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PF-04217903 mesylate

CAS No. : 956906-93-7

MCE 国际站：PF-04217903 mesylate

产品活性：PF-04217903 mesylate 是一种高效的ATP竞争性 c-Met 激酶抑制剂，K_i 为 4.8 nM。PF-04217903 mesylate 相对于 208 个激酶显示出 1000 倍以上的选择性。具有抗血管生成特性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Met/HGFR

In Vitro: PF-04217903 mesylate (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively.
PF-04217903 mesylate induces apoptosis of GTL-16 cells (IC₅₀=31 nM) .
PF-04217903 mesylate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC₅₀= 7-12.5 nM).
PF-04217903 mesylate displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC₅₀ of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC₅₀ of >10 μM.

In Vivo: PF-04217903 mesylate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors .
PF-04217903 mesylate (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 mesylate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 mesylate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors.

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