一般描述
A cell-permeable pyridinylimidazole compound that acts as a potent, reversible, and ATP-binding site-targeting inhibitor of Tie2 (IC50 = 250 nM) with ~ 200-fold selectivity over p38 MAPK and greater than 10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β. Shown to exhibit antiangiogenesis activity in a Matrigel assay (70% reduction, 50 mg/kg/0.5 day, i.p.) and inhibit the growth of xenografted tumor (no apparent growth up to 20 days, 25 mg/kg/0.5 day, i.p.) in mice in vivo.
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
储存分类代码
10-13 - German Storage Class 10 to 13
法规信息
新产品
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Marcus Semones et al.
Bioorganic & medicinal chemistry letters, 17(17), 4756-4760 (2007-07-10)
This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315
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