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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3 Customer Reviews

  • Nature, 2016, 537(7620):422-429.. 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 NUC2epRzU2mwYYPlJIF{e2G7 NVnUPIZwhjFyIN88US=> NIjFVWRFVVOR NXvzW|NtcW6qaXLpeJMhTkGNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVEhdk1? NIXuZ5UyPzN7NUW5OC=>
REF52 MXfLbY5ie2ViYYPzZZk> MoixglExKM7:TR?= MYDEUXNQ MorPbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kB,OTByIH7N NWDLV4p5OTd|OUW1PVQ>
PC3 NXLZPGtrU2mwYYPlJIF{e2G7 Mo\4glExKM7:TR?= NUnlVIlYTE2VTx?= NXLkcGdncW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iBzMECgcm0> M3nRd|E4Ozl3NUm0
SKOV-3 MXLLbY5ie2ViYYPzZZk> NFPaOmF,OTBizszN MVvEUXNQ NWfDWXpGcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB3MDDuUS=> MVyxO|M6PTV7NB?=
L3.6p1 NI\HfoVMcW6jc3WgZZN{[Xl? MoXXglExKM7:TR?= M1rHcGROW09? NVfPbnRycW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MECgcm0> Mn21NVc{QTV3OUS=
F-G MlH0T4lv[XOnIHHzd4F6 Mn74glExKM7:TR?= MlG1SG1UVw>? M{\Rb4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzBibl2= MlHnNVc{QTV3OUS=
MDCK NXL1bnA5U2mwYYPlJIF{e2G7 NGDWUVN,OTBizszN MYXEUXNQ MnvjbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2ODBibl2= NFvVcGIyPzN7NUW5OC=>
PC3 NFLrcmRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHnOV2wyOCEQvF2= M2jwNWROW09? NELi[od{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> NH3TN|AyPzN7NUW5OC=>
REF52 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4TxRVExKM7:TR?= NXPQbWpxTE2VTx?= MYTzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= Mn[2NVc{QTV3OUS=
MDCK NWHTRlY5SXCxcITvd4l{KGG|c3H5 MXSxNEDPxE1? MVrEUXNQ NH\uPFdqdmS3Y3XzJIFxd3C2b4Ppdy=> NV;EZ|VrOTd|OUW1PVQ>
REF52 MYXBdI9xfG:|aYOgZZN{[Xl? Mkn4NVAh|ryP NUjncZJVTE2VTx?= MVLpcoR2[2W|IHHwc5B1d3Orcx?= MXexO|M6PTV7NB?=
REF52 NWH0S4NxTnWwY4Tpc44h[XO|YYm= MknVNVAh|ryP MlvOSG1UVw>? MUTicI9kc3Nic3XyeY0h[W6mIF\OMZN1cW23bHH0[YQhdWmpcnH0bY9v NYrrVI1nOTd|OUW1PVQ>
platelet MlfHSpVv[3Srb36gZZN{[Xl? M3u5SlEh|ryP NIj1TJRFVVOR MXPpcohq[mm2czDwcIF1\WyndDDh[4dz\WejdHnvckBidmRic4Dy[YFlcW6p NHHsb2QyQTdzNkiwNy=>
platelet MUjGeY5kfGmxbjDhd5NigQ>? M3fGV|Eh|ryP MWHEUXNQ MkG2cIVi\HNidH:gbY5pcWKrdHnvckBw\iCSQVugZY5lKEGNVB?= NH\mZnMyQTdzNkiwNy=>
platelet M1ztRmZ2dmO2aX;uJIF{e2G7 NFj0[pgyKM7:TR?= MmjhSG1UVw>? NIP6elNjdG:la4OgZ4Ft[2m3bTDtc4JqdGm8YYTpc44h[W6mIHTlcpNmKGe{YX71cIUhe2WlcnX0bY9v NH7td2cyQTdzNkiwNy=>
4T1 M{PqRWZ2dmO2aX;uJIF{e2G7 MV\EUXNQ MkHRZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? MXOxPVc1ODR|Mx?=
MCF7 M1[4VGtqdmG|ZTDhd5NigQ>? M{fLOp4yOCEQvF2= NFiweY1FVVOR MXTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFQ{OCCwTR?= NETrUGszODN3NEe4NC=>
TamR NVyydoM1U2mwYYPlJIF{e2G7 MlL6glExKM7:TR?= MXfEUXNQ MWfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxKG6P NF7LWmIzODN3NEe4NC=>
FasR MYPLbY5ie2ViYYPzZZk> MX;+NVAh|ryP M{j3PGROW09? M4\ZR4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N MlfZNlA{PTR5OEC=
TamR NG[3OZZHfW6ldHnvckBie3OjeR?= MlToNUDPxE1? M4nCcmROW09? NUj4NI9ZcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NEnkO3czODN3NEe4NC=>
FasR M3j1TGZ2dmO2aX;uJIF{e2G7 MUOxJO69VQ>? M33VXGROW09? MV\pcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? Mn7SNlA{PTR5OEC=
endothelial cell M2KxWGtqdmG|ZTDhd5NigQ>? M2H5cVQxKG6P NV7UfG1PTE2VTx?= NHToSldqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MonqNlEzOTJ2MEK=
endothelial cell MWLGeY5kfGmxbjDhd5NigQ>? NYD5eVRGPDBibl2= MUTEUXNQ MnX4bY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHO2cnXzd{BncWKncjDmc5Ju[XSrb36= MkDVNlEzOTJ2MEK=
endothelial cell MWrBdI9xfG:|aYOgZZN{[Xl? MV[0NEBvVQ>? NI\GZ4hFVVOR NHmwUI9qdmirYnn0d{BieG:ydH;zbZM> M{ja[VIyOjF{NECy
GH3 NEjKTXFHfW6ldHnvckBie3OjeR?= NHm3WGE{KM7:TR?= MoHuSG1UVw>? MVLpcoNz\WG|ZYOgTWspS2FrIHHtdIxqfHWmZR?= MWOyNVkzPTVzMh?=
GH3 NHPQNY5HfW6ldHnvckBie3OjeR?= M{HkeVMh|ryP MWXEUXNQ MYDlcohidmOnczDCT2NiNWOqYX7u[Ywh[WO2aY\peJk> MXyyNVkzPTVzMh?=
HUVEC NGjzd|hkgXSxdH;4bYNqfHliYYPzZZk> NIHac2R,OTBizszN MXTEUXNQ Mn7wbY1x[Wm{czDlcoRwfGinbHnhcEBk\WyuII\pZYJqdGm2eR?= NG\jUJIzOjB5NUC1Oy=>
HUVEC M1nWdGtqdmG|ZTDhd5NigQ>? MmW1OUDPxE1? M1rZ[2ROW09? MYPpcohq[mm2czDGRWshc2mwYYPlJIFkfGm4aYT5 M{jUT|IzODd3MEW3
HUVEC NH62VY5HfW6ldHnvckBie3OjeR?= MYS1JO69VQ>? Mn[1SG1UVw>? MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NU\ORZVLOjJyN{WwOVc>
HUVEC NWrERnY2SXCxcITvd4l{KGG|c3H5 M4\3[|Uh|ryP M3fGOmROW09? M3XaOolv\HWlZYOgZZBweHSxc3nz MofYNlIxPzVyNUe=
HUVEC NVHQ[IJkTnWwY4Tpc44h[XO|YYm= NGS0c4k2KM7:TR?= NIr5VpJFVVOR M{HYZ4lueGWmZYOg[Y5ld3SqZXzpZYwh[2WubDDtbYdz[XSrb36gZY5lKGGudHXyd{B1cGViY3XscJVt[XJiYXP0bY4h[3m2b4Pr[YxmfG:w MVmyNlA4PTB3Nx?=
HUVEC NEjhSVdHfW6ldHnvckBie3OjeR?= MojnOUDPxE1? MX\EUXNQ MXHicI9kc3NiSGXWSWMhe3C{b4X0bY5oKG:wIHPvcIxi\2WwIFmg[4Vtew>? MXKyNlA4PTB3Nx?=
human peripheral blood T cells NHvmS21McW6jc3WgZZN{[Xl? M4rqRZ4yOCEQvF2= M4jEN2ROW09? NYj4TYs4cW6qaXLpeJMhe2m2ZT3zdIVkcW[rYzDwbI9{eGixconsZZRqd25ib3[gSmFM MWqyN|kzQDF6OB?=
human peripheral blood T cells NV3Xe4J5TnWwY4Tpc44h[XO|YYm= M4rlU54yOCEQvF2= NVzMU3U1TE2VTx?= NHzRSZJqdXCjaYLzJHREWi2rbnT1Z4VlKFRiY3XscEBud3KyaH;sc4dq[2GuIHPoZY5o\XNiYX7kJIFtfGW{czDhZ5Rqfmm2eTDv[kBTcG:D NUDqcIg{OjN7MkixPFg>
human peripheral blood T cells MVzGeY5kfGmxbjDhd5NigQ>? MYf+NVAh|ryP M1\T[GROW09? MXjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gXmFRNTdyIHHu[EBNSVR? NX3q[5pOOjN7MkixPFg>
human peripheral blood T cells M{TKfWZ2dmO2aX;uJIF{e2G7 MmXkglExKM7:TR?= NGLKfXZFVVOR M2PyRolueGGrcoOgRY51cWenbj3k[ZBmdmSnboSgWEBk\WyuIHPvcop2\2G2aX;u M2XQRlI{QTJ6MUi4

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay
+ 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
+ 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 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 Information

Molecular Weight 491.49
Formula

C22H20F3N5O3S

CAS No. 869288-64-2
Storage powder
in solvent
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.

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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID