616463 TGF-β RI Kinase Inhibitor IX - Calbiochem

TGF-β RI Kinase Inhibitor IX - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX

616463
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₈N₄O₃S

Pricing & Availability

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616463-10MG
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      Description
      OverviewA 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 Number616463
      Brand Family Calbiochem®
      Synonyms4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX
      References
      ReferencesGoldberg, F.W., et al. 2009. J. Med. Chem. 52, 7901.
      Product Information
      FormOff-white powder
      Hill FormulaC₁₈H₁₈N₄O₃S
      Chemical formulaC₁₈H₁₈N₄O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      TGF-β RI Kinase Inhibitor IX - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      TGF-β RI Kinase Inhibitor IX - Calbiochem Certificates of Analysis

      TitleLot 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.

      Revision14-March-2011 RFH
      Synonyms4-((4-((2,6-Dimethylpyridin-3-yl)oxy)pyridin-2-yl)amino)benzenesulfonamide, ALK5 Inhibitor IX
      DescriptionA 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.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₈N₄O₃S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesGoldberg, F.W., et al. 2009. J. Med. Chem. 52, 7901.