GZD856

GZD856 is an orally bioavailable inhibitor of PDGFRα and PDGFRβ with IC50 values of 68.6 and 136.6 nM, respectively. GZD856 has demonstrated anti-lung cancer activities in experimental studies. The molecular activity profile of GZD856 supports its utilization in research investigating PDGFR-associated signaling pathways, tumor biology, kinase inhibition, and mechanisms relevant to lung cancer progression.

PDGFRβ:136.6 nM, PDGFRα:68.6 nM, BCR-ABL:15.4 nM, BCR-ABL (T315I):19.9 nM

Method: The inhibitory activities of GZD856 against platelet-derived growth factor receptors alpha and beta were evaluated using a cell-free kinase assay.
Rresult: GZD856 inhibited platelet-derived growth factor receptor alpha and beta kinase activities with IC50 values of 68.6 and 136.6 nM, respectively.[1]
Method: The inhibitory activities of GZD856 against native Bcr-Abl and the Bcr-Abl T315I mutant were evaluated using a cell-free kinase assay.
Rresult: GZD856 inhibited native Bcr-Abl and Bcr-Abl T315I mutant kinase activities with IC50 values of 19.9 and 15.4 nM, respectively.[2]

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%.