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 NFK4b25McW6jc3WgZZN{[Xl? NV35d4pJhjFyIN88US=> M3nHZmROW09? NELCWGtqdmirYnn0d{BHSUticHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxNUBvVQ>? NV3YRYpCOTd|OUW1PVQ>
REF52 M{LDVWtqdmG|ZTDhd5NigQ>? MUT+NVAh|ryP NF7BN41FVVOR NX\5VJlrcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iC-MUCwJI5O MXWxO|M6PTV7NB?=
PC3 M1XTfmtqdmG|ZTDhd5NigQ>? NEnqco5,OTBizszN MmLJSG1UVw>? MmDMbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kAyODBibl2= Mlu2NVc{QTV3OUS=
SKOV-3 NXz4fYxWU2mwYYPlJIF{e2G7 NV;yVJk2hjFyIN88US=> MWDEUXNQ NFny[nNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N MXKxO|M6PTV7NB?=
L3.6p1 NILVR2lMcW6jc3WgZZN{[Xl? MluzglExKM7:TR?= M{HuTWROW09? MljUbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{ODBibl2= NUnJSlJXOTd|OUW1PVQ>
F-G MkLRT4lv[XOnIHHzd4F6 NFHHNGd,OTBizszN NGDFW5pFVVOR Ml36bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{OCCwTR?= NXX1bHJxOTd|OUW1PVQ>
MDCK MnrzT4lv[XOnIHHzd4F6 M1yxWp4yOCEQvF2= NF\EN41FVVOR NImzOYJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=> NGLpV2UyPzN7NUW5OC=>
PC3 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1TOT|ExKM7:TR?= M4LlOGROW09? M17xeJNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NVHTdop5OTd|OUW1PVQ>
REF52 NEnCOlNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWHTSolZOTBizszN NYjmeW9OTE2VTx?= NFflU3p{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M2OzZ|E4Ozl3NUm0
MDCK NEHofoNCeG:ydH;zbZMh[XO|YYm= M175NVExKM7:TR?= NGK0UWdFVVOR NFXmW|BqdmS3Y3XzJIFxd3C2b4Ppdy=> NU[weZpMOTd|OUW1PVQ>
REF52 M2PPcGFxd3C2b4Ppd{Bie3OjeR?= NIHQfHQyOCEQvF2= M{fp[2ROW09? M33PUIlv\HWlZYOgZZBweHSxc3nz MoXVNVc{QTV3OUS=
REF52 MnvwSpVv[3Srb36gZZN{[Xl? NEH5VYwyOCEQvF2= NEPhNHRFVVOR MlvJZoxw[2u|IIPldpVuKGGwZDDGUk1{fGmvdXzheIVlKG2rZ4LheIlwdg>? MoflNVc{QTV3OUS=
platelet Mnv6SpVv[3Srb36gZZN{[Xl? M2GzSVEh|ryP MoXISG1UVw>? M1P3XolvcGmkaYTzJJBt[XSnbHX0JIFo\3KnZ3H0bY9vKGGwZDDzdJJm[WSrbne= NYDhbJhCOTl5MU[4NFM>
platelet NULjZYk3TnWwY4Tpc44h[XO|YYm= MYmxJO69VQ>? M2m3cGROW09? MV7s[YFleyC2bzDpcohq[mm2aX;uJI9nKFCDSzDhcoQhSUuW NI\CTFEyQTdzNkiwNy=>
platelet M4C1SGZ2dmO2aX;uJIF{e2G7 MkLmNUDPxE1? M3L5NmROW09? NFLZc3VjdG:la4OgZ4Ft[2m3bTDtc4JqdGm8YYTpc44h[W6mIHTlcpNmKGe{YX71cIUhe2WlcnX0bY9v NEPY[oQyQTdzNkiwNy=>
4T1 NG\BNY1HfW6ldHnvckBie3OjeR?= NUfiUmVtTE2VTx?= MmLGZYJwdGm|aHXzJJRp\SCrboTldoFkfGmxbjDi[ZR4\WWwIN8yN{BqdnSnZ4LpckBidmRiVN8yVk1KUQ>? NFj1bHQyQTd2MESzNy=>
MCF7 M1LFSGtqdmG|ZTDhd5NigQ>? MnLMglExKM7:TR?= NGXa[GZFVVOR MWnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFQ{OCCwTR?= NVX6VHJEOjB|NUS3PFA>
TamR NHTIdFhMcW6jc3WgZZN{[Xl? M37rc54yOCEQvF2= NYjDZZFiTE2VTx?= M3rJRolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTBibl2= M3jFRlIxOzV2N{iw
FasR NV;lbWNUU2mwYYPlJIF{e2G7 MW\+NVAh|ryP NWrIb3VNTE2VTx?= M3TrbolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N NYmyXlBTOjB|NUS3PFA>
TamR NFr5T3RHfW6ldHnvckBie3OjeR?= MXKxJO69VQ>? NGrvNGhFVVOR NECydmNqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MVmyNFM2PDd6MB?=
FasR MkToSpVv[3Srb36gZZN{[Xl? NWDrXJMyOSEQvF2= MnrFSG1UVw>? NFK0THVqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MWiyNFM2PDd6MB?=
endothelial cell Ml[zT4lv[XOnIHHzd4F6 NY\yU29jPDBibl2= M{LRdGROW09? MWXpcohq[mm2czDINm8zNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKE[DSx?= NIrDU5YzOTJzMkSwNi=>
endothelial cell NHvhS|FHfW6ldHnvckBie3OjeR?= NYPxN2JUPDBibl2= M4HCNmROW09? NELMNGZqdmirYnn0d{BJOk9{LXnu[JVk\WRic4Ty[ZN{KG[rYnXyJIZwem2jdHnvci=> NV:5ZlBOOjF{MUK0NFI>
endothelial cell MV7BdI9xfG:|aYOgZZN{[Xl? NYXpb49GPDBibl2= Mn7SSG1UVw>? MoLubY5pcWKrdIOgZZBweHSxc3nz MkXFNlEzOTJ2MEK=
GH3 NH\6VIxHfW6ldHnvckBie3OjeR?= M{[0RlMh|ryP M{fOWGROW09? MWHpcoNz\WG|ZYOgTWspS2FrIHHtdIxqfHWmZR?= NHnpdIIzOTl{NUWxNi=>
GH3 NHzXW4hHfW6ldHnvckBie3OjeR?= M4XqbVMh|ryP MkPKSG1UVw>? M2\xfIVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? MmXhNlE6OjV3MUK=
HUVEC MnGzZ5l1d3SxeHnjbZR6KGG|c3H5 M3TPNZ4yOCEQvF2= MnmxSG1UVw>? M3nRUYlueGGrcoOg[Y5ld3SqZXzpZYwh[2WubDD2bYFjcWyrdIm= M1n6bVIzODd3MEW3
HUVEC NGr4eXJMcW6jc3WgZZN{[Xl? MkDqOUDPxE1? NVHYfGxrTE2VTx?= NW\FVZc1cW6qaXLpeJMhTkGNIHvpcoF{\SCjY4Tpeol1gQ>? NGPvTI4zOjB5NUC1Oy=>
HUVEC NHS1[JlHfW6ldHnvckBie3OjeR?= M1fhdFUh|ryP Mli5SG1UVw>? NFewU4dqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MW[yNlA4PTB3Nx?=
HUVEC NV\1UGFMSXCxcITvd4l{KGG|c3H5 MkDZOUDPxE1? NF;mU3pFVVOR M2e2cIlv\HWlZYOgZZBweHSxc3nz NWnxNYJTOjJyN{WwOVc>
HUVEC NVvnXYZ3TnWwY4Tpc44h[XO|YYm= M4OwZ|Uh|ryP NEjWVHVFVVOR MknNbY1x\WSnczDlcoRwfGinbHnhcEBk\WyuIH3p[5JifGmxbjDhcoQh[Wy2ZYLzJJRp\SClZXzseYxieiCjY4TpckBkgXSxc3vlcIV1d25? M2DlTlIzODd3MEW3
HUVEC MmrOSpVv[3Srb36gZZN{[Xl? M2DSNlUh|ryP MmTZSG1UVw>? M{TwOIJtd2OtczDIWXZGSyC|cILveZRqdmdib36gZ49tdGGpZX6gTUBo\Wy| M1;6OVIzODd3MEW3
human peripheral blood T cells Ml\OT4lv[XOnIHHzd4F6 MYL+NVAh|ryP MXfEUXNQ M{S5bolvcGmkaYTzJJNqfGVvc4DlZ4lncWNicHjvd5Bpd3K7bHH0bY9vKG:oIF\BTy=> M1iyRlI{QTJ6MUi4
human peripheral blood T cells MkT5SpVv[3Srb36gZZN{[Xl? NXW4R3FvhjFyIN88US=> NEDNXXBFVVOR NX7mXpdvcW2yYXnyd{BVS1JvaX7keYNm\CCWIHPlcIwhdW:{cHjvcI9ocWOjbDDjbIFv\2W|IHHu[EBidHSncoOgZYN1cX[rdImgc4YhWmixQR?= MnzoNlM6OjhzOEi=
human peripheral blood T cells MXrGeY5kfGmxbjDhd5NigQ>? MVT+NVAh|ryP MVrEUXNQ M{\mNYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBbSVBvN{CgZY5lKEyDVB?= MVuyN|kzQDF6OB?=
human peripheral blood T cells MnO2SpVv[3Srb36gZZN{[Xl? MVL+NVAh|ryP NWHtOIx1TE2VTx?= Mk\WbY1x[Wm{czDBcpRq\2WwLXTldIVv\GWwdDDUJINmdGxiY3;ubpVo[XSrb36= NVHDRY9IOjN7MkixPFg>

... 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:
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
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