ERK5-IN-2 是具有口服活性，亚微摩尔效力，选择性ERK5抑制剂，对ERK5和ERK5 MEF2D的IC50s 分别是 0.82 和 3 μM。它抑制肿瘤异种移植生长和碱性成纤维细胞生长因子驱动的基质胶塞血管生成。

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.

ERK5-IN-2 (compound 46) (p.o.; 100?mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin.ERK5-IN-2 (i.v. or p.o.; 10?mg/kg for 0.083-24?hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2?cell permeability assay in both human and mouse.

1888305-96-1

C17H11BrFN3O2

388.196

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years