PF 573228

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Cat.No. 3239 - PF 573228 | C22H20F3N5O3S | CAS No. 869288-64-2
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)
Datasheet
Citations (31)
Literature

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Product Action

View all Focal Adhesion Kinase Inhibitors

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

31 Citations for PF 573228

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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