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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4 Customer Reviews

  • Nature, 2016, 537(7620):422-429.. 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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NXHvNHFvU2mwYYPlJIF{e2G7 NH\yOm1,OTBizszN M{DpZWROW09? NFjiboRqdmirYnn0d{BHSUticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNUBvVQ>? M2HybFE4Ozl3NUm0
REF52 NGrvOWZMcW6jc3WgZZN{[Xl? NV;zWVU1hjFyIN88US=> MUfEUXNQ M3voVIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhhjFyMDDuUS=> MlTQNVc{QTV3OUS=
PC3 MU\LbY5ie2ViYYPzZZk> M1nEVZ4yOCEQvF2= MVLEUXNQ NEnn[5lqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDFyMDDuUS=> NHK0V3EyPzN7NUW5OC=>
SKOV-3 NXXSNZQ{U2mwYYPlJIF{e2G7 MVv+NVAh|ryP MUjEUXNQ NH3jPGRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N M33TXFE4Ozl3NUm0
L3.6p1 MnjLT4lv[XOnIHHzd4F6 M{fSXp4yOCEQvF2= NHPjTIVFVVOR MVPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxOCCwTR?= MoXwNVc{QTV3OUS=
F-G NVjHUVJ4U2mwYYPlJIF{e2G7 NYLQPIpKhjFyIN88US=> M4DLWWROW09? NVvJdmt3cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MDDuUS=> Ml;zNVc{QTV3OUS=
MDCK NFnhRllMcW6jc3WgZZN{[Xl? NV\pT2NZhjFyIN88US=> MX;EUXNQ MXjpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxOCCwTR?= MkLGNVc{QTV3OUS=
PC3 M4OyS2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHfkSo0yOCEQvF2= NEXLOo9FVVOR M3juPJNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NXH4PGU3OTd|OUW1PVQ>
REF52 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYLiZZVpOTBizszN M1i5[WROW09? M1nnfZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NXXabWhEOTd|OUW1PVQ>
MDCK MUnBdI9xfG:|aYOgZZN{[Xl? M2XzOVExKM7:TR?= NIDDZVNFVVOR M1vONYlv\HWlZYOgZZBweHSxc3nz NVvxe3pKOTd|OUW1PVQ>
REF52 MVrBdI9xfG:|aYOgZZN{[Xl? NWe4b3h6OTBizszN NHrhTZRFVVOR NI\nUmVqdmS3Y3XzJIFxd3C2b4Ppdy=> MmW2NVc{QTV3OUS=
REF52 NUC5WJRTTnWwY4Tpc44h[XO|YYm= NULjb4txOTBizszN NHTNdItFVVOR MWTicI9kc3Nic3XyeY0h[W6mIF\OMZN1cW23bHH0[YQhdWmpcnH0bY9v NEH1WpUyPzN7NUW5OC=>
platelet NU[2dmJyTnWwY4Tpc44h[XO|YYm= MnG5NUDPxE1? NWXMS3JTTE2VTx?= NED4ZWtqdmirYnn0d{BxdGG2ZXzleEBi\2e{ZXfheIlwdiCjbnSgd5Bz\WGmaX7n MUOxPVcyPjhyMx?=
platelet Mlf0SpVv[3Srb36gZZN{[Xl? NH3pWYsyKM7:TR?= NWrRN4dlTE2VTx?= MX7s[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW MVixPVcyPjhyMx?=
platelet NHnRVVhHfW6ldHnvckBie3OjeR?= NIfyWFEyKM7:TR?= MnTzSG1UVw>? MmLJZoxw[2u|IHPhcINqfW1ibX;ibYxqgmG2aX;uJIFv\CCmZX7z[UBoemGwdXzlJJNm[3KndHnvci=> MXWxPVcyPjhyMx?=
4T1 MlH6SpVv[3Srb36gZZN{[Xl? NYXtTFlITE2VTx?= MXLhZo9tcXOqZYOgeIhmKGmwdHXyZYN1cW:wIHLleJdm\W5izsKzJIlvfGWpcnnuJIFv\CCWzsLSMWlK MUexPVc1ODR|Mx?=
MCF7 MYjLbY5ie2ViYYPzZZk> MnLJglExKM7:TR?= M{jNOmROW09? NH;ofmFqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDR|MDDuUS=> M1\udlIxOzV2N{iw
TamR NXrMVVVbU2mwYYPlJIF{e2G7 NXznW49QhjFyIN88US=> NGHCc4tFVVOR M4DWUolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= NEXzTFYzODN3NEe4NC=>
FasR NF;6eXVMcW6jc3WgZZN{[Xl? M3HXN54yOCEQvF2= M1e1[GROW09? M3TCTolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N M2H5bFIxOzV2N{iw
TamR M1f5WmZ2dmO2aX;uJIF{e2G7 NVThcG5kOSEQvF2= MYXEUXNQ MUDpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? M{GyelIxOzV2N{iw
FasR NF7ld3JHfW6ldHnvckBie3OjeR?= NYf3XnRVOSEQvF2= NVP2R2VFTE2VTx?= MlXibY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? M1HaTVIxOzV2N{iw
endothelial cell M4CzPGtqdmG|ZTDhd5NigQ>? NYPTcZFZPDBibl2= MULEUXNQ MUjpcohq[mm2czDINm8zNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKE[DSx?= NYnZfnlWOjF{MUK0NFI>
endothelial cell MVTGeY5kfGmxbjDhd5NigQ>? NFrCXpQ1OCCwTR?= M4\Rc2ROW09? NWr4R3ZxcW6qaXLpeJMhUDKRMj3pcoR2[2WmIIP0doV{eyCoaXLldkBnd3KvYYTpc44> MknrNlEzOTJ2MEK=
endothelial cell NGjRSHNCeG:ydH;zbZMh[XO|YYm= NUPtXWJEPDBibl2= NITCfm5FVVOR NWXwV21RcW6qaXLpeJMh[XCxcITvd4l{ M3mxXlIyOjF{NECy
GH3 NUPpSo06TnWwY4Tpc44h[XO|YYm= MVKzJO69VQ>? NGr5RoRFVVOR NX3VcoF4cW6lcnXhd4V{KEmNKFPhLUBidXCuaYT1[IU> MlTPNlE6OjV3MUK=
GH3 MWXGeY5kfGmxbjDhd5NigQ>? NX\zN2pjOyEQvF2= NYrKUVRwTE2VTx?= M4q1bYVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? NUPJNndFOjF7MkW1NVI>
HUVEC MYTjfZRwfG:6aXPpeJkh[XO|YYm= MV\+NVAh|ryP MYjEUXNQ MUTpcZBicXK|IHXu[I91cGWuaXHsJINmdGxidnnhZoltcXS7 MU[yNlA4PTB3Nx?=
HUVEC MmH4T4lv[XOnIHHzd4F6 MVe1JO69VQ>? M4DFXWROW09? M{PTeolvcGmkaYTzJGZCUyCtaX7hd4Uh[WO2aY\peJk> NECwNGgzOjB5NUC1Oy=>
HUVEC M2TVc2Z2dmO2aX;uJIF{e2G7 MYG1JO69VQ>? M4TTUGROW09? M4HRXIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHj3UpgzOjB5NUC1Oy=>
HUVEC NH2zTVFCeG:ydH;zbZMh[XO|YYm= M1;CWVUh|ryP M4\XcmROW09? MUnpcoR2[2W|IHHwc5B1d3Orcx?= NXPrPFd4OjJyN{WwOVc>
HUVEC NEfSOmRHfW6ldHnvckBie3OjeR?= MoHTOUDPxE1? NEnkboRFVVOR M1PoTYlueGWmZYOg[Y5ld3SqZXzpZYwh[2WubDDtbYdz[XSrb36gZY5lKGGudHXyd{B1cGViY3XscJVt[XJiYXP0bY4h[3m2b4Pr[YxmfG:w MmDpNlIxPzVyNUe=
HUVEC NYj4SJhsTnWwY4Tpc44h[XO|YYm= MV61JO69VQ>? NYDVOWd4TE2VTx?= MWricI9kc3NiSGXWSWMhe3C{b4X0bY5oKG:wIHPvcIxi\2WwIFmg[4Vtew>? MkLQNlIxPzVyNUe=
human peripheral blood T cells NXfZV45oU2mwYYPlJIF{e2G7 NHu4R4F,OTBizszN M1TJemROW09? M4jydolvcGmkaYTzJJNqfGVvc4DlZ4lncWNicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> NFrwOWgzOzl{OEG4PC=>
human peripheral blood T cells MXnGeY5kfGmxbjDhd5NigQ>? MkS0glExKM7:TR?= NFvGTHZFVVOR MULpcZBicXK|IGTDVk1qdmS3Y3XkJHQh[2WubDDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZMh[W6mIHHseIVzeyCjY4Tpeol1gSCxZjDSbI9C MljnNlM6OjhzOEi=
human peripheral blood T cells NH\zOYVHfW6ldHnvckBie3OjeR?= M4fUTJ4yOCEQvF2= MmOySG1UVw>? NUTufoR{cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFqDUD23NEBidmRiTFHU M{XX[|I{QTJ6MUi4
human peripheral blood T cells NEHwN2lHfW6ldHnvckBie3OjeR?= MofNglExKM7:TR?= NXPYVZBSTE2VTx?= NYfWe|lTcW2yYXnyd{BCdnSrZ3XuMYRmeGWwZHXueEBVKGOnbHygZ49vcnWpYYTpc44> NWfFS|B2OjN7MkixPFg>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+45% PEG 300+ddH2O 8mg/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 Information

Molecular Weight 491.49
Formula

C22H20F3N5O3S

CAS No. 869288-64-2
Storage powder
in solvent
Synonyms N/A

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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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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID