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

  • FAK inhibition blunted the increased migration induced by PGC1α depletion. G361 cells were subjected to 24 h transwell migration assays in the presence of DMSO or various doses of FAK inhibitor PF-573228. Images represent three pictures captured with scale bar representing 100 μm.

    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

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 NVnCcJBGU2mwYYPlJIF{e2G7 NGXxeox,OTBizszN Mn3jSG1UVw>? Mn\NbY5pcWKrdIOgSmFMKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMUGgcm0> NWGxRohsOTd|OUW1PVQ>
REF52 NELt[XdMcW6jc3WgZZN{[Xl? Mlv3glExKM7:TR?= M2TyNmROW09? MnzkbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kB,OTByIH7N M2TiblE4Ozl3NUm0
PC3 NV7qTJJLU2mwYYPlJIF{e2G7 M{i4ep4yOCEQvF2= NEfOVYhFVVOR NUfnS4ppcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzMECgcm0> M{DXWlE4Ozl3NUm0
SKOV-3 M17hWWtqdmG|ZTDhd5NigQ>? M320c54yOCEQvF2= NGe1N2hFVVOR NV3EdmtNcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=> NHuyNHAyPzN7NUW5OC=>
L3.6p1 MofuT4lv[XOnIHHzd4F6 M3H4SZ4yOCEQvF2= NX71XWxHTE2VTx?= NYXSS4hlcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MECgcm0> NWjHfpd5OTd|OUW1PVQ>
F-G Mle3T4lv[XOnIHHzd4F6 NEL6U2Z,OTBizszN M4\Y[GROW09? MWDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxKG6P MXmxO|M6PTV7NB?=
MDCK M4\NWmtqdmG|ZTDhd5NigQ>? NWDpT5hWhjFyIN88US=> M1HpOmROW09? NWPjT3hxcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MECgcm0> M{HQU|E4Ozl3NUm0
PC3 MnfVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MY[xNEDPxE1? NX:3d2NqTE2VTx?= NYXENYZ[e2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> M1L4SFE4Ozl3NUm0
REF52 MofzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3;FS|ExKM7:TR?= NHrxWVFFVVOR M3XUepNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu MUCxO|M6PTV7NB?=
MDCK MYTBdI9xfG:|aYOgZZN{[Xl? NYjqU|Z1OTBizszN MnGxSG1UVw>? MWrpcoR2[2W|IHHwc5B1d3Orcx?= NHLWRYwyPzN7NUW5OC=>
REF52 M{jCS2Fxd3C2b4Ppd{Bie3OjeR?= NUTBfmZwOTBizszN NEP1T3NFVVOR MoDSbY5lfWOnczDhdI9xfG:|aYO= MoezNVc{QTV3OUS=
REF52 M{HHRmZ2dmO2aX;uJIF{e2G7 NGTHcYUyOCEQvF2= MULEUXNQ M3y2c4Jtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? MV:xO|M6PTV7NB?=
platelet MYrGeY5kfGmxbjDhd5NigQ>? MmjyNUDPxE1? NIH3RWVFVVOR MUXpcohq[mm2czDwcIF1\WyndDDh[4dz\WejdHnvckBidmRic4Dy[YFlcW6p MUGxPVcyPjhyMx?=
platelet MXLGeY5kfGmxbjDhd5NigQ>? NXrlXYJ4OSEQvF2= NIfV[3RFVVOR NHXnV21t\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU Mn;XNVk4OTZ6MEO=
platelet MWXGeY5kfGmxbjDhd5NigQ>? M4fZZ|Eh|ryP NVTsdWJLTE2VTx?= NVrKTZB{[myxY3vzJINidGOrdX2gcY9jcWyrenH0bY9vKGGwZDDk[Y5{\SCpcnHueYxmKHOnY4LleIlwdg>? NFW5SGgyQTdzNkiwNy=>
4T1 Mk\vSpVv[3Srb36gZZN{[Xl? NVfOSJliTE2VTx?= NH6wW5pi[m:uaYPo[ZMhfGinIHnueIVz[WO2aX;uJIJmfHenZX6g{tI{KGmwdHXndolvKGGwZDDU{tJTNUmL MlHqNVk4PDB2M{O=
MCF7 M3PCeGtqdmG|ZTDhd5NigQ>? MlG0glExKM7:TR?= M2TXfGROW09? NF\IbXRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDR|MDDuUS=> M3Hr[VIxOzV2N{iw
TamR Mk\oT4lv[XOnIHHzd4F6 NFuwbIt,OTBizszN M1vLVGROW09? MkTWbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MYiyNFM2PDd6MB?=
FasR M4jQSmtqdmG|ZTDhd5NigQ>? Mo\OglExKM7:TR?= Ml3WSG1UVw>? M17lcYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N M2X5RlIxOzV2N{iw
TamR NGrGbVdHfW6ldHnvckBie3OjeR?= NXHqWGlUOSEQvF2= M1T0OWROW09? MoTDbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? Ml3WNlA{PTR5OEC=
FasR MYTGeY5kfGmxbjDhd5NigQ>? NIe5T5IyKM7:TR?= NYTn[VJHTE2VTx?= NInsUFdqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= M3TYcFIxOzV2N{iw
endothelial cell NVjQboZQU2mwYYPlJIF{e2G7 M1\lWFQxKG6P NX\HNJJ2TE2VTx?= MX3pcohq[mm2czDINm8zNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKE[DSx?= NIHGUW4zOTJzMkSwNi=>
endothelial cell MXPGeY5kfGmxbjDhd5NigQ>? M4fTPVQxKG6P M1rycmROW09? MVXpcohq[mm2czDINm8zNWmwZIXj[YQhe3S{ZYPzJIZq[mW{IH\vdo1ifGmxbh?= MVqyNVIyOjRyMh?=
endothelial cell MUjBdI9xfG:|aYOgZZN{[Xl? MnfHOFAhdk1? M2TZRWROW09? Mn\IbY5pcWKrdIOgZZBweHSxc3nz M3Hxb|IyOjF{NECy
GH3 NGTRNlVHfW6ldHnvckBie3OjeR?= NFXZZ2k{KM7:TR?= MWPEUXNQ NU\oO|VmcW6lcnXhd4V{KEmNKFPhLUBidXCuaYT1[IU> MUGyNVkzPTVzMh?=
GH3 M1rhTGZ2dmO2aX;uJIF{e2G7 MnzFN{DPxE1? NFyzPGtFVVOR MUjlcohidmOnczDCT2NiNWOqYX7u[Ywh[WO2aY\peJk> M1jxc|IyQTJ3NUGy
HUVEC MVzjfZRwfG:6aXPpeJkh[XO|YYm= M1W5fZ4yOCEQvF2= MnPGSG1UVw>? MojObY1x[Wm{czDlcoRwfGinbHnhcEBk\WyuII\pZYJqdGm2eR?= NXTGR|d[OjJyN{WwOVc>
HUVEC NYe5c3VFU2mwYYPlJIF{e2G7 M3jKRVUh|ryP M121d2ROW09? NX:zU|l6cW6qaXLpeJMhTkGNIHvpcoF{\SCjY4Tpeol1gQ>? NXjGc5J3OjJyN{WwOVc>
HUVEC MWnGeY5kfGmxbjDhd5NigQ>? NXfKSXNOPSEQvF2= MmfKSG1UVw>? M1vrcolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MYmyNlA4PTB3Nx?=
HUVEC MV3BdI9xfG:|aYOgZZN{[Xl? MXO1JO69VQ>? MWjEUXNQ M1fHfYlv\HWlZYOgZZBweHSxc3nz MmrRNlIxPzVyNUe=
HUVEC MonKSpVv[3Srb36gZZN{[Xl? M3\uc|Uh|ryP NIfSdYNFVVOR MXHpcZBm\GW|IHXu[I91cGWuaXHsJINmdGxibXnndoF1cW:wIHHu[EBidHSncoOgeIhmKGOnbHz1cIFzKGGldHnuJIN6fG:|a3Xs[ZRwdg>? Mmf1NlIxPzVyNUe=
HUVEC MonLSpVv[3Srb36gZZN{[Xl? MlLoOUDPxE1? NGjaPJJFVVOR M3X1ZoJtd2OtczDIWXZGSyC|cILveZRqdmdib36gZ49tdGGpZX6gTUBo\Wy| NVr0N|M6OjJyN{WwOVc>
human peripheral blood T cells MnjwT4lv[XOnIHHzd4F6 NFfKeWx,OTBizszN M{jyb2ROW09? NXTVS4JpcW6qaXLpeJMhe2m2ZT3zdIVkcW[rYzDwbI9{eGixconsZZRqd25ib3[gSmFM NVLrRZFXOjN7MkixPFg>
human peripheral blood T cells M1S2U2Z2dmO2aX;uJIF{e2G7 M1LyRZ4yOCEQvF2= Mlz0SG1UVw>? MVXpcZBicXK|IGTDVk1qdmS3Y3XkJHQh[2WubDDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZMh[W6mIHHseIVzeyCjY4Tpeol1gSCxZjDSbI9C MXqyN|kzQDF6OB?=
human peripheral blood T cells Mn\HSpVv[3Srb36gZZN{[Xl? MUj+NVAh|ryP M{XsN2ROW09? M3T1W4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBbSVBvN{CgZY5lKEyDVB?= NYL1UGh6OjN7MkixPFg>
human peripheral blood T cells MWTGeY5kfGmxbjDhd5NigQ>? NVzucJdNhjFyIN88US=> MXvEUXNQ NIT1RndqdXCjaYLzJGFvfGmpZX6t[IVx\W6mZX70JHQh[2WubDDjc45rfWejdHnvci=> NXmzXpp3OjN7MkixPFg>

... Click to View More Cell Line Experimental Data

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]

+ 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
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)
Animal Research:

[2]

+ Expand
  • 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 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
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

Tel: +1-832-582-8158 Ext:3

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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