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Submit ReviewPF 573228
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% (HPLC)
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.
Compound Libraries
PF 573228 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 491.49 |
| Formula | C22H20F3N5O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 869288-64-2 |
| PubChem ID | 11612883 |
| InChI Key | HESLKTSGTIBHJU-UHFFFAOYSA-N |
| Smiles | O=C(N3)CCC1=C3C=CC(NC2=NC(NCC4=CC=CC(S(=O)(C)=O)=C4)=C(C(F)(F)F)C=N2)=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 491.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.03 mL | 10.17 mL | 20.35 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.07 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.03 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Slack-Davis et al (2007) Cellular characterization of a novel focal adhesion kinase inhibitor. J.Biol.Chem. 282 14845 PMID: 17395594
Kostourou et al (2013) FAK-heterozygous mice display enhanced tumour angiogenesis. Nat.Commun. 5 2020 PMID: 23799510
If you know of a relevant reference for PF 573228, please let us know.
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Keywords: PF 573228, PF 573228 supplier, Potent, selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, PF573228, Kinase, 3239, Tocris Bioscience
47 Citations for PF 573228
Citations are publications that use Tocris products. Selected citations for PF 573228 include:
Kouam et al (2019) The increased adhesion of tumor cells to endothelial cells after irradiation can be reduced by FAK-inhibition. Radiat Oncol 14 25 PMID: 30717801
Canonici et al (2011) Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor. Hepatology 6 e18427 PMID: 21483797
Schrader et al (2011) Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells. Biochem Biophys Res Commun 53 1192 PMID: 21442631
Keasey et al (2018) Blood vitronectin is a major activator of LIF and IL-6 in the brain through integrin-FAK and uPAR signaling. J Cell Sci 131 PMID: 29222114
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
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
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Redox Biol 5 10468 PMID: 26020477
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
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
Bastounis et al (2018) Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin. Mol Biol Cell 29 1571 PMID: 29718765
Wang et al (2016) Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2. Br J Pharmacol 173 3342 PMID: 27638545
Deevi et al (2014) Essential function for PDLIM2 in cell polarization in three-dimensional cultures by feedback regulation of the β1-integrin-RhoA signaling axis. Neoplasia 16 422 PMID: 24863845
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
Ahrendsen et al (2018) The protein tyrosine phosphatase Shp2 regulates oligodendrocyte differentiation and early myelination and contributes to timely remyelination. J Neurosci 38 787 PMID: 29217681
Nasrollahi and Pathak (2016) Topographic confinement of epithelial clusters induces epithelial-to-mesenchymal transition in compliant matrices. PLoS One 6 18831 PMID: 26728047
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
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540
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
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
Du et al (2016) Extracellular matrix stiffness dictates Wnt expression through integrin pathway. Sci Rep 6 20395 PMID: 26854061
Roa-Espitia et al (2016) Focal adhesion kinase is required for actin polymerization and remodeling of the cytoskeleton during sperm capacitation. Biol Open 5 1189 PMID: 27402964
Frolov et al (2016) Imatinib and nilo. increase glioblastoma cell invasion via Abl-independent stimulation of p130Cas and FAK signalling. Sci Rep 6 27378 PMID: 27293031
Barbelanne et al (2013) Pathogenic NPHP5 mutations impair protein interaction with Cep290, a prerequisite for ciliogenesis. Hum Mol Genet 22 2482 PMID: 23446637
Curtis et al (2013) Microdomain heterogeneity in 3D affects the mechanics of neonatal cardiac myocyte contraction. Biomech Model Mechanobiol 12 95 PMID: 22407215
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
Sero and Bakal (2017) Multiparametric Analysis of Cell Shape Demonstrates that β-PIX Directly Couples YAP Activation to Extracellular Matrix Adhesion. Cell Syst 4 84 PMID: 28065575
Song (2017) Disruption of outer blood-retinal barrier by Toxoplasma gondii-infected monocytes is mediated by paracrinely activated FAK signaling PLoS One 12 e0175159 PMID: 28406972
Robinson et al (2015) Segmentation of Image Data from Complex Organotypic 3D Models of Cancer Tissues with Markov Random Fields. PLoS One 10 e0143798 PMID: 26630674
Ji et al (2015) WISP-2 in human gastric cancer and its potential metastatic suppressor role in gastric cancer cells mediated by JNK and PLC-γ pathways. Br J Cancer 113 921 PMID: 26291058
Chapman et al (2013) Focal adhesion kinase negatively regulates Lck function downstream of the T cell antigen receptor. J Immunol 191 6208 PMID: 24227778
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
Wiel et al (2013) Lysyl oxidase activity regulates oncogenic stress response and tumorigenesis. Cell Death Dis 4 e855 PMID: 24113189
Huang et al (2011) β1 integrin mediates an alternative survival pathway in breast cancer cells resistant to lapa. Breast Cancer Res 13 R84 PMID: 21884573
Jones et al (2009) Characterization of a novel focal adhesion kinase inhibitor in human platelets. Nat Med 389 198 PMID: 19716803
Fu et al (2017) Tenascin-C Is a Major Component of the Fibrogenic Niche in Kidney Fibrosis. J Am Soc Nephrol 28 785 PMID: 27612995
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
Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069 PMID: 25621765
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
Shih et al (2014) Astroglial-derived periostin promotes axonal regeneration after spinal cord injury. J Biol Chem 34 2438 PMID: 24523534
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
Garrison et al (2013) Reversal of myofibroblast differentiation by prostaglandin E(2). Mol Cancer Ther 48 550 PMID: 23470625
Yamashita et al (2013) Periostin links mechanical strain to inflammation in abdominal aortic aneurysm. J Neurosci 8 e79753 PMID: 24260297
Daley et al (2011) A focal adhesion protein-based mechanochemical checkpoint regulates cleft progression during branching morphogenesis. Dev Dyn 240 2069 PMID: 22016182
Do you know of a great paper that uses PF 573228 from Tocris? Please let us know.
Reviews for PF 573228
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Filter by:
Inhibitor of FAK and effects on E0771 extracellular flux.
By
Anonymous on 10/10/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: E0771
Extracellular flux analysis (Seahorse experiments) of breast cancer cells. 5uM dose used for 48hrs
Inhibiting FAK expression in 2D and 3D cell culture.
By
Aesha Desai on 01/04/2018
Species: Human
Effective at inhibiting FAK expression when used in 2D (monolayer) and 3D (spheroid/microtissue) cell culture
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