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 MWfLbY5ie2ViYYPzZZk> NULSW2hJhjFyIN88US=> MljNSG1UVw>? NHPqfm5qdmirYnn0d{BHSUticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNUBvVQ>? NFnl[4cyPzN7NUW5OC=>
REF52 NGnqcJlMcW6jc3WgZZN{[Xl? NFfxTll,OTBizszN Mo\qSG1UVw>? MoPnbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kB,OTByIH7N M2nmd|E4Ozl3NUm0
PC3 NFzIPFRMcW6jc3WgZZN{[Xl? MUj+NVAh|ryP M2HXcWROW09? MoXKbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kAyODBibl2= NXLFco8{OTd|OUW1PVQ>
SKOV-3 NWLKZYR{U2mwYYPlJIF{e2G7 MkftglExKM7:TR?= NUL1VGJGTE2VTx?= MkHxbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= M3\0cFE4Ozl3NUm0
L3.6p1 MYLLbY5ie2ViYYPzZZk> MVf+NVAh|ryP M2G2dGROW09? NHPCNoZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDNyMDDuUS=> M4SwZVE4Ozl3NUm0
F-G MYfLbY5ie2ViYYPzZZk> NHPKeWF,OTBizszN NELTcGJFVVOR M1jNcYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOzBibl2= NYCyXJhxOTd|OUW1PVQ>
MDCK NIfT[YlMcW6jc3WgZZN{[Xl? NWTHc|BxhjFyIN88US=> Ml7lSG1UVw>? MYfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxOCCwTR?= MWWxO|M6PTV7NB?=
PC3 M4HhcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF71d|YyOCEQvF2= MnjHSG1UVw>? NV7VdIsxe2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKGe{b4f0bE4> NVT4OYVtOTd|OUW1PVQ>
REF52 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGX6TVMyOCEQvF2= M{TydGROW09? MXzzbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHyg[5Jwf3SqLh?= NVvRcno1OTd|OUW1PVQ>
MDCK M172TGFxd3C2b4Ppd{Bie3OjeR?= NEfxXWsyOCEQvF2= M4e0[GROW09? MnLlbY5lfWOnczDhdI9xfG:|aYO= M1TsZVE4Ozl3NUm0
REF52 MmLORZBweHSxc3nzJIF{e2G7 M3P4UVExKM7:TR?= NYfrc4VLTE2VTx?= NXn4fFdncW6mdXPld{BieG:ydH;zbZM> M1\qbFE4Ozl3NUm0
REF52 MVvGeY5kfGmxbjDhd5NigQ>? NXnBRYYxOTBizszN NGf5TGlFVVOR MXficI9kc3Nic3XyeY0h[W6mIF\OMZN1cW23bHH0[YQhdWmpcnH0bY9v NY\Jc41QOTd|OUW1PVQ>
platelet MlvqSpVv[3Srb36gZZN{[Xl? NFPKWFYyKM7:TR?= MlnBSG1UVw>? NWHNNpI3cW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> NX\3do5[OTl5MU[4NFM>
platelet NXz4ZnZsTnWwY4Tpc44h[XO|YYm= MV:xJO69VQ>? MV;EUXNQ NF7NS4Ft\WGmczD0c{BqdmirYnn0bY9vKG:oIGDBT{BidmRiQVvU MVOxPVcyPjhyMx?=
platelet NGG0PJdHfW6ldHnvckBie3OjeR?= M3vOO|Eh|ryP MoL2SG1UVw>? MVHicI9kc3NiY3HsZ4l2dSCvb3LpcIl7[XSrb36gZY5lKGSnboPlJIdz[W63bHWgd4VkemW2aX;u MknyNVk4OTZ6MEO=
4T1 NH;LZ5BHfW6ldHnvckBie3OjeR?= MXfEUXNQ M1e5OYFjd2yrc3jld{B1cGViaX70[ZJi[3Srb36gZoV1f2WnbjFOtlMhcW62ZXfybY4h[W6mIGVOtnIuUUl? NW\5XndzOTl5NEC0N|M>
MCF7 MkTqT4lv[XOnIHHzd4F6 M2DkUJ4yOCEQvF2= NUTiUYJwTE2VTx?= MXHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFQ{OCCwTR?= NESyZlAzODN3NEe4NC=>
TamR MkjGT4lv[XOnIHHzd4F6 MWr+NVAh|ryP NVnUWo9LTE2VTx?= MkXSbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MX:yNFM2PDd6MB?=
FasR M{HSU2tqdmG|ZTDhd5NigQ>? MXv+NVAh|ryP MUHEUXNQ M3y4folvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N MorrNlA{PTR5OEC=
TamR NHKxXoFHfW6ldHnvckBie3OjeR?= MXOxJO69VQ>? MUfEUXNQ MWjpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? M1n6UVIxOzV2N{iw
FasR NHK5cVhHfW6ldHnvckBie3OjeR?= NGr5emIyKM7:TR?= M4nDUmROW09? NFnocIxqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= NGr1[WYzODN3NEe4NC=>
endothelial cell M{PwNmtqdmG|ZTDhd5NigQ>? NUWxNlFxPDBibl2= MX\EUXNQ NWDHXpJScW6qaXLpeJMhUDKRMj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> M1HrblIyOjF{NECy
endothelial cell MUDGeY5kfGmxbjDhd5NigQ>? M1vYWVQxKG6P NHvReGdFVVOR Mm[zbY5pcWKrdIOgTFJQOi2rbnT1Z4VlKHO2cnXzd{BncWKncjDmc5Ju[XSrb36= NFvx[pczOTJzMkSwNi=>
endothelial cell NYjuNlZMSXCxcITvd4l{KGG|c3H5 MYW0NEBvVQ>? NWXLOWJJTE2VTx?= M4PO[olvcGmkaYTzJIFxd3C2b4Ppdy=> MkXzNlEzOTJ2MEK=
GH3 NUG5bJUyTnWwY4Tpc44h[XO|YYm= M3KyN|Mh|ryP M2fscWROW09? NVzvbWU4cW6lcnXhd4V{KEmNKFPhLUBidXCuaYT1[IU> M1KzXFIyQTJ3NUGy
GH3 MlXiSpVv[3Srb36gZZN{[Xl? Ml\lN{DPxE1? NHzNdlVFVVOR M4e3[IVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? NW\obmlGOjF7MkW1NVI>
HUVEC NHPqdmFkgXSxdH;4bYNqfHliYYPzZZk> MUD+NVAh|ryP M17EdmROW09? NFzo[GJqdXCjaYLzJIVv\G:2aHXsbYFtKGOnbHygeoli[mmuaYT5 M1fDWlIzODd3MEW3
HUVEC MWrLbY5ie2ViYYPzZZk> MWG1JO69VQ>? Mn3KSG1UVw>? NYTuVGM2cW6qaXLpeJMhTkGNIHvpcoF{\SCjY4Tpeol1gQ>? M1Lt[FIzODd3MEW3
HUVEC MVHGeY5kfGmxbjDhd5NigQ>? NYfoPVJNPSEQvF2= NIT1UFhFVVOR MmrRbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mlv3NlIxPzVyNUe=
HUVEC NVvuRY9KSXCxcITvd4l{KGG|c3H5 MYK1JO69VQ>? MYjEUXNQ NGTLeZRqdmS3Y3XzJIFxd3C2b4Ppdy=> NUjDeYlTOjJyN{WwOVc>
HUVEC MVXGeY5kfGmxbjDhd5NigQ>? NWHOdZF3PSEQvF2= MnXhSG1UVw>? MVzpcZBm\GW|IHXu[I91cGWuaXHsJINmdGxibXnndoF1cW:wIHHu[EBidHSncoOgeIhmKGOnbHz1cIFzKGGldHnuJIN6fG:|a3Xs[ZRwdg>? M1\E[|IzODd3MEW3
HUVEC M3f1UmZ2dmO2aX;uJIF{e2G7 NXfuNZJnPSEQvF2= MXvEUXNQ NH3yN4NjdG:la4OgTHVXTUNic4Dyc5V1cW6pIH;uJINwdGyjZ3XuJGkh\2Wucx?= NH3vVnQzOjB5NUC1Oy=>
human peripheral blood T cells M4PlVWtqdmG|ZTDhd5NigQ>? NFvNc3R,OTBizszN NEnvOlVFVVOR NIHDdGpqdmirYnn0d{B{cXSnLYPw[YNq\mmlIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> Ml;jNlM6OjhzOEi=
human peripheral blood T cells NYnFTINWTnWwY4Tpc44h[XO|YYm= MlTLglExKM7:TR?= NWDadIJtTE2VTx?= MnLIbY1x[Wm{czDUR3IucW6mdXPl[EBVKGOnbHygcY9zeGixbH;nbYNidCClaHHu[4V{KGGwZDDhcJRmenNiYXP0bZZqfHlib3[gVohwSQ>? Ml;UNlM6OjhzOEi=
human peripheral blood T cells MkXqSpVv[3Srb36gZZN{[Xl? MkHCglExKM7:TR?= MWjEUXNQ NU\IfI52cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFqDUD23NEBidmRiTFHU M3PRflI{QTJ6MUi4
human peripheral blood T cells MnPOSpVv[3Srb36gZZN{[Xl? MkfPglExKM7:TR?= Ml7aSG1UVw>? MW\pcZBicXK|IFHueIlo\W5vZHXw[Y5l\W62IGSgZ4VtdCClb37qeYdifGmxbh?= MnPHNlM6OjhzOEi=

... 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 to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+2% Tween 80+30% PEG 300+ddH2O
For best results, use promptly after mixing.
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
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.

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