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 MofYT4lv[XOnIHHzd4F6 M2G1SZ4yOCEQvF2= MnzuSG1UVw>? NIXQbmRqdmirYnn0d{BHSUticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNUBvVQ>? NE\JcngyPzN7NUW5OC=>
REF52 MnuxT4lv[XOnIHHzd4F6 MV3+NVAh|ryP NHfOblFFVVOR NXjxXHQ6cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iC-MUCwJI5O NWO0OWozOTd|OUW1PVQ>
PC3 Mme0T4lv[XOnIHHzd4F6 NV\SWXNzhjFyIN88US=> NYrnXItRTE2VTx?= MWfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFExOCCwTR?= MYCxO|M6PTV7NB?=
SKOV-3 MUfLbY5ie2ViYYPzZZk> M2n1fJ4yOCEQvF2= NY[zeY9QTE2VTx?= MlLpbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= NH6yclQyPzN7NUW5OC=>
L3.6p1 Ml;VT4lv[XOnIHHzd4F6 MlHUglExKM7:TR?= M2Gzd2ROW09? NWLyZ2JucW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MECgcm0> NFzTVYMyPzN7NUW5OC=>
F-G M17nXmtqdmG|ZTDhd5NigQ>? NYm2dHR4hjFyIN88US=> NETIfHJFVVOR MYDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxKG6P M4jiVFE4Ozl3NUm0
MDCK NFTRbmtMcW6jc3WgZZN{[Xl? MXr+NVAh|ryP NEfXXY9FVVOR M4D0UIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTByIH7N NH;O[oYyPzN7NUW5OC=>
PC3 Ml7PS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUPEclJCOTBizszN NE\XNmNFVVOR NVWyVHVxe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> M4XzOVE4Ozl3NUm0
REF52 NVrZd3NuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;xbXMxOTBizszN NFrQVmxFVVOR NIPrfGN{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M3K3fVE4Ozl3NUm0
MDCK NXWxZXR5SXCxcITvd4l{KGG|c3H5 NEjEN3gyOCEQvF2= MYrEUXNQ NWjuUGZmcW6mdXPld{BieG:ydH;zbZM> M1zPSFE4Ozl3NUm0
REF52 MofkRZBweHSxc3nzJIF{e2G7 MmrzNVAh|ryP M1zoXGROW09? MXzpcoR2[2W|IHHwc5B1d3Orcx?= M2iwfVE4Ozl3NUm0
REF52 MYTGeY5kfGmxbjDhd5NigQ>? NHW4OHcyOCEQvF2= NYjQSpJQTE2VTx?= M4W1eoJtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? NHnuVYQyPzN7NUW5OC=>
platelet NH:zSmxHfW6ldHnvckBie3OjeR?= NU[0OJlTOSEQvF2= MlO3SG1UVw>? NXLXe4ZXcW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> NFfkV4UyQTdzNkiwNy=>
platelet NHfM[|RHfW6ldHnvckBie3OjeR?= NGTENo4yKM7:TR?= NIf3NG5FVVOR NFHX[HZt\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU NHHHUVMyQTdzNkiwNy=>
platelet NIWxepBHfW6ldHnvckBie3OjeR?= MXqxJO69VQ>? NWDxbIh6TE2VTx?= MoW3Zoxw[2u|IHPhcINqfW1ibX;ibYxqgmG2aX;uJIFv\CCmZX7z[UBoemGwdXzlJJNm[3KndHnvci=> NUjEcItMOTl5MU[4NFM>
4T1 MUDGeY5kfGmxbjDhd5NigQ>? NH;hUoxFVVOR NHPobXNi[m:uaYPo[ZMhfGinIHnueIVz[WO2aX;uJIJmfHenZX6g{tI{KGmwdHXndolvKGGwZDDU{tJTNUmL NI\Nc48yQTd2MESzNy=>
MCF7 NYnOZXlCU2mwYYPlJIF{e2G7 NWPGNnY4hjFyIN88US=> NFnDbGVFVVOR MYrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFQ{OCCwTR?= M4XlTVIxOzV2N{iw
TamR M4X1WGtqdmG|ZTDhd5NigQ>? NEfNRVh,OTBizszN MVfEUXNQ MkK1bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= M{jjSlIxOzV2N{iw
FasR MXvLbY5ie2ViYYPzZZk> M2L3dp4yOCEQvF2= NH6zUYxFVVOR MV\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFE{OCCwTR?= Mm\4NlA{PTR5OEC=
TamR M{fieGZ2dmO2aX;uJIF{e2G7 M1q4VVEh|ryP MUTEUXNQ MmDqbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NHPG[YEzODN3NEe4NC=>
FasR MXXGeY5kfGmxbjDhd5NigQ>? NGTtU2MyKM7:TR?= MnLCSG1UVw>? NX3XdIZIcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NG\2VlQzODN3NEe4NC=>
endothelial cell NHfmbWxMcW6jc3WgZZN{[Xl? MofVOFAhdk1? M3\6TGROW09? NGH5d4RqdmirYnn0d{BJOk9{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> MYiyNVIyOjRyMh?=
endothelial cell M4HCbmZ2dmO2aX;uJIF{e2G7 M1qze|QxKG6P MkfPSG1UVw>? NXP1c|V6cW6qaXLpeJMhUDKRMj3pcoR2[2WmIIP0doV{eyCoaXLldkBnd3KvYYTpc44> NHzuOWwzOTJzMkSwNi=>
endothelial cell NIfaeVRCeG:ydH;zbZMh[XO|YYm= NGfXTFc1OCCwTR?= NEntbmVFVVOR NHnMdXJqdmirYnn0d{BieG:ydH;zbZM> NIPWd5IzOTJzMkSwNi=>
GH3 NW[zWGJKTnWwY4Tpc44h[XO|YYm= NWjLdlA3OyEQvF2= NXXsSlRHTE2VTx?= Mmf2bY5kemWjc3XzJGlMMEOjKTDhcZBtcXS3ZHW= Mo\GNlE6OjV3MUK=
GH3 MkX0SpVv[3Srb36gZZN{[Xl? NWjYSGVuOyEQvF2= NEfseJZFVVOR NH;kWXZmdmijbnPld{BDU0OjLXPoZY5v\WxiYXP0bZZqfHl? NV;TfYRMOjF7MkW1NVI>
HUVEC NXP3SXhx[3m2b4TvfIlkcXS7IHHzd4F6 NVPFPWV5hjFyIN88US=> MUHEUXNQ M{jvW4lueGGrcoOg[Y5ld3SqZXzpZYwh[2WubDD2bYFjcWyrdIm= MV[yNlA4PTB3Nx?=
HUVEC MVLLbY5ie2ViYYPzZZk> NEXjcoY2KM7:TR?= MmOzSG1UVw>? MlewbY5pcWKrdIOgSmFMKGurbnHz[UBi[3Srdnn0fS=> Ml;xNlIxPzVyNUe=
HUVEC NHvwR|dHfW6ldHnvckBie3OjeR?= NFXxeo82KM7:TR?= NXHsVYdKTE2VTx?= M3;aOYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MmGxNlIxPzVyNUe=
HUVEC NG\VZ5FCeG:ydH;zbZMh[XO|YYm= NYfzOIpLPSEQvF2= MVzEUXNQ NGLNTWlqdmS3Y3XzJIFxd3C2b4Ppdy=> NYnjU3M6OjJyN{WwOVc>
HUVEC MnW1SpVv[3Srb36gZZN{[Xl? MVq1JO69VQ>? NEfV[HpFVVOR NWTV[5FEcW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= M2jyS|IzODd3MEW3
HUVEC NGLQZWxHfW6ldHnvckBie3OjeR?= M3W3NlUh|ryP Mm[zSG1UVw>? MmXiZoxw[2u|IFjVWmVEKHOycn;1eIlv\yCxbjDjc4xt[WenbjDJJIdmdHN? M3HKT|IzODd3MEW3
human peripheral blood T cells NW\DSZNSU2mwYYPlJIF{e2G7 MlnzglExKM7:TR?= M37EeGROW09? MV3pcohq[mm2czDzbZRmNXOyZXPp[olkKHCqb4PwbI9zgWyjdHnvckBw\iCIQVu= NIXvSJgzOzl{OEG4PC=>
human peripheral blood T cells MWTGeY5kfGmxbjDhd5NigQ>? NW\2[2FVhjFyIN88US=> NXLvUWFqTE2VTx?= MlfZbY1x[Wm{czDUR3IucW6mdXPl[EBVKGOnbHygcY9zeGixbH;nbYNidCClaHHu[4V{KGGwZDDhcJRmenNiYXP0bZZqfHlib3[gVohwSQ>? Mn7CNlM6OjhzOEi=
human peripheral blood T cells MV;GeY5kfGmxbjDhd5NigQ>? MXP+NVAh|ryP NILkW3hFVVOR MYTpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gXmFRNTdyIHHu[EBNSVR? NG\tVIozOzl{OEG4PC=>
human peripheral blood T cells M1P0ZWZ2dmO2aX;uJIF{e2G7 MmLtglExKM7:TR?= MmSySG1UVw>? NYnCR45pcW2yYXnyd{BCdnSrZ3XuMYRmeGWwZHXueEBVKGOnbHygZ49vcnWpYYTpc44> M3XSU|I{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 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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID