PF-573228

• CAT Number: I005228
• CAS Number: 869288-64-2
• Molecular Formula: C₂₂H₂₀F₃N₅O₃S
• Molecular Weight: 491.49
• Purity: ≥95%
• Target: FAK
• Solubility: DMSO: ≥ 51 mg/mL
• Storage: 3 years -20C powder
• IC50: 4 nM
• InChI: InChI=1S/C22H20F3N5O3S/c1-34(32,33)16-4-2-3-13(9-16)11-26-20-17(22(23,24)25)12-27-21(30-20)28-15-6-7-18-14(10-15)5-8-19(31)29-18/h2-4,6-7,9-10,12H,5,8,11H2,1H3,(H,29,31)(H2,26,27,28,30)
• InChIKey: HESLKTSGTIBHJU-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4

PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for inhibiton of purified recombinant catalytic fragment of FAK; inhibits FAK phosphorylation on Tyr(397) with an IC(50) of 30-100 nM.
IC50 value: 4 nM [1]
Target: FAK
in vitro: inhibited purified recombinant catalytic fragment of FAK with an IC(50) of 4 nM. In cultured cells, PF-573,228 inhibited FAK phosphorylation on Tyr(397) with an IC(50) of 30-100 nM. Treatment of cells with concentrations of PF-573,228 that significantly decreased FAK Tyr(397) phosphorylation failed to inhibit cell growth or induce apoptosis [1]. Treatment with either FAK Inhibitor 14 or PF-573,228 resulted in reduced HUVEC viability, migration and tube formation in response to vascular endothelial growth factor (VEGF). Furthermore, we found that PF-573,228 had the added ability to induce apoptosis of endothelial cells within 36 h post-drug administration even in the continued presence of VEGF stimulation [2]. In whole-cell experiments, PF573228 reversibly increased the amplitude of Ca(2+)-activated K(+) currents (I(K(Ca))) in GH(3) cells. In inside-out recordings, this compound added to the bath did not modify single-channel conductance but stimulated large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels with an EC(50) value of 3.2 μM [3].

Reference

[1]. Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
[2]. Cabrita MA, et al. Focal adhesion kinase inhibitors are potent anti-angiogenic agents. Mol Oncol. 2011 Dec;5(6):517-26.
[3]. So EC, et al. Evidence for activation of BK Ca channels by a known inhibitor of focal adhesion kinase, PF573228. Life Sci. 2011 Nov 7;89(19-20):691-701.