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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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 NHzrVJRMcW6jc3WgZZN{[Xl? NXm2Omh1hjFyIN88US=> NUHpUmROTE2VTx?= M3jo[olvcGmkaYTzJGZCUyCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGxJI5O MXSxO|M6PTV7NB?=
REF52 NXm2cI42U2mwYYPlJIF{e2G7 M2PLZp4yOCEQvF2= M4q0dmROW09? M{XjcIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhhjFyMDDuUS=> NV74fZJ5OTd|OUW1PVQ>
PC3 MX\LbY5ie2ViYYPzZZk> NGf6Ond,OTBizszN MV;EUXNQ NFf0WXRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDFyMDDuUS=> NInj[IgyPzN7NUW5OC=>
SKOV-3 NGrET|VMcW6jc3WgZZN{[Xl? MXL+NVAh|ryP M3LpR2ROW09? NWH3SYpzcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=> MVyxO|M6PTV7NB?=
L3.6p1 MWrLbY5ie2ViYYPzZZk> NWr1XnpihjFyIN88US=> NWDKSWVxTE2VTx?= MofUbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{ODBibl2= NXX4V5JmOTd|OUW1PVQ>
F-G MWnLbY5ie2ViYYPzZZk> M4DGOJ4yOCEQvF2= MXrEUXNQ NVLhSYx2cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MDDuUS=> NInSWpIyPzN7NUW5OC=>
MDCK NED6TJpMcW6jc3WgZZN{[Xl? M3viW54yOCEQvF2= M1HBZWROW09? NG\kNJBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=> NXvLXYRTOTd|OUW1PVQ>
PC3 Ml3OS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWW5[FRIOTBizszN MXjEUXNQ M4Pr[pNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NYDQWWd3OTd|OUW1PVQ>
REF52 MmDNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mkn3NVAh|ryP Ml\XSG1UVw>? Mn62d4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= MV[xO|M6PTV7NB?=
MDCK M1vKU2Fxd3C2b4Ppd{Bie3OjeR?= NVvF[pJXOTBizszN NV7iSGV7TE2VTx?= NYDFNVdncW6mdXPld{BieG:ydH;zbZM> MVOxO|M6PTV7NB?=
REF52 NEnvSo5CeG:ydH;zbZMh[XO|YYm= NECzepMyOCEQvF2= MXLEUXNQ NYLiOJFzcW6mdXPld{BieG:ydH;zbZM> NXfRNJA1OTd|OUW1PVQ>
REF52 M1XEfGZ2dmO2aX;uJIF{e2G7 NVi3WmdqOTBizszN MV\EUXNQ M3rDXoJtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? MXuxO|M6PTV7NB?=
platelet M2jBZWZ2dmO2aX;uJIF{e2G7 MX6xJO69VQ>? NUHRWodXTE2VTx?= M4LIfYlvcGmkaYTzJJBt[XSnbHX0JIFo\3KnZ3H0bY9vKGGwZDDzdJJm[WSrbne= M{XYTVE6PzF4OECz
platelet MXHGeY5kfGmxbjDhd5NigQ>? Ml2xNUDPxE1? MnHoSG1UVw>? MYXs[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW NIL2S3YyQTdzNkiwNy=>
platelet M4fnSmZ2dmO2aX;uJIF{e2G7 M4nYc|Eh|ryP M4L3PGROW09? MUDicI9kc3NiY3HsZ4l2dSCvb3LpcIl7[XSrb36gZY5lKGSnboPlJIdz[W63bHWgd4VkemW2aX;u NV\vbmxjOTl5MU[4NFM>
4T1 Mn2zSpVv[3Srb36gZZN{[Xl? Ml7OSG1UVw>? MUPhZo9tcXOqZYOgeIhmKGmwdHXyZYN1cW:wIHLleJdm\W5izsKzJIlvfGWpcnnuJIFv\CCWzsLSMWlK M1rESVE6PzRyNEOz
MCF7 MWrLbY5ie2ViYYPzZZk> MYT+NVAh|ryP MVzEUXNQ M1jhO4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPDNyIH7N Mo\QNlA{PTR5OEC=
TamR MWDLbY5ie2ViYYPzZZk> NEH6ZXN,OTBizszN NUX2TlVwTE2VTx?= MnrMbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MoLDNlA{PTR5OEC=
FasR NHLTdFRMcW6jc3WgZZN{[Xl? M3yyOZ4yOCEQvF2= NXHtZ4pNTE2VTx?= MkfYbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kAyOzBibl2= MWiyNFM2PDd6MB?=
TamR NGfsTIVHfW6ldHnvckBie3OjeR?= MkjONUDPxE1? NYf4N|ZITE2VTx?= M2jNTolvcGmkaYTzJINmdGxibXnndoF1cW:w MYeyNFM2PDd6MB?=
FasR M2n2SWZ2dmO2aX;uJIF{e2G7 MXexJO69VQ>? Mn3JSG1UVw>? MoLkbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MmDnNlA{PTR5OEC=
endothelial cell Mn:2T4lv[XOnIHHzd4F6 MV60NEBvVQ>? NXTTRVhrTE2VTx?= Ml3hbY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCIQVu= MlzkNlEzOTJ2MEK=
endothelial cell MUPGeY5kfGmxbjDhd5NigQ>? M2i3XFQxKG6P MlWzSG1UVw>? MXfpcohq[mm2czDINm8zNWmwZIXj[YQhe3S{ZYPzJIZq[mW{IH\vdo1ifGmxbh?= NFq5[5kzOTJzMkSwNi=>
endothelial cell NUTTOVZoSXCxcITvd4l{KGG|c3H5 NFm1SHk1OCCwTR?= MWjEUXNQ NW\ub3lCcW6qaXLpeJMh[XCxcITvd4l{ NYP4OVFqOjF{MUK0NFI>
GH3 NY\LWY9ITnWwY4Tpc44h[XO|YYm= MWKzJO69VQ>? NVTZ[nZsTE2VTx?= MmnkbY5kemWjc3XzJGlMMEOjKTDhcZBtcXS3ZHW= NUP5ZphJOjF7MkW1NVI>
GH3 NIPBT4lHfW6ldHnvckBie3OjeR?= NFvKTYw{KM7:TR?= MnP6SG1UVw>? M3;MWoVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? NGrwS4UzOTl{NUWxNi=>
HUVEC NIPi[3hkgXSxdH;4bYNqfHliYYPzZZk> NWrhc|NyhjFyIN88US=> M{\iPWROW09? MmjJbY1x[Wm{czDlcoRwfGinbHnhcEBk\WyuII\pZYJqdGm2eR?= NGGwfJczOjB5NUC1Oy=>
HUVEC MVnLbY5ie2ViYYPzZZk> MmXEOUDPxE1? M3jab2ROW09? Mof1bY5pcWKrdIOgSmFMKGurbnHz[UBi[3Srdnn0fS=> NFPiXJUzOjB5NUC1Oy=>
HUVEC MlXKSpVv[3Srb36gZZN{[Xl? NX7WNXVvPSEQvF2= NXzsbIFVTE2VTx?= NHzSfZpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M{H2dFIzODd3MEW3
HUVEC NHy2OoRCeG:ydH;zbZMh[XO|YYm= MXG1JO69VQ>? MnS0SG1UVw>? NHfzTGxqdmS3Y3XzJIFxd3C2b4Ppdy=> MnHKNlIxPzVyNUe=
HUVEC NYnz[Ih2TnWwY4Tpc44h[XO|YYm= M2DEcVUh|ryP MoLsSG1UVw>? NWDtcJg6cW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= MkW4NlIxPzVyNUe=
HUVEC NFX4R4FHfW6ldHnvckBie3OjeR?= MXi1JO69VQ>? MmjnSG1UVw>? M2PUfIJtd2OtczDIWXZGSyC|cILveZRqdmdib36gZ49tdGGpZX6gTUBo\Wy| NHrqcHUzOjB5NUC1Oy=>
human peripheral blood T cells MVnLbY5ie2ViYYPzZZk> NHPufXp,OTBizszN Moq3SG1UVw>? MWXpcohq[mm2czDzbZRmNXOyZXPp[olkKHCqb4PwbI9zgWyjdHnvckBw\iCIQVu= M13Vd|I{QTJ6MUi4
human peripheral blood T cells NGDu[XNHfW6ldHnvckBie3OjeR?= NVXTOmVbhjFyIN88US=> NVvU[GlJTE2VTx?= NED0Z2VqdXCjaYLzJHREWi2rbnT1Z4VlKFRiY3XscEBud3KyaH;sc4dq[2GuIHPoZY5o\XNiYX7kJIFtfGW{czDhZ5Rqfmm2eTDv[kBTcG:D M3HUZlI{QTJ6MUi4
human peripheral blood T cells M4LC[2Z2dmO2aX;uJIF{e2G7 Mk\SglExKM7:TR?= Ml;USG1UVw>? M3z0VIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBbSVBvN{CgZY5lKEyDVB?= NULtOpFWOjN7MkixPFg>
human peripheral blood T cells MkHXSpVv[3Srb36gZZN{[Xl? M{ixfZ4yOCEQvF2= M2n6TGROW09? NF[3ZnNqdXCjaYLzJGFvfGmpZX6t[IVx\W6mZX70JHQh[2WubDDjc45rfWejdHnvci=> MkDjNlM6OjhzOEi=

... 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+2% Tween 80+30% PEG 300+ddH2O
5mg/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