PF 573228

Name: PF 573228
Brand: Tocris Bioscience
SKU: 3239
Rating: 5 (3 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 3239

Citations (48)

(3)

COA / SDS

Catalog #

Availability

Size / Price

Qty

Key Product Details

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)
Molecular Weight:	491.49

View Full Technical Details for PF 573228

Biological Activity for PF 573228

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 573228

PF 573228 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 573228

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 for PF 573228

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	49.15	100

Preparing Stock Solutions for PF 573228

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	0.20 mL	1.02 mL	2.03 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for PF 573228

References are publications that support the biological activity of the product.

Kostourou FAK-heterozygous mice display enhanced tumour angiogenesis. Nat.Commun. 2013 PMID: 23799510
Slack-Davis Cellular characterization of a novel focal adhesion kinase inhibitor. J.Biol.Chem. 2007 PMID: 17395594

Citations for PF 573228 (48)

Showing 1 - 10 of 48 citations Showing All

Search Title:

Citations are publications that use Bio-Techne 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
Beerli et al. (2019) Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility. Nat Microbiol. 4:216
PMID: 30420785
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
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
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
Song (2017) Disruption of outer blood-retinal barrier by Toxoplasma gondii-infected monocytes is mediated by paracrinely activated FAK signaling PLoS One. 12(4):e0175159
PMID: 28406972
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Jones et al. (2009) Characterization of a novel focal adhesion kinase inhibitor in human platelets. Nat Med. 389:198
PMID: 19716803

There are no citations that match your criteria.

Showing 1 - 10 of 48 citations Showing All

Customer Reviews for PF 573228 (3)

4.7 out of 5

3 customer ratings

5 stars

67%

4 stars

33%

3 stars

2 stars

1 star

Customer Images

Showing 1 - 3 of 3 reviews Showing All

Filter By:

Cell cultures with ECM proteins, integrin blockade and In vitro drug treatments

Name: Anonymous

Species: Rat

Assay Type: In Vitro

Cell Line/Tissue: rat astroglioma C6 cells

pharmacological antagonists of FAK for 4 h before RNA or protein isolation. FAK antagonists were PF573228

PMID: 29222114
Inhibitor of FAK and effects on E0771 extracellular flux

Name: Anonymous

Species: Mouse

Assay Type: In Vitro

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

Name: Aesha Desai

Species: Human

Effective at inhibiting FAK expression when used in 2D (monolayer) and 3D (spheroid/microtissue) cell culture

There are no reviews that match your criteria.

Showing 1 - 3 of 3 reviews Showing All

Product Documents for PF 573228

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.