PF 573228

  ( 39 citations ) ( 1 Review )    
Product Datasheet
Catalog Number:3239
Chemical Name:3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
Product Details
Citations (39)
Reviews
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.
Product Datasheets
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Citations:

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

39 Citations: Showing 1 - 10
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  1. Multiparametric Analysis of Cell Shape Demonstrates that β-PIX Directly Couples YAP Activation to Extracellular Matrix Adhesion.
    Authors: Sero and Bakal
    Cell Syst  2017;4:84
  2. 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
  3. Imatinib and Nilotinib increase glioblastoma cell invasion via Abl-independent stimulation of p130Cas and FAK signalling.
    Authors: Frolov Et al.
    Sci Rep  2016;6:27378
  4. Extracellular matrix stiffness dictates Wnt expression through integrin pathway.
    Authors: Du Et al.
    Sci Rep  2016;6:20395
  5. Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices.
    Authors: Nasrollahi and Pathak
    PLoS One  2016;6:18831
  6. Focal adhesion kinase is required for actin polymerization and remodeling of the cytoskeleton during sperm capacitation.
    Authors: Roa-Espitia Et al.
    Biol Open  2016;5:1189
  7. 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
  8. 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
  9. Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
    Authors: Rengarajan Et al.
    Sci Rep  2016;12:e1005603
  10. 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
  11. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Redox Biol  2015;5:10468
  12. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
    Elife  2015;4:e04069
  13. 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
  14. IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
    Authors: Cheng Et al.
    Sci Rep  2015;212:513
  15. WISP-2 in human gastric cancer and its potential metastatic suppressor role in gastric cancer cells mediated by JNK and PLC-γ pathways.
    Authors: Ji Et al.
    Br J Cancer  2015;113:921
  16. Segmentation of Image Data from Complex Organotypic 3D Models of Cancer Tissues with Markov Random Fields.
    Authors: Robinson Et al.
    PLoS One  2015;10:e0143798
  17. Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
    Authors: Shih Et al.
    J Biol Chem  2014;34:2438
  18. The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis.
    Authors: Flannagan Et al.
    Mol Biol Cell  2014;25:1511
  19. Essential function for PDLIM2 in cell polarization in three-dimensional cultures by feedback regulation of the β1-integrin-RhoA signaling axis.
    Authors: Deevi Et al.
    Neoplasia  2014;16:422
  20. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86.
    Authors: Alao Et al.
    BMC Cancer  2014;14:853
  21. Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins.
    Authors: Wrighton Et al.
    PLoS Pathog  2014;111:18126
  22. Periostin links mechanical strain to inflammation in abdominal aortic aneurysm.
    Authors: Yamashita Et al.
    J Neurosci  2013;8:e79753
  23. Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
    Authors: Wiel Et al.
    Cell Death Dis  2013;4:e855
  24. Reversal of myofibroblast differentiation by prostaglandin E(2).
    Authors: Garrison Et al.
    Mol Cancer Ther  2013;48:550
  25. 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
  26. Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor.
    Authors: Chapman Et al.
    J Immunol  2013;191:6208
  27. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal  2013;11:35
  28. 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
  29. 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
  30. 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
  31. 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
  32. Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
    Authors: Canonici Et al.
    Hepatology  2011;6:e18427
  33. Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells.
    Authors: Schrader Et al.
    Biochem Biophys Res Commun  2011;53:1192
  34. A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis.
    Authors: Daley Et al.
    Dev Dyn  2011;240:2069
  35. β1 integrin mediates an alternative survival pathway in breast cancer cells resistant to lapatinib.
    Authors: Huang Et al.
    Breast Cancer Res  2011;13:R84
  36. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci  2010;30:749
  37. DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway.
    Authors: Ocak Et al.
    Oncogene  2010;29:6331
  38. 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
  39. Characterization of a novel focal adhesion kinase inhibitor in human platelets.
    Authors: Jones Et al.
    Nat Med  2009;389:198
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Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

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