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
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USD 570 In stock
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Cited by 19 Publications

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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 MUHLbY5ie2ViYYPzZZk> NHnGWGR,OTBizszN MmrRSG1UVw>? NVr4SVVIcW6qaXLpeJMhTkGNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVEhdk1? Mn3iNVc{QTV3OUS=
REF52 NFvrWpdMcW6jc3WgZZN{[Xl? NGHrVlV,OTBizszN MX3EUXNQ NGT4boNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKH5zMECgcm0> MnvjNVc{QTV3OUS=
PC3 NVrub|g2U2mwYYPlJIF{e2G7 Ml\sglExKM7:TR?= M3T1bWROW09? M374SIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTByIH7N M1XxXFE4Ozl3NUm0
SKOV-3 MorHT4lv[XOnIHHzd4F6 MoHCglExKM7:TR?= NYPwZVVMTE2VTx?= MULpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFUxKG6P MnrVNVc{QTV3OUS=
L3.6p1 NYi3WXlOU2mwYYPlJIF{e2G7 NUH3R5BHhjFyIN88US=> NUPI[WkzTE2VTx?= NFiydItqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDNyMDDuUS=> NVTrOZRROTd|OUW1PVQ>
F-G M2XvcWtqdmG|ZTDhd5NigQ>? MYf+NVAh|ryP NEe2SYNFVVOR MoXIbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA{OCCwTR?= MkDvNVc{QTV3OUS=
MDCK NG\S[|BMcW6jc3WgZZN{[Xl? MUj+NVAh|ryP NIntWlhFVVOR NGTiUndqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyMDDuUS=> Mn7lNVc{QTV3OUS=
PC3 M1vadmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3nndVExKM7:TR?= NYTObVlKTE2VTx?= MonPd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= M1fSc|E4Ozl3NUm0
REF52 M3\lcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFn6PIEyOCEQvF2= NVzYVZFPTE2VTx?= M{jiZZNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEBoem:5dHiu NFLX[3cyPzN7NUW5OC=>
MDCK M3vYO2Fxd3C2b4Ppd{Bie3OjeR?= MXixNEDPxE1? Mnj3SG1UVw>? NFTpRW1qdmS3Y3XzJIFxd3C2b4Ppdy=> Mm[yNVc{QTV3OUS=
REF52 MUHBdI9xfG:|aYOgZZN{[Xl? M1TTWVExKM7:TR?= NH;OZ|RFVVOR M3HDfolv\HWlZYOgZZBweHSxc3nz NVuwbIh3OTd|OUW1PVQ>
REF52 MVfGeY5kfGmxbjDhd5NigQ>? MX[xNEDPxE1? NHjxOnlFVVOR MXTicI9kc3Nic3XyeY0h[W6mIF\OMZN1cW23bHH0[YQhdWmpcnH0bY9v M1LTOlE4Ozl3NUm0
platelet NF;V[IVHfW6ldHnvckBie3OjeR?= Mn2yNUDPxE1? NVO4ZWRNTE2VTx?= MnTxbY5pcWKrdIOgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIIPwdoVi\GmwZx?= M3nLVlE6PzF4OECz
platelet MoLxSpVv[3Srb36gZZN{[Xl? MoXoNUDPxE1? MUTEUXNQ M3K2Voxm[WS|IITvJIlvcGmkaYTpc44hd2ZiUFHLJIFv\CCDS2S= M3nWR|E6PzF4OECz
platelet Mk[5SpVv[3Srb36gZZN{[Xl? MknKNUDPxE1? NIDGTZRFVVOR NV;EO|A{[myxY3vzJINidGOrdX2gcY9jcWyrenH0bY9vKGGwZDDk[Y5{\SCpcnHueYxmKHOnY4LleIlwdg>? Ml7FNVk4OTZ6MEO=
4T1 NUS1[|Z3TnWwY4Tpc44h[XO|YYm= NYPlc|c2TE2VTx?= M{nn[YFjd2yrc3jld{B1cGViaX70[ZJi[3Srb36gZoV1f2WnbjFOtlMhcW62ZXfybY4h[W6mIGVOtnIuUUl? NIXObZMyQTd2MESzNy=>
MCF7 MV7LbY5ie2ViYYPzZZk> NGPoU4F,OTBizszN M4rHbGROW09? MlHRbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA1OzBibl2= MYSyNFM2PDd6MB?=
TamR MWjLbY5ie2ViYYPzZZk> MmjIglExKM7:TR?= MmDMSG1UVw>? Mn\LbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= NWfXPZcxOjB|NUS3PFA>
FasR Mn3zT4lv[XOnIHHzd4F6 MV;+NVAh|ryP MXPEUXNQ M1PUNYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTNyIH7N NW\YNWlUOjB|NUS3PFA>
TamR NXruPZNPTnWwY4Tpc44h[XO|YYm= NE\qcm4yKM7:TR?= MWjEUXNQ MnLrbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NH31bpUzODN3NEe4NC=>
FasR MVTGeY5kfGmxbjDhd5NigQ>? NHL1SpUyKM7:TR?= MmrxSG1UVw>? MYPpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MonWNlA{PTR5OEC=
endothelial cell MYDLbY5ie2ViYYPzZZk> NHPUR|A1OCCwTR?= NUTye3NrTE2VTx?= NULwOot1cW6qaXLpeJMhUDKRMj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDGRWs> NYTYNpF7OjF{MUK0NFI>
endothelial cell MV\GeY5kfGmxbjDhd5NigQ>? NEjlVpc1OCCwTR?= MlvtSG1UVw>? MXPpcohq[mm2czDINm8zNWmwZIXj[YQhe3S{ZYPzJIZq[mW{IH\vdo1ifGmxbh?= MXiyNVIyOjRyMh?=
endothelial cell NUPLWoduSXCxcITvd4l{KGG|c3H5 NFnrcoM1OCCwTR?= MmrJSG1UVw>? MV7pcohq[mm2czDhdI9xfG:|aYO= MY[yNVIyOjRyMh?=
GH3 M3jJRWZ2dmO2aX;uJIF{e2G7 MV[zJO69VQ>? NVr5OVZTTE2VTx?= MoW4bY5kemWjc3XzJGlMMEOjKTDhcZBtcXS3ZHW= MUOyNVkzPTVzMh?=
GH3 Mk\hSpVv[3Srb36gZZN{[Xl? NHnvfZA{KM7:TR?= NH3RVppFVVOR M1zEdIVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? NVLDU2ZxOjF7MkW1NVI>
HUVEC MVvjfZRwfG:6aXPpeJkh[XO|YYm= MYH+NVAh|ryP NIrDRYVFVVOR NWnCTXhJcW2yYXnyd{BmdmSxdHjlcIlidCClZXzsJJZq[WKrbHn0fS=> NEK0W4wzOjB5NUC1Oy=>
HUVEC MmGxT4lv[XOnIHHzd4F6 NFTrRlc2KM7:TR?= MWrEUXNQ NGrVSlZqdmirYnn0d{BHSUtia3nuZZNmKGGldHn2bZR6 NULsXZN5OjJyN{WwOVc>
HUVEC NXLBTYkyTnWwY4Tpc44h[XO|YYm= MYK1JO69VQ>? NEHYeJNFVVOR NIXSR2FqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4W1UFIzODd3MEW3
HUVEC M1;NcGFxd3C2b4Ppd{Bie3OjeR?= NH3oTYw2KM7:TR?= M3faVWROW09? NHm3OI9qdmS3Y3XzJIFxd3C2b4Ppdy=> NFjHTHYzOjB5NUC1Oy=>
HUVEC MnK0SpVv[3Srb36gZZN{[Xl? MUW1JO69VQ>? MmHCSG1UVw>? NWm0[lJTcW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= MUiyNlA4PTB3Nx?=
HUVEC MYTGeY5kfGmxbjDhd5NigQ>? MWm1JO69VQ>? MnP2SG1UVw>? MV\icI9kc3NiSGXWSWMhe3C{b4X0bY5oKG:wIHPvcIxi\2WwIFmg[4Vtew>? M4DCZVIzODd3MEW3
human peripheral blood T cells NVLjcXZwU2mwYYPlJIF{e2G7 NEe4U3p,OTBizszN Mlz0SG1UVw>? MlXsbY5pcWKrdIOgd4l1\S2|cHXjbYZq[yCyaH;zdIhwenmuYYTpc44hd2ZiRlHL NGW4VnozOzl{OEG4PC=>
human peripheral blood T cells NHTlO4RHfW6ldHnvckBie3OjeR?= MknPglExKM7:TR?= NVjlSYJWTE2VTx?= MW\pcZBicXK|IGTDVk1qdmS3Y3XkJHQh[2WubDDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZMh[W6mIHHseIVzeyCjY4Tpeol1gSCxZjDSbI9C MljsNlM6OjhzOEi=
human peripheral blood T cells MX3GeY5kfGmxbjDhd5NigQ>? MXf+NVAh|ryP MnHGSG1UVw>? MXvpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gXmFRNTdyIHHu[EBNSVR? M16zVVI{QTJ6MUi4
human peripheral blood T cells NGHWZmhHfW6ldHnvckBie3OjeR?= NHvGPWR,OTBizszN M3q1[mROW09? MVvpcZBicXK|IFHueIlo\W5vZHXw[Y5l\W62IGSgZ4VtdCClb37qeYdifGmxbh?= MUSyN|kzQDF6OB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1; 

PubMed: 30761269     


(D) On the third day, PF-573228-treated cells were harvested and subjected to Western blot analysis for cyclin B1. Cyclin B1 levels were much higher in A549 cells with 1 μM PF-573228 or without PF-573228 treatment than in the cells treated with higher concentrations of PF-573228. (E) After 10 μM PF-573228 treatment, cyclin B1 levels declined markedly in H460 cells. (F) PF-573228 administration slightly reduced cyclin B1 levels in H1299 cells. 

p-FAK / FAK ; 

PubMed: 30761269     


FAK expression levels and FAK activity, as measured by the phosphorylation of FAK at tyrosine 576 and 577, were quantified by Western blot analysis after treatment of lung cancer cells with PF-573228 for 3 days.

Lamin A / Lamin C; 

PubMed: 30761269     


(B) The cells treated with 10 μM PF-573228 exhibited a decrease in p-FAK levels. Lamin A and lamin C expression levels were much lower in A549 cells exposed to 10 μM PF-573228. 

30761269
Immunofluorescence
FAK / F-actin; 

PubMed: 30761269     


(B) The cells were stained with phalloidin to visualize F-actin (red) and a FAK antibody to visualize the FAK distribution (green). In cells without PF-573228 administration, FAK translocated to focal adhesions at the tips of actin stress fibers, and the focal adhesions were relatively large. When cells were exposed to 10 μM PF-573228, FAK translocation to focal adhesions was reduced, and the sizes of the focal adhesions were smaller. Nuclei in cells treated with PF-573228 were deformed, as visualized with DAPI staining, whereas most nuclei in cells without PF-573228 treatment were oval shaped. 

Emerin; 

PubMed: 30761269     


(A) After PF-573228 treatment of A549 cells, the cells were fixed and stained with phalloidin to label F-actin (red) and an antibody against emerin (green) to outline the nuclear shape. Cells treated with PF-573228 were extremely large and had deformed nuclei, whereas mostly oval-like nuclei were present in the cells without PF-573228 treatment. 

30761269
Growth inhibition assay
Cell viability; 

PubMed: 30761269     


Three different types of lung cancer cells, (A) A549 lung adenocarcinoma and (B) H460, and (C) H1299 large cell carcinoma, were selected for the PF-573228 administration regimen. Cell growth curves of the three lung cancer cell lines treated with various doses of PF-573228 for 4 days were established. The administration of PF-573228 at 10 μM to the lung cancer cells effectively suppressed cell growth in vitro, as proliferative activity totally ceased in the cells exposed to 10 μM PF-573228.

30761269
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

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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