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Beschreibung

A cell-permeable, quinoline that binds directly to ezrin (Kd = 12.6 µ,M) in a reversible manner, and inhibits PKCiota-mediated ezrin phosphorylation at Thr567 (IC50 = 8.1 µ,M) and ezrin-actin binding, in vitro. It also inhibits murine osteosarcoma K7M2 cell invasion in a monolayer of HUVEC cells, dose-dependently, from 1 to 10 µ,M. At 10 µ,M, it causes a unique developmental defect in zebrafish, characterized by reduced motility of eye progenitor cells. Furthermore, this small molecule prevents metastatic growth in an ex vivo mouse lung organ culture assay at 10 µ,M and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vivo at 2.26 mg/kg/day.