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Description

"A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFbeta RI/ALK5 (IC50 = 72 nM, [ATP] = 1 mM) by targeting both the ATP-binding site and the ""selectivity pocket"", while exhibiting much reduced or little activity against a panel of 75 other kinases (IC50<1 µ,M). Shown to reduce TGFbeta1-induced nuclear translocation of a GFP-Smad2 fusion reporter in MDA-MB-468 cells (IC50 = 22 nM) in vitro and exhibit excellent oral bioavailability (F = 75%, AUC = 4.95 µ,M.h) with low clearance (12 ml/min/kg) in rats in vivo."