PF 573228

Cat. No. 3239

PF 573228 C22H20F3N5O3S [869288-64-2]

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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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Kostourou et al (2013) FAK-heterozygous mice display enhanced tumour angiogenesis. Nat.Commun. 5 2020. PMID: 23799510.

Slack-Davis et al (2007) Cellular characterization of a novel focal adhesion kinase inhibitor. J.Biol.Chem. 282 14845. PMID: 17395594.

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If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PF 573228 include:

Alowayed et al (2016) LEFTY2 Controls Migration of Human Endometrial Cancer Cells via Focal Adhesion Kinase Activity (FAK) and miRNA-200a Cell Physiol Biochem 39 815. PMID: 27497669.

Hennigan et al (2016) Eosinophil peroxidase activates cells by HER2 receptor engagement and β1-integrin clustering with downstream MAPK cell signaling Clinical Immunology 171 1. PMID: 27519953.

Nasrollahi and Pathak (2016) Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices. PLoS One 6 18831. PMID: 26728047.

Rengarajan et al (2016) Endothelial Cells Use a Formin-Dependent Phagocytosis-Like Process to Internalize the Bacterium Listeria monocytogenes. Sci Rep 12 e1005603. PMID: 27152864.

Carrim et al (2015) Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIbα. J Exp Med 6 640. PMID: 26569550.

Cheng et al (2015) IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function. Sci Rep 212 513. PMID: 25779634.

Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069. PMID: 25621765.

Webber et al (2015) Combination of heat shock protein 90 and focal adhesion kinase inhibitors synergistically inhibits the growth of non-small cell lung cancer cells. Oncoscience 2 765. PMID: 26501082.

Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Redox Biol 5 10468. PMID: 26020477.

Alao et al (2014) Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer 14 853. PMID: 25409876.

Flannagan et al (2014) The phosphatidylserine receptor TIM4 utilizes integrins as coreceptors to effect phagocytosis. Mol Biol Cell 25 1511. PMID: 24623723.

Shih et al (2014) Astroglial-derived periostin promotes axonal regeneration after spinal cord injury. J Biol Chem 34 2438. PMID: 24523534.

Wrighton et al (2014) Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins. PLoS Pathog 111 18126. PMID: 25422477.

Chapman et al (2013) Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor. J Immunol 191 6208. PMID: 24227778.

Garrison et al (2013) Reversal of myofibroblast differentiation by prostaglandin E(2). Mol Cancer Ther 48 550. PMID: 23470625.

Keasey et al (2013) Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression. Cell Commun Signal 11 35. PMID: 23693126.

Quint et al (2013) Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways. PLoS One 288 5398. PMID: 23300082.

Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855. PMID: 24113189.

Yamashita et al (2013) Periostin links mechanical strain to inflammation in abdominal aortic aneurysm. J Neurosci 8 e79753. PMID: 24260297.

Beauséjour et al (2012) 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. Apoptosis 17 566. PMID: 22402981.

Chu et al (2012) Contractile Activity Regulates Inducible Nitric Oxide Synthase Expression and NO(i) Production in Cardiomyocytes via a FAK-Dependent Signaling Pathway. J Signal Transduct 2012 473410. PMID: 22900166.

Guessous et al (2012) Cooperation between c-Met and focal adhesion kinase family members in medulloblastoma and implications for therapy. Mol Cancer 11 288. PMID: 22188814.

Wong et al (2012) Focal adhesion kinase links mechanical force to skin fibrosis via inflammatory signaling. Am J Respir Cell Mol Biol 18 148. PMID: 22157678.

Canonici et al (2011) Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor. Hepatology 6 e18427. PMID: 21483797.

Daley et al (2011) A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis. Dev Dyn 240 2069. PMID: 22016182.

Schrader et al (2011) Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells. Biochem Biophys Res Commun 53 1192. PMID: 21442631.

Hao et al (2010) tPA is a potent mitogen for renal interstitial fibroblasts: role of beta1 integrin/focal adhesion kinase signaling. Am J Pathol 177 1164. PMID: 20639453.

Ocak et al (2010) DNA copy number aberrations in small-cell lung cancer reveal activation of the focal adhesion pathway. Oncogene 29 6331. PMID: 20802517.

Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749. PMID: 20071540.

Jones et al (2009) Characterization of a novel focal adhesion kinase inhibitor in human platelets. Nat Med 389 198. PMID: 19716803.

Do you know of a great paper that uses PF 573228 from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: PF 573228, supplier, Potent, selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, PF573228, Tocris Bioscience, Focal Adhesion Kinase Inhibitor products

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