PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively[1]. Anti-hyperalgesic effect[1].
PF-6683324 (Trk-IN-4) (Compound 10b) exhibits superb Trk selectivity with >95% inhibition of TrkA and >40% inhibition of only 1 other kinase VEGFR2 (cell-based assay for VEGFR2 IC50>5 μM)[1].
[1]. Bagal SK, et al. Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain. J Med Chem. 2018 Aug 9;61(15):6779-6800.