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PF-562271 besylate — Datasheet

CAT. NO. DC3168

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ParameterValue
Chemical NamePF-562271 Besylate
CAS No.939791-38-5
SynonymsPF-562271 PhSO3H salt;benzenesulfonic acid,N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide;PF 562271 Besylate;PF-562271;N-(3-(((2-((2,3-Dihydro-2-oxo-1H-indol-5-yl)amino)-5- (trifluoromethyl)-4-pyrimidinyl)amino)methyl)-2-pyridinyl)-N-methyl-methanesulfonamide benzenesulfonate;PF 562271;N-[3-[[[2-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide benzenesulfonate;PF-00562271;PF562271 besylate;N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide benzenesulfonate;FK2M84H8UI;HMS3651N09;BCP14770;s2672;C21H20F3N7O3S.C6H6O3S;SB12448;AK31;PF-562271 besylate
FormulaC27H26F3N7O6S2
M.Wt665.66
SMILESO=C1NC2=C(C1)C=C(C=C2)NC3N=C(NCC4C(=NC=CC=4)N(C)S(=O)(C)=O)C(=CN=3)C(F)(F)F.OS(=O)(=O)C1=CC=CC=C1
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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.

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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