PF 573228

Cat. No. 3239

PF 573228 C22H20F3N5O3S [869288-64-2]

Price and Availability

For PF 573228 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View 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.

.

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.

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.

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.

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.

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.

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

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.

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

View Related Products by Target

View Related Products by Product Action

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

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Kinase Inhibitor Toolbox

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

Kinases Product Listing

Kinases Product Listing

Our Kinase listing highlights over 400 products for kinase research. Request copy or view PDF today.

divider line

VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Life Science Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance. Request copy today.

divider line

New Products in this Area

rac-CCT 250863

Potent Nek2 inhibitor

Roscovitine

Potent, selective cyclin-dependent kinase inhibitor

Enzastaurin

Potent PKCβ inhibitor

BMS 265246

Potent cdk1/2 inhibitor

Autocamtide-2-related inhibitory peptide, myristoylated

CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptide

MP A08

Selective ATP competitive SphK1 and 2 inhibitor; cell permeable

Akti-1/2

Potent and selective dual Akt1 and 2 inhibitor

VX 680

High affinity and selective Aurora kinase inhibitor

Imatinib mesylate

Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kit

TGX 221

Potent and selective PI 3-kinase β inhibitor

PF 543 hydrochloride

Potent and selective SphK1 inhibitor

JX 06

Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor

MRT 68601 hydrochloride

Potent TBK1 inhibitor

Sign-up for new product e-alerts
divider line

LinkedIn Updates

Follow Tocris on LinkedIn

Follow us on LinkedIn!

Visit our LinkedIn page for the latest Tocris news, events and updates.