Bioactivity | 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]. | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | PF-6683324 | ||||||||||||
CAS | 1799788-94-5 | ||||||||||||
Formula | C24H23F4N5O4 | ||||||||||||
Molar Mass | 521.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |