PF-00562271 Besylate

Catalog No.S2672 Synonyms: PF-562271 Besylate

For research use only.

PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.

PF-00562271 Besylate Chemical Structure

CAS No. 939791-38-5

Selleck's PF-00562271 Besylate has been cited by 23 publications

Purity & Quality Control

Choose Selective FAK Inhibitors

Other FAK Products

Biological Activity

Description PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
FAK [1]
(Cell-free assay)
PYK2 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK3/CyclinE [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
Click to View More Targets
1.5 nM 13 nM 30 nM 47 nM 58 nM
In vitro

PF-562271 Besylate shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. [1] In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 cell M4G1[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfoZ5ZkUW6qaXLpeIlwdiCxZjDoeY1idiCPVj20MVEyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{N{[2JO69VQ>? M{LpU3NCVkeHUh?=
human SW982 cell NGjEfmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLjTY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|I5OiEQvF2= MUPTRW5ITVJ?
human KM12 cell NGK3XWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mk\lTY5pcWKrdHnvckBw\iCqdX3hckBMVTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPFU2PyEQvF2= NXXF[IdCW0GQR1XS
human COLO-205 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vMkC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QDZ3ODFOwG0> NES5XYFUSU6JRWK=
human COLO-829 cell NGjZdY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3zmSGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd4MUe2JO69VQ>? M3jT[3NCVkeHUh?=
human MG-63 cell Mlr6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1v3N2lvcGmkaYTpc44hd2ZiaIXtZY4hVUdvNkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgxPjN5IN88US=> MUTTRW5ITVJ?
human IGROV-1 cell NHv5eo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PhNWlvcGmkaYTpc44hd2ZiaIXtZY4hUUeUT2[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDFyM{ig{txO M3;BPXNCVkeHUh?=
human NCI-H650 cell MkD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTRTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDNzNUSg{txO NV\XWWFoW0GQR1XS
human RT-112 cell M4fpV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3zkVmlvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46QDR4IN88US=> NYfDRm5kW0GQR1XS
human BCPAP cell MmPqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFfENGtKdmirYnn0bY9vKG:oIHj1cYFvKEKFUFHQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xOTJ6ODFOwG0> NUPYS2luW0GQR1XS
ALL-PO cell NILpWpFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFE2QDRizszN NVrte|Q6W0GQR1XS
human KYSE-270 cell MmTuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnzNTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUK3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODR5MUSg{txO MWjTRW5ITVJ?
human 8305C cell M3TjeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGPKPJZKdmirYnn0bY9vKG:oIHj1cYFvKDh|MEXDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xQTlyNDFOwG0> NIPuWmNUSU6JRWK=
NCI-H810 cell NVrUfJRTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoTtTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOTB5N{[g{txO NVnQUpRMW0GQR1XS
human CAL-33 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{OydmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4yOjl|ODFOwG0> M3nHbnNCVkeHUh?=
human AN3-CA cell NVX4[mlnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYn3WVI4UW6qaXLpeIlwdiCxZjDoeY1idiCDTkOtR2Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJzOE[3JO69VQ>? NGnwN3pUSU6JRWK=
human NKM-1 cell M13FZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6yO|UxPiEQvF2= NHv5S5NUSU6JRWK=
human BPH-1 cell NGXpOWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4jkNmlvcGmkaYTpc44hd2ZiaIXtZY4hSlCKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI5PzZ4IN88US=> M4X1eHNCVkeHUh?=
human MES-SA cell M3rFdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKGi3bXHuJG1GWy2VQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|A3QDJizszN MYjTRW5ITVJ?
human CAL-62 cell NYroV|k1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|E6ODlizszN NVTQ[lR7W0GQR1XS
human KYSE-150 cell NVzXWnR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\NNWVKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNVUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|NUKzOkDPxE1? MY\TRW5ITVJ?
human SK-UT-1 cell NF\xbnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFz5ZllKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR2NkS3JO69VQ>? MmPtV2FPT0WU
human HUTU-80 cell NFjBW4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnCd5NYUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52NEi4OkDPxE1? M2rOZnNCVkeHUh?=
human SIG-M5 cell NWPmZWYzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWW2PJlqUW6qaXLpeIlwdiCxZjDoeY1idiCVSVetUVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR6NEi3JO69VQ>? MW\TRW5ITVJ?
human AGS cell NU\hXZZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoHCTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkWyNVI1KM7:TR?= M37aXXNCVkeHUh?=
human ST486 cell Mmq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzTZ|BKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42OzJ5ODFOwG0> M3\6fnNCVkeHUh?=
human HSC-2 cell NYWxbZFVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61N|k2KM7:TR?= MVrTRW5ITVJ?
human BC-1 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4\o[GlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlE3PjRizszN NVn2UpBiW0GQR1XS
human CGTH-W-1 cell MmfkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVPJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43OTZ5OTFOwG0> M1i5UXNCVkeHUh?=
human MZ1-PC cell M2LWZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvSfI9KdmirYnn0bY9vKG:oIHj1cYFvKE2cMT3QR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjJ|MUKg{txO Mn\2V2FPT0WU
human SW1710 cell M2LoXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlI3OjhizszN Mnj3V2FPT0WU
human EW-13 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVLvfoFmUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjN2Nk[g{txO MonTV2FPT0WU
human U251 cell M3H0Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXLJcohq[mm2aX;uJI9nKGi3bXHuJHUzPTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke0NFMyKM7:TR?= MnK5V2FPT0WU
human NCI-H460 cell NIX6VW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofuTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSES2NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvODR6M{mg{txO NEnhc5pUSU6JRWK=
human DU-4475 cell MlzkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEX1XW1KdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjF2N{W5JO69VQ>? NVnZOlUyW0GQR1XS
human MFE-296 cell M4Oybmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKGi3bXHuJG1HTS1{OU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlQ4Pzl{IN88US=> MYnTRW5ITVJ?
human DU-145 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fLVGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvMUS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QTFzODFOwG0> MVzTRW5ITVJ?
human MDA-MB-231 cell NFO5UYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWj4V5E4UW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOjNzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj60PVU4OiEQvF2= Mn3FV2FPT0WU
human SNU-387 cell NYK4TFRuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS1|OEegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlUzQDJizszN NXrGfnAyW0GQR1XS
In vivo In several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. [1] PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. [3] In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy. [4]

Protocol (from reference)

Kinase Assay:


  • Recombinant kinase assay and enzyme kinetics :

    Briefly, purified-activated FAK kinase domain (amino acid 410–689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 minutes. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted PF-562271 at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 M H2SO4). IC50 values are determined using the Hill-Slope Model. Broad kinase selectivity profiling is performed in house and by using the KinaseProfiler Selectivity Screening Service available through UpState Biotechnology.

Cell Research:


  • Cell lines: Squamous cell carcinoma (SCC)
  • Concentrations: 0 to 1 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.

Animal Research:


  • Animal Models: PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice .
  • Dosages: ≤100 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.


Chemical Information

Molecular Weight 665.66


CAS No. 939791-38-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.C1=CC=C(C=C1)S(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00666926 Completed Drug: PF00562271 Head and Neck Neoplasm|Prostatic Neoplasm|Pancreatic Neoplasm Verastem Inc. December 2005 Phase 1

(data from, updated on 2022-08-01)

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
We are planning both in vitro and in vivo experiments and want to know how to reconstitute the drug for these purposes?

PF-00562271 has poor solubility in DMSO and water. Its solubility in DMSO is only 0.4mg/ml. In a previous literature report (, the author used 5% Gelucire to formulate the compound. You can also consider other co-solvents such as PEG400, CMC, Tween80, and Captisol.

Question 2:
Can you provide with a few common vehicles for PF-00562271, S2672 for use as oral gavage?

S2672 PF-00562271 can be dissolved in 0.5% CMC Na at 30 mg/ml as a suspension. If 4% DMSO can be used in your experiment, it will help dissolving the suspension more homogeneously.

Tags: buy PF-00562271 Besylate | PF-00562271 Besylate supplier | purchase PF-00562271 Besylate | PF-00562271 Besylate cost | PF-00562271 Besylate manufacturer | order PF-00562271 Besylate | PF-00562271 Besylate distributor