General description
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria to qualify for the following awards: