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Product Description
PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 13 nM, and has > 100-fold selectivity against other protein kinases, except for some CDKs.
IC50 & Target: IC50: 1.5 nM (FAK), 13 nM (Pyk2)
In Vitro: PF-562,271 is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays[1]. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays[2]. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength[3].
In Vivo: PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo[3].
Information
CAS No939791-38-5
FormulaC27H26F3N7O6S2
Clinical Informationclinicalinformation
PathwayProtein Tyrosine Kinase/RTK Protein Tyrosine Kinase/RTK
TargetPyk2 FAK
Specifications
Purity / Grade>98%
SolubilityDMSO : 21.4 mg/mL (32.15 mM; Need ultrasonic and warming)
Smilessmiles
Misc Information
Alternative NamesPF562271 besylate;PF 562271 besylate
Observed Molecular Weight665.66
related data
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