TGF-β RI Kinase Inhibitor IX

A cell-permeable pyridinyloxypyridine compound that acts as a potent and highly selective inhibitor against TGFβ 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 µM). Shown to reduce TGFβ1-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 µM.h) with low clearance (12 ml/min/kg) in rats in vivo.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany