Home / Focal Adhesion Kinase Inhibitors / PF 573228

PF 573228

Catalog #: 3239
48 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3239/10
3239/50
PF 573228 | CAS No. 869288-64-2 | Focal Adhesion Kinase Inhibitors
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Description: Potent and selective FAK inhibitor

Chemical Name: 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone

Purity: ≥98%

Product Details
Citations (48)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PF 573228 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins.
    Wrighton, Paul J, Klim, Joseph R, Hernandez, Brandon, Koonce, Chad H, Kamp, Timothy, Kiessling, Laura L
    Proc Natl Acad Sci U S A, 2014;111(51):18126-31.
  2. Hic-5 promotes invadopodia formation and invasion during TGF-beta-induced epithelial-mesenchymal transition.
    Pignatelli J, Tumbarello DA, Schmidt RP, Turner CE
    J. Cell Biol., 2012;197(3):421-37.
  3. Focal adhesion kinase and Wnt signaling regulate human ductal carcinoma in situ stem cell activity and response to radiotherapy.
    Williams K, Bundred N, Landberg G, Clarke R, Farnie G
    Stem Cells, 2015;33(2):327-41.
  4. Focal adhesion kinase splice variants maintain primitive acute myeloid leukemia cells through altered wnt signaling.
    Despeaux M, Chicanne G, Rouer E, De Toni-Costes F, Bertrand J, Mansat-De Mas V, Vergnolle N, Eaves C, Payrastre B, Girault JA, Racaud-Sultan C
    Stem Cells, 2012;30(8):1597-610.
  5. The matricellular protein Cyr61 is a key mediator of platelet-derived growth factor-induced cell migration.
    Zhang F, Hao F, An D, Zeng L, Wang Y, Xu X, Cui M
    J Biol Chem, 2015;290(13):8232-42.
  6. Transmembrane collagen XVII modulates integrin dependent keratinocyte migration via PI3K/Rac1 signaling.
    Loffek S, Hurskainen T, Jackow J, Sigloch F, Schilling O, Tasanen K, Bruckner-Tuderman L, Franzke C
    PLoS ONE, 2014;9(2):e87263.
  7. A novel and essential role for FcgammaRIIa in cancer cell-induced platelet activation.
    Mitrugno A, Williams D, Kerrigan S, Moran N
    Blood, 2013;123(2):249-60.
  8. Suppression of anoikis in human intestinal epithelial cells: differentiation state-selective roles of alpha2beta1, alpha3beta1, alpha5beta1, and alpha6beta4 integrins.
    Beausejour M, Thibodeau S, Demers M, Bouchard V, Gauthier R, Beaulieu J, Vachon P
    BMC Cell Biol, 2013;14(0):53.
  9. Disruption of outer blood-retinal barrier by Toxoplasma gondii-infected monocytes is mediated by paracrinely activated FAK signaling
    HB Song, HO Jun, JH Kim, YH Lee, MH Choi, JH Kim
    PLoS ONE, 2017;12(4):e0175159.
  10. Nanog increases focal adhesion kinase (FAK) promoter activity and expression and directly binds to FAK protein to be phosphorylated.
    Ho B, Olson G, Figel S
    J. Biol. Chem., 2012;287(22):18656-73.
  11. The small GTPase RhoA regulates the contraction of smooth muscle tissues by catalyzing the assembly of cytoskeletal signaling complexes at membrane adhesion sites.
    Zhang W, Huang Y, Gunst S
    J Biol Chem, 2012;287(41):33996-4008.
  12. Thioredoxin reductase linked to cytoskeleton by focal adhesion kinase reverses actin S-nitrosylation and restores neutrophil beta(2) integrin function.
    Thom S, Bhopale V, Milovanova T, Yang M, Bogush M
    J Biol Chem, 2012;287(36):30346-57.
  13. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation.
    Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P
    PLoS ONE, 2014;9(11):e113679.
  14. Periostin links mechanical strain to inflammation in abdominal aortic aneurysm.
    Yamashita, Osamu, Yoshimura, Koichi, Nagasawa, Ayako, Ueda, Koshiro, Morikage, Noriyasu, Ikeda, Yasuhiro, Hamano, Kimikazu
    PLoS ONE, 2013;8(11):e79753.
  15. Cellular characterization of a novel focal adhesion kinase inhibitor.
    Slack-Davis et al.
    J.Biol.Chem., 2007;282:14845
  16. FAK-heterozygous mice display enhanced tumour angiogenesis.
    Kostourou et al.
    Nat.Commun., 2013;5:2020
  17. Increased nuclear stiffness via FAK-ERK1/2 signaling is necessary for synthetic mechano-growth factor E peptide-induced tenocyte migration.
    Bingyu Zhang, Qing Luo, Zhen Chen, Yisong Shi, Yang Ju, Li Yang, Guanbin Song
    Scientific Reports, 2016;0(0):2045-2322.

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Citations for PF 573228

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

48 Citations: Showing 1 - 10

  1. Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility.
    Authors: Beerli Et al.
    Nat Microbiol  2019;4:216
  2. The increased adhesion of tumor cells to endothelial cells after irradiation can be reduced by FAK-inhibition.
    Authors: Kouam Et al.
    Radiat Oncol  2019;14:25
  3. The protein tyrosine phosphatase Shp2 regulates oligodendrocyte differentiation and early myelination and contributes to timely remyelination.
    Authors: Ahrendsen Et al.
    J Neurosci  2018;38:787
  4. Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin.
    Authors: Bastounis Et al.
    Mol Biol Cell  2018;29:1571
  5. Blood vitronectin is a major activator of LIF and IL-6 in the brain through integrin-FAK and uPAR signaling.
    Authors: Keasey Et al.
    J Cell Sci  2018;131
  6. 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
  7. Tenascin-C Is a Major Component of the Fibrogenic Niche in Kidney Fibrosis.
    Authors: Fu Et al.
    J Am Soc Nephrol  2017;28:785
  8. 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
  9. Imatinib and nilo. increase glioblastoma cell invasion via Abl-independent stimulation of p130Cas and FAK signalling.
    Authors: Frolov Et al.
    Sci Rep  2016;6:27378
  10. Extracellular matrix stiffness dictates Wnt expression through integrin pathway.
    Authors: Du Et al.
    Sci Rep  2016;6:20395
  11. Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices.
    Authors: Nasrollahi and Pathak
    PLoS One  2016;6:18831
  12. 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
  13. 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
  14. Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2.
    Authors: Wang Et al.
    Br J Pharmacol  2016;173:3342
  15. 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
  16. Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes.
    Authors: Rengarajan Et al.
    Sci Rep  2016;12:e1005603
  17. 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
  18. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Redox Biol  2015;5:10468
  19. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
    Elife  2015;4:e04069
  20. 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
  21. IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function.
    Authors: Cheng Et al.
    Sci Rep  2015;212:513
  22. 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
  23. 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
  24. Astroglial-derived periostin promotes axonal regeneration after spinal cord injury.
    Authors: Shih Et al.
    J Biol Chem  2014;34:2438
  25. The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis.
    Authors: Flannagan Et al.
    Mol Biol Cell  2014;25:1511
  26. 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
  27. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86.
    Authors: Alao Et al.
    BMC Cancer  2014;14:853
  28. Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins.
    Authors: Wrighton Et al.
    PLoS Pathog  2014;111:18126
  29. Periostin links mechanical strain to inflammation in abdominal aortic aneurysm.
    Authors: Yamashita Et al.
    J Neurosci  2013;8:e79753
  30. Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis.
    Authors: Wiel Et al.
    Cell Death Dis  2013;4:e855
  31. Reversal of myofibroblast differentiation by prostaglandin E(2).
    Authors: Garrison Et al.
    Mol Cancer Ther  2013;48:550
  32. 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
  33. Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis.
    Authors: Barbelanne Et al.
    Hum Mol Genet  2013;22:2482
  34. Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor.
    Authors: Chapman Et al.
    J Immunol  2013;191:6208
  35. Microdomain heterogeneity in 3D affects the mechanics of neonatal cardiac myocyte contraction.
    Authors: Curtis Et al.
    Biomech Model Mechanobiol  2013;12:95
  36. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal  2013;11:35
  37. 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
  38. 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
  39. 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
  40. 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
  41. Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
    Authors: Canonici Et al.
    Hepatology  2011;6:e18427
  42. Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells.
    Authors: Schrader Et al.
    Biochem Biophys Res Commun  2011;53:1192
  43. A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis.
    Authors: Daley Et al.
    Dev Dyn  2011;240:2069
  44. β1 integrin mediates an alternative survival pathway in breast cancer cells resistant to lapa.
    Authors: Huang Et al.
    Breast Cancer Res  2011;13:R84
  45. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci  2010;30:749
  46. DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway.
    Authors: Ocak Et al.
    Oncogene  2010;29:6331
  47. 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
  48. Characterization of a novel focal adhesion kinase inhibitor in human platelets.
    Authors: Jones Et al.
    Nat Med  2009;389:198

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