Description |
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
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Target |
IC50: 4 nM (FAK)[1]
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In Vitro |
PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC50 of 4 nM. In cultured cells, PF-573228 inhibits FAK phosphorylation on Tyr397 with an IC50 of 30-100 nM. Treatment of cells with concentrations of PF-573228 that significantly decreased FAK Tyr397 phosphorylation fails to inhibit cell growth or induce apoptosis. In contrast, treatment with PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover[1].
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Cell Assay |
REF52 or PC3 cells are seeded into a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor (PF-573228) for 3 days. Subsequently, the cells are harvested and counted. Apoptosis assays are performed using a cell death detection ELISA. REF52, PC3 or MDCKcells are treated for 24 h (16 h for MDCK) with the indicated concentrations of each inhibitor prior to lysis. Cells suspended for 16-24 h in serum-free medium served as a positive control. The cell lysates are incubated in duplicate in the ELISA system. The data represent the means±standard deviation of one of three experiments performed in duplicate[1].
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Density | 1.5±0.1 g/cm3 |
Exact Mass | 491.123901 |
PSA | 121.46000 |
LogP | 1.03 |
Storage condition | Store at +4°C |