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PF-562271 besylate

Chemical Structure : PF-562271 besylate

CAS No.: 939791-38-5

PF-562271 besylate (PF562271 besylate;PF 562271 besylate)

Catalog No.: PC-42600Not For Human Use, Lab Use Only.

A potent, selective, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 14 nM, respectively.

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Biological Activity

PF-562271 besylate is a potent, selective, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 14 nM, respectively.
PF-562271 displayes robust inhibition in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM.
PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (EC50=93 ng/mL) after in tumor-bearing mice; orally bioavailable.

Physicochemical Properties

M.Wt 665.6639
Formula C27H26F3N7O6S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 21.4 mg/mL

Chemical Name/SMILES

Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-, benzenesulfonate (1:1)

References

1. Roberts WG, et al. Cancer Res. 2008 Mar 15;68(6):1935-44.

2. Stokes JB, et al. Mol Cancer Ther. 2011 Nov;10(11):2135-45.

3. Slack-Davis JK, et al. Mol Cancer Ther. 2009 Aug;8(8):2470-7.

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