PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk泛抑制剂。

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).

1402438-74-7

C23H22ClN7O3

479.92

PF 06273340;PF6273340;PF 6273340;PF-6273340

DMSO:90 mg/mL (187.53 mM)
H2O:Insoluble
Ethanol:1 mg/mL (2.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years