PF-573228

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WARNING: This product is for research use only, not for human or veterinary use.

Description: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. PF573228 was recognized to affect cell adhesion and migration in many types of cells.

Price and Availability

PF-573228,purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406126Name: PF-573228CAS#: 869288-64-2Chemical Formula: C22H20F3N5O3SExact Mass: 491.12389Molecular Weight: 491.48611Elemental Analysis: C, 53.76; H, 4.10; F, 11.60; N, 14.25; O, 9.77; S, 6.52

Synonym:PF573228; PF 573228; PF-573228; PF573,228; PF 573,228; PF-573,228.

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

InChi Key:HESLKTSGTIBHJU-UHFFFAOYSA-N

InChi Code:InChI=1S/C22H20F3N5O3S/c1-34(32,33)16-4-2-3-13(9-16)11-26-20-17(22(23,24)25)12-27-21(30-20)28-15-6-7-18-14(10-15)5-8-19(31)29-18/h2-4,6-7,9-10,12H,5,8,11H2,1H3,(H,29,31)(H2,26,27,28,30)

SMILES Code:O=C1NC2=C(C=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC(S(=O)(C)=O)=C4)=N3)C=C2)CC1

Technical Data

Additional Information

References

1: Melo TG, Tucci AR, Nogueira AR, Meirelles Mde N,Pereira MC. The involvement of FAK and Src in the invasion ofcardiomyocytes by Trypanosoma cruzi. Exp Parasitol. 2014 Apr;139:49-57.doi: 10.1016/j.exppara.2014.02.008. Epub 2014 Feb 25. PubMed PMID:24582948.

2: Xu B, Ju Y, Song G. Role of p38, ERK1/2, focal adhesion kinase, RhoA/ROCKand cytoskeleton in the adipogenesis of human mesenchymal stem cells. JBiosci Bioeng. 2014 May;117(5):624-31. doi:10.1016/j.jbiosc.2013.10.018. Epub 2013 Dec 9. PubMed PMID: 24331979.

3: Beauséjour M, Thibodeau S, Demers MJ, Bouchard V, Gauthier R,Beaulieu JF, Vachon PH. Suppression of anoikis in human intestinalepithelial cells: differentiation state-selective roles of α2β1, α3β1,α5β1, and α6β4 integrins. BMC Cell Biol. 2013 Dec 1;14:53. doi:10.1186/1471-2121-14-53. PubMed PMID: 24289209.

4: Chan D, Thomas CJ, Taylor VJ, Burke RD. Integrins on eggs: focaladhesion kinase is activated at fertilization, forms a complex withintegrins, and is necessary for cortex formation and cell cycleinitiation. Mol Biol Cell. 2013 Nov;24(21):3472-81. doi:10.1091/mbc.E13-03-0148. Epub 2013 Aug 28. PubMed PMID: 23985318; PubMedCentral PMCID: PMC3814141.

5: Wiemer AJ, Wernimont SA, Cung TD, Bennin DA, Beggs HE, HuttenlocherA. The focal adhesion kinase inhibitor PF-562,271 impairs primary CD4+ Tcell activation. Biochem Pharmacol. 2013 Sep 15;86(6):770-81. doi:10.1016/j.bcp.2013.07.024. Epub 2013 Aug 5. PubMed PMID: 23928188;PubMed Central PMCID: PMC3762933.

6: Kline ER, Shupe J, Gilbert-Ross M, Zhou W, Marcus AI. LKB1 repressesfocal adhesion kinase (FAK) signaling via a FAK-LKB1 complex to regulateFAK site maturation and directional persistence. J Biol Chem. 2013 Jun14;288(24):17663-74. doi: 10.1074/jbc.M112.444620. Epub 2013 May 1.PubMed PMID: 23637231; PubMed Central PMCID: PMC3682567.

7: Moore SW, Zhang X, Lynch CD, Sheetz MP. Netrin-1 attracts axonsthrough FAK-dependent mechanotransduction. J Neurosci. 2012 Aug22;32(34):11574-85. doi: 10.1523/JNEUROSCI.0999-12.2012. PubMed PMID:22915102; PubMed Central PMCID: PMC3461192.

8: Hori Y, Kashimoto T, Yonezawa T, Sano N, Saitoh R, Igarashi S,Chikazawa S, Kanai K, Hoshi F, Itoh N, Higuchi S. Matrixmetalloproteinase-2 stimulates collagen-I expression throughphosphorylation of focal adhesion kinase in rat cardiac fibroblasts. AmJ Physiol Cell Physiol. 2012 Nov 1;303(9):C947-53. doi:10.1152/ajpcell.00401.2011. Epub 2012 Aug 22. PubMed PMID: 22914642.

9: Tse KW, Lin KB, Dang-Lawson M, Guzman-Perez A, Aspnes GE, BuckbinderL, Gold MR. Small molecule inhibitors of the Pyk2 and FAK kinasesmodulate chemoattractant-induced migration, adhesion and Akt activationin follicular and marginal zone B cells. Cell Immunol. 2012Jan-Feb;275(1-2):47-54. doi: 10.1016/j.cellimm.2012.03.002. Epub 2012Mar 29. PubMed PMID: 22507871.

10: Guessous F, Yang Y, Johnson E, Marcinkiewicz L, Smith M, Zhang Y,Kofman A, Schiff D, Christensen J, Abounader R. Cooperation betweenc-Met and focal adhesion kinase family members in medulloblastoma andimplications for therapy. Mol Cancer Ther. 2012 Feb;11(2):288-97. doi:10.1158/1535-7163.MCT-11-0490. Epub 2011 Dec 21. PubMed PMID: 22188814;PubMed Central PMCID: PMC3277676.