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Description
Overview
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.
Catalogue Number
616463
Brand Family
Calbiochem®
Synonyms
4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX
References
References
Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.
TGF-β RI Kinase Inhibitor IX - Calbiochem Certificates of Analysis
Title
Lot Number
616463
References
Reference overview
Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
14-March-2011 RFH
Synonyms
4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX
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.
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₁₈H₁₈N₄O₃S
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Goldberg, F.W., et al. 2009. J. Med. Chem.52, 7901.
