlqdmO{ZXHz[ZMhUUtqQ3GpJIFueGyrdIXk[S=>MUGyNVkzPTVzMh?=
GH3NXHaZ2NCTnWwY4Tpc44h[XO|YYm=NGrmO24{KM7:TR?=M1fTb2ROW09?NFfveIRmdmijbnPld{BDU0OjLXPoZY5v\WxiYXP0bZZqfHl?NHuwXW4zOTl{NUWxNi=>
HUVECMmH4Z5l1d3SxeHnjbZR6KGG|c3H5M2PEdJ4yOCEQvF2=M{HrXWROW09?MXHpcZBicXK|IHXu[I91cGWuaXHsJINmdGxidnnhZoltcXS7MUiyNlA4PTB3Nx?=
HUVECNHP6c41McW6jc3WgZZN{[Xl?M{e2V|Uh|ryPMVfEUXNQNXLQN2NNcW6qaXLpeJMhTkGNIHvpcoF{\SCjY4Tpeol1gQ>?MkjoNlIxPzVyNUe=
HUVECNIrIOXJHfW6ldHnvckBie3OjeR?=NV3qbpp4PSEQvF2=M2fuZ2ROW09?NET1PGpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0NE\aZlYzOjB5NUC1Oy=>
HUVECM1fJRWFxd3C2b4Ppd{Bie3OjeR?=Mlm1OUDPxE1?MmTOSG1UVw>?M33hNolv\HWlZYOgZZBweHSxc3nzNEH0XVkzOjB5NUC1Oy=>
HUVECNFzmNWtHfW6ldHnvckBie3OjeR?=NUDmWJozPSEQvF2=MkHiSG1UVw>?NXHz[IQ1cW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36=MonONlIxPzVyNUe=
HUVECM2X4cWZ2dmO2aX;uJIF{e2G7NFrTV5Y2KM7:TR?=NFHjOINFVVORNIrjRZFjdG:la4OgTHVXTUNic4Dyc5V1cW6pIH;uJINwdGyjZ3XuJGkh\2Wucx?=MkjJNlIxPzVyNUe=
human peripheral blood T cellsNE\QNINMcW6jc3WgZZN{[Xl?M2TvN54yOCEQvF2=MYrEUXNQNUjucoxncW6qaXLpeJMhe2m2ZT3zdIVkcW[rYzDwbI9{eGixconsZZRqd25ib3[gSmFMNEDlVmUzOzl{OEG4PC=>
human peripheral blood T cellsNI\oTHVHfW6ldHnvckBie3OjeR?=NWLLcllVhjFyIN88US=>M4W0d2ROW09?MW\pcZBicXK|IGTDVk1qdmS3Y3XkJHQh[2WubDDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZMh[W6mIHHseIVzeyCjY4Tpeol1gSCxZjDSbI9CMo\ENlM6OjhzOEi=
human peripheral blood T cellsMoftSpVv[3Srb36gZZN{[Xl?M4GxZp4yOCEQvF2=MlK5SG1UVw>?NUm4eHZJcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFqDUD23NEBidmRiTFHUMlLYNlM6OjhzOEi=
human peripheral blood T cellsM4PPN2Z2dmO2aX;uJIF{e2G7MoTCglExKM7:TR?=NIHGeIhFVVORMoTtbY1x[Wm{czDBcpRq\2WwLXTldIVv\GWwdDDUJINmdGxiY3;ubpVo[XSrb36=M13mPFI{QTJ6MUi4

... Click to View More Cell Line Experimental Data

In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Slack-Davis JK, et al. J Biol Chem, 2007, 282(20), 14845-14852.

Chemical Information

Download PF-573228 SDF
Molecular Weight (MW) 491.49
Formula

C22H20F3N5O3S

CAS No. 869288-64-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 26 mg/mL (52.9 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 2(1H)-Quinolinone, 3,4-dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-

Customer Product Validation (2)


Click to enlarge
Rating
Source PLoS One 2014 9(2), e88588. PF-573228 purchased from Selleck
Method Western blot
Cell Lines OVISE cells
Concentrations 0.01-10 uM
Incubation Time 24 h
Results OVISE cells were incubated for 25 hr at the indicated concentrations of the FAK inhibitors. Immunoblots wereperformed to assess inhibition of auto-phosphorylation by the FAK inhibitors.

Click to enlarge
Rating
Source 2014 Dr.Milica Pesic from Institute for Biological Research. PF-573228 purchased from Selleck
Method MTT
Cell Lines NC-H460, COR-L23
Concentrations 0-25 uM
Incubation Time 72 h
Results Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Focal adhesion kinase (FAK) inhibitor PF-573228.

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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