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

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 M{DjSmtqdmG|ZTDhd5NigQ>? MWj+NVAh|ryP MmfGSG1UVw>? NEPhdJZqdmirYnn0d{BHSUticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNUBvVQ>? MmTRNVc{QTV3OUS=
REF52 MXPLbY5ie2ViYYPzZZk> NGjhe3Z,OTBizszN NVzjepBoTE2VTx?= NHmzdYFqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKH5zMECgcm0> NWnJd4d6OTd|OUW1PVQ>
PC3 MY\LbY5ie2ViYYPzZZk> MoPwglExKM7:TR?= NGTyeZNFVVOR NGP2N3RqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDFyMDDuUS=> NHT2N48yPzN7NUW5OC=>
SKOV-3 NVSwUmJHU2mwYYPlJIF{e2G7 NVXSe5hlhjFyIN88US=> MmS3SG1UVw>? NEj6U29qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N NX3lPWJ3OTd|OUW1PVQ>
L3.6p1 NVrGSWF5U2mwYYPlJIF{e2G7 NEXMRZp,OTBizszN MUTEUXNQ M33jZYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzByIH7N Mnf4NVc{QTV3OUS=
F-G MWnLbY5ie2ViYYPzZZk> MY\+NVAh|ryP NU\BeFdxTE2VTx?= NWT4TJI4cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MDDuUS=> NGSwZ44yPzN7NUW5OC=>
MDCK MUnLbY5ie2ViYYPzZZk> NGjsO3Z,OTBizszN MYTEUXNQ NF61[pBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=> MWKxO|M6PTV7NB?=
PC3 M3HFOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3zVelExKM7:TR?= M1fJV2ROW09? MX\zbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= M{PKNFE4Ozl3NUm0
REF52 M3GwTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;BTFExKM7:TR?= MlXCSG1UVw>? MWrzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= MWKxO|M6PTV7NB?=
MDCK NXjJRWZtSXCxcITvd4l{KGG|c3H5 MUixNEDPxE1? NULNVm9sTE2VTx?= NH3tXpdqdmS3Y3XzJIFxd3C2b4Ppdy=> MXKxO|M6PTV7NB?=
REF52 MmqyRZBweHSxc3nzJIF{e2G7 M3P3UFExKM7:TR?= M1SyUmROW09? NI\OWZBqdmS3Y3XzJIFxd3C2b4Ppdy=> MlHYNVc{QTV3OUS=
REF52 MWfGeY5kfGmxbjDhd5NigQ>? NHP4V3MyOCEQvF2= MYnEUXNQ MljPZoxw[2u|IIPldpVuKGGwZDDGUk1{fGmvdXzheIVlKG2rZ4LheIlwdg>? NIGxTXQyPzN7NUW5OC=>
platelet MXjGeY5kfGmxbjDhd5NigQ>? Mn;6NUDPxE1? M2TVbmROW09? NUPFc|F1cW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> NXXVUW9LOTl5MU[4NFM>
platelet M{DGeGZ2dmO2aX;uJIF{e2G7 M3W0XlEh|ryP M{\Ed2ROW09? NELMN5Vt\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU M3W0[lE6PzF4OECz
platelet MlLGSpVv[3Srb36gZZN{[Xl? M1zDUlEh|ryP M{PEVGROW09? MmXnZoxw[2u|IHPhcINqfW1ibX;ibYxqgmG2aX;uJIFv\CCmZX7z[UBoemGwdXzlJJNm[3KndHnvci=> NIfCcmkyQTdzNkiwNy=>
4T1 M4HxdmZ2dmO2aX;uJIF{e2G7 Ml3VSG1UVw>? MUnhZo9tcXOqZYOgeIhmKGmwdHXyZYN1cW:wIHLleJdm\W5izsKzJIlvfGWpcnnuJIFv\CCWzsLSMWlK M1\iU|E6PzRyNEOz
MCF7 Mn3aT4lv[XOnIHHzd4F6 NFj4Oo1,OTBizszN M1\ndGROW09? NW\MXpc6cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB2M{Cgcm0> NHjyTnMzODN3NEe4NC=>
TamR NXjLVWw5U2mwYYPlJIF{e2G7 MV\+NVAh|ryP NYXZNIh3TE2VTx?= NXrL[FNUcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=> MVmyNFM2PDd6MB?=
FasR NXH1eWlPU2mwYYPlJIF{e2G7 M2LJWZ4yOCEQvF2= NGDOWpBFVVOR NFP4T4FqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDF|MDDuUS=> NF3pfpkzODN3NEe4NC=>
TamR NI\4S5lHfW6ldHnvckBie3OjeR?= Ml\qNUDPxE1? MX\EUXNQ MmDGbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NFnmOWozODN3NEe4NC=>
FasR Mlv4SpVv[3Srb36gZZN{[Xl? Mn;xNUDPxE1? M3fTdmROW09? MWXpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? Mom5NlA{PTR5OEC=
endothelial cell NXT4b3I{U2mwYYPlJIF{e2G7 NUnYO2diPDBibl2= NXfIS5BwTE2VTx?= NXvjV3FUcW6qaXLpeJMhUDKRMj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> MYqyNVIyOjRyMh?=
endothelial cell MmfrSpVv[3Srb36gZZN{[Xl? NH7vc|E1OCCwTR?= NEnIUG1FVVOR MlzQbY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHO2cnXzd{BncWKncjDmc5Ju[XSrb36= Ml\RNlEzOTJ2MEK=
endothelial cell MoHuRZBweHSxc3nzJIF{e2G7 NVf2elRvPDBibl2= M{\1NmROW09? NU\vNIhxcW6qaXLpeJMh[XCxcITvd4l{ M2\W[|IyOjF{NECy
GH3 NGjORWFHfW6ldHnvckBie3OjeR?= MWqzJO69VQ>? M2TJTmROW09? NH3WXmRqdmO{ZXHz[ZMhUUtqQ3GpJIFueGyrdIXk[S=> M1T0SFIyQTJ3NUGy
GH3 MlvXSpVv[3Srb36gZZN{[Xl? M{fGfFMh|ryP NEPGNWRFVVOR NEPVXZlmdmijbnPld{BDU0OjLXPoZY5v\WxiYXP0bZZqfHl? MXqyNVkzPTVzMh?=
HUVEC NX;FfmVO[3m2b4TvfIlkcXS7IHHzd4F6 NXvPW282hjFyIN88US=> MWPEUXNQ Mki1bY1x[Wm{czDlcoRwfGinbHnhcEBk\WyuII\pZYJqdGm2eR?= MWeyNlA4PTB3Nx?=
HUVEC MXXLbY5ie2ViYYPzZZk> NIDtfY82KM7:TR?= MVHEUXNQ M3v0N4lvcGmkaYTzJGZCUyCtaX7hd4Uh[WO2aY\peJk> NFL2NGozOjB5NUC1Oy=>
HUVEC MVXGeY5kfGmxbjDhd5NigQ>? M{W1XlUh|ryP MVfEUXNQ M4D6SYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NIHtT|gzOjB5NUC1Oy=>
HUVEC NGnUUmlCeG:ydH;zbZMh[XO|YYm= MYm1JO69VQ>? M3rVTGROW09? NE\4dJRqdmS3Y3XzJIFxd3C2b4Ppdy=> MmD2NlIxPzVyNUe=
HUVEC MUHGeY5kfGmxbjDhd5NigQ>? MWS1JO69VQ>? M2G4TWROW09? MUTpcZBm\GW|IHXu[I91cGWuaXHsJINmdGxibXnndoF1cW:wIHHu[EBidHSncoOgeIhmKGOnbHz1cIFzKGGldHnuJIN6fG:|a3Xs[ZRwdg>? MoLUNlIxPzVyNUe=
HUVEC MWrGeY5kfGmxbjDhd5NigQ>? M{\CclUh|ryP MX;EUXNQ NH\3THBjdG:la4OgTHVXTUNic4Dyc5V1cW6pIH;uJINwdGyjZ3XuJGkh\2Wucx?= NIfORmUzOjB5NUC1Oy=>
human peripheral blood T cells NFfFWI1McW6jc3WgZZN{[Xl? NV\q[YpOhjFyIN88US=> MonUSG1UVw>? Mnr4bY5pcWKrdIOgd4l1\S2|cHXjbYZq[yCyaH;zdIhwenmuYYTpc44hd2ZiRlHL NYrJNXQ5OjN7MkixPFg>
human peripheral blood T cells NVi1d5BzTnWwY4Tpc44h[XO|YYm= MofQglExKM7:TR?= NUnkenh5TE2VTx?= M3\aVIlueGGrcoOgWGNTNWmwZIXj[YQhXCClZXzsJI1wenCqb3zv[4lk[WxiY3jhcodmeyCjbnSgZYx1\XK|IHHjeIl3cXS7IH;mJHJpd0F? MWKyN|kzQDF6OB?=
human peripheral blood T cells M1XwdGZ2dmO2aX;uJIF{e2G7 NF3R[JB,OTBizszN NVzLUIZLTE2VTx?= NYDoVWJpcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFqDUD23NEBidmRiTFHU MnnrNlM6OjhzOEi=
human peripheral blood T cells MWLGeY5kfGmxbjDhd5NigQ>? NWHLXYVXhjFyIN88US=> MVjEUXNQ NEnobJpqdXCjaYLzJGFvfGmpZX6t[IVx\W6mZX70JHQh[2WubDDjc45rfWejdHnvci=> M4XR[lI{QTJ6MUi4

... 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