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PF-562271 HCl

In stock
Catalog No.
A8345
FAK/Pyk2 inhibitor
Grouped product items
SizePriceStock Qty
Evaluation Sample
$28.00
In stock
5mg
$120.00
In stock
10mg
$190.00
In stock
50mg
$470.00
In stock

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PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.

References:
[1]Stokes JB, Adair SJ, Slack-Davis JK, Walters DM, Tilghman RW, Hershey ED, Lowrey B, Thomas KS, Bouton AH, Hwang RF, Stelow EB, Parsons JT, Bauer TW. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45. doi: 10.1158/1535-7163.MCT-11-0261. Epub 2011 Sep 8.
[2]Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt543.95
Cas No.939791-41-0
FormulaC21H21ClF3N7O3S
SynonymsPF562271 HCl;PF 562271 HCl
Solubility≥26.35mg/mL in DMSO with gentle warming
Chemical NameN-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide hydrochloride
SDFDownload SDF
Canonical SMILESO=C1NC2=C(C1)C=C(C=C2)NC3=NC=C(C(F)(F)F)C(NCC4=C(N(S(=O)(C)=O)C)N=CC=C4)=N3.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description PF-562271 HCl, the hydrochloride salt of PF-562271, is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Targets FAK Pyk2        
IC50 1.5 nM 14 nM        

Quality Control

Chemical structure

PF-562271 HCl

Related Biological Data

PF-562271 HCl

Related Biological Data

PF-562271 HCl