PF-6683324 (Trk-IN-4) 是一种有效的 pan-Trk 抑制剂，抑制 TrkA，TrkB 和 TrkC 细胞，IC50 分别为 1.9 nM，2.6 nM 和 1.1 nM。具有抗痛觉过敏作用。
货号:ajcx38734
CAS:1799788-94-5
分子式:C24H23F4N5O4
分子量：521.46
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

Protocol:

TrkA 1.9nM(IC50,incell-basedassays)

TrkB 2.6nM(IC50,incell-basedassays)

TrkC 1.1nM(IC50,incell-basedassays)