GZD856  (Synonyms: GZD856 )

GZD856 is a novel PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities.

Description :

GZD856 is a novel PDGFRα/β inhibitor with IC₅₀s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities.

GZD856 (0.0032-10 μM) exerts antiproliferative activity against a panel of lung cancer cells^[1].

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 (10 and 30 mg/kg/day) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models^[1].