GZD856 shows dose-dependent inhibition of PDGFRα and PDGFRβ phosphorylation in H1703 and A549 cells, respectively.?The activation of downstream AKT (phosphorylation of S473 but not T308), ERK1/2 and STAT3 is also observed after exposure to GZD856, with no obvious effects on total protein levels.GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells.

GZD856 (10 and 30 mg/kg/day, 16 days) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models.?A 25-mg/kg oral dose of GZD856 exhibits a long half-life of 22.2 h, optimal plasma exposure (Cmax, 899.5 μg/L) and a good oral bioavailability of 78%.