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GZD856

CAS No. : 1257628-64-0

MCE 站：GZD856

产品活性：GZD856是一种新型，有口服活性的 PDGFRα/β 抑制剂，IC₅₀ 分别为68.6和136.6 nM。 具有抗肺癌活性。也是 Bcr-Abl^T315I 的抑制剂，对Bcr-Abl 和T315I突变型的 IC₅₀ 分别为19.9 和 15.4?nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：PDGFR  |  Bcr-Abl

In Vitro: GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells.

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

GZD856 strongly suppresses the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-Abl^WT and Bcr-Abl^T315I, with IC₅₀s of 2.2, 67.0, 0.64 and 10.8?nM, respectively.

In Vivo: 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%.

GZD856 (10?mg/kg/day, 8 days, oral) potently suppresses tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-Abl^T315I.

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