GZD856

GZD856 is a novel PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities[1].

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

Research Areas >> Cancer

IC50: 68.6 nM (PDGFRα), 136.6 nM (PDGFRβ)[1]

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[1]. GZD856 induces dose-dependent G0/G1 phase arrest and apoptosis in H1703 cells but not in A549 cells[1].

GZD856 (10 and 30 mg/kg/day) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models[1]. GZD856 exhibits dose-dependent suppression of PDGFRα and PDGFRβ activation and downstream signaling in H1703 and A549 tumor tissues[1]. GZD856 displays promising in vivo therapeutic effects on PDGFRα-/PDGFRβ+ A549 cancer cells in a Luc orthotopic model, inhibiting both tumor growth and tumor metastasis[1].

[1]. Zhang Z, et al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178.

Nintedanib (BIBF 1120) | Crenolanib | SU 5402 | Linifanib (ABT-869) | Cediranib | Masitinib (AB1010) | SU14813 | Dovitinib (TKI-258, CHIR-258) | CHIR-124 | CP-673451 | ENMD-2076 | TG 100572 (Hydrochloride) | DCC-2618 | Telatinib | PP121