Catalog Number: 3239
Chemical Name: 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
Biological Activity
Potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM). Displays 50 - 250-fold selectivity for FAK over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro.
Technical Data
  • M.Wt:
    491.49
  • Formula:
    C22H20F3N5O3S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    869288-64-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. FAK-heterozygous mice display enhanced tumour angiogenesis.
    Kostourou et al.
    Nat.Commun., 2013;5:2020
  2. Cellular characterization of a novel focal adhesion kinase inhibitor.
    Slack-Davis et al.
    J.Biol.Chem., 2007;282:14845
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PF 573228 include:

31 Citations: Showing 1 - 10
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  1. Disruption of outer blood-retinal barrier by Toxoplasma gondii-infected monocytes is mediated by paracrinely activated FAK signaling
    Authors: Song
    PLoS One 2017;12(4):e0175159
  2. Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices.
    Authors: Nasrollahi and Pathak
    PLoS One 2016;6:18831
  3. LEFTY2 Controls Migration of Human Endometrial Cancer Cells via Focal Adhesion Kinase Activity (FAK) and miRNA-200a
    Authors: Alowayed Et al.
    Cell Physiol Biochem 2016;39:815
  4. Eosinophil peroxidase activates cells by HER2 receptor engagement and β1-integrin clustering with downstream MAPK cell signaling
    Authors: Hennigan Et al.
    Clinical Immunology 2016;171:1
  5. Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
    Authors: Rengarajan Et al.
    Sci Rep 2016;12:e1005603
  6. Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα.
    Authors: Carrim Et al.
    J Exp Med 2015;6:640
  7. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Redox Biol 2015;5:10468
  8. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
    Elife 2015;4:e04069
  9. Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells.
    Authors: Webber Et al.
    Oncoscience 2015;2:765
  10. IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
    Authors: Cheng Et al.
    Sci Rep 2015;212:513
  11. Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
    Authors: Shih Et al.
    J Biol Chem 2014;34:2438
  12. The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis.
    Authors: Flannagan Et al.
    Mol Biol Cell 2014;25:1511
  13. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86.
    Authors: Alao Et al.
    BMC Cancer 2014;14:853
  14. Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins.
    Authors: Wrighton Et al.
    PLoS Pathog 2014;111:18126
  15. Periostin links mechanical strain to inflammation in abdominal aortic aneurysm.
    Authors: Yamashita Et al.
    J Neurosci 2013;8:e79753
  16. Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
    Authors: Wiel Et al.
    Cell Death Dis 2013;4:e855
  17. Reversal of myofibroblast differentiation by prostaglandin E(2).
    Authors: Garrison Et al.
    Mol Cancer Ther 2013;48:550
  18. Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways.
    Authors: Quint Et al.
    PLoS One 2013;288:5398
  19. Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor.
    Authors: Chapman Et al.
    J Immunol 2013;191:6208
  20. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal 2013;11:35
  21. Contractile Activity Regulates Inducible Nitric Oxide Synthase Expression and NO(i) Production in Cardiomyocytes via a FAK-Dependent Signaling Pathway.
    Authors: Chu Et al.
    J Signal Transduct 2012;2012:473410
  22. Focal adhesion kinase links mechanical force to skin fibrosis via inflammatory signaling.
    Authors: Wong Et al.
    Am J Respir Cell Mol Biol 2012;18:148
  23. Integrin/Fak/Src-mediated regulation of cell survival and anoikis in human intestinal epithelial crypt cells: selective engagement and roles of PI3-K isoform complexes.
    Authors: Beauséjour Et al.
    Apoptosis 2012;17:566
  24. Cooperation between c-Met and focal adhesion kinase family members in medulloblastoma and implications for therapy.
    Authors: Guessous Et al.
    Mol Cancer 2012;11:288
  25. Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
    Authors: Canonici Et al.
    Hepatology 2011;6:e18427
  26. Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells.
    Authors: Schrader Et al.
    Biochem Biophys Res Commun 2011;53:1192
  27. A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis.
    Authors: Daley Et al.
    Dev Dyn 2011;240:2069
  28. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci 2010;30:749
  29. DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway.
    Authors: Ocak Et al.
    Oncogene 2010;29:6331
  30. tPA is a potent mitogen for renal interstitial fibroblasts: role of beta1 integrin/focal adhesion kinase signaling.
    Authors: Hao Et al.
    Am J Pathol 2010;177:1164
  31. Characterization of a novel focal adhesion kinase inhibitor in human platelets.
    Authors: Jones Et al.
    Nat Med 2009;389:198
Expand to show all 31 Citations

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