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505819 Syk Inhibitor VI, R406 - CAS 841290-80-0 - Calbiochem

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Synonymes: N⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one

Primary Target: Syk kinase
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      841290-80-0C₂₂H₂₃FN₆O₅
      Description
      OverviewA cell-permeable, orally bioavailable pyrimidinediamino compound with anti-inflammatory and anti-tumor properties. Acts as a potent, reversible and ATP-competitive inhibitor of Syk kinase (IC50 = 41 nM; Ki = 30 nM). Exhibits high selectivity over a broad panel of other protein kinases (˜300 nM), ion channels, and enzymes. Blocks Syk-dependent FcR-mediated activation of monocytes/macrophages, and neutrophils and inhibits Anti-IgE-mediated degranulation in cultured human mast cells (EC50 = 56 nM as measured by tryptase release). At higher concentrations, it is shown to block adenosine A3 receptors, adenosine transporter, and monoamine transporter (IC50 = 81 nM, 1.84 µM, and 2.74 µM, respectively), and Flt3 autophosphorylation. Shown to reduce immune complex-mediated inflammation in murine models (˜10 mg/kg) and diminish airway hyper-responsiveness in asthma models.
      Catalogue Number505819
      Brand Family Calbiochem®
      SynonymsN⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
      References
      ReferencesFriedberg, J.W., et al. 2010. Blood 115, 2578.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Chen, L., et al. 2008. Blood 111, 2230.
      Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.
      Product Information
      CAS number841290-80-0
      FormOff-white powder
      Hill FormulaC₂₂H₂₃FN₆O₅
      Chemical formulaC₂₂H₂₃FN₆O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSyk kinase
      Primary Target K<sub>i</sub>30 nM)
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      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 reconstitution, 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
      Global Trade Item Number
      Référence GTIN
      505819 0

      Documentation

      Syk Inhibitor VI, R406 - CAS 841290-80-0 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Friedberg, J.W., et al. 2010. Blood 115, 2578.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Chen, L., et al. 2008. Blood 111, 2230.
      Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.
      Fiche technique

      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.

      Revision27-September-2013 JSW
      SynonymsN⁴-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N²-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
      DescriptionA cell-permeable, orally bioavailable pyrimidinediamino compound with anti-inflammatory and anti-tumor properties. Acts as a potent, reversible and ATP-competitive inhibitor of Syk kinase (IC50 = 41 nM; Ki = 30 nM). Exhibits high selectivity over a broad panel of other protein kinases (˜300 nM), ion channels, and enzymes. Blocks Syk-dependent FcR-mediated activation of monocytes/macrophages, and neutrophils and inhibits Anti-IgE-mediated degranulation in cultured human mast cells (EC50 = 56 nM as measured by tryptase release). At higher concentrations, it is shown to block adenosine A3 receptors, adenosine transporter, and monoamine transporter (IC50 = 81 nM, 1.84 µM, and 2.74 µM, respectively), and Flt3 autophosphorylation. Shown to reduce immune complex-mediated inflammation in murine models (˜10 mg/kg) and diminish airway hyper-responsiveness in asthma models.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number841290-80-0
      Chemical formulaC₂₂H₂₃FN₆O₅
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesFriedberg, J.W., et al. 2010. Blood 115, 2578.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Young, R.M., et al. 2009. Blood 113, 2508.
      Chen, L., et al. 2008. Blood 111, 2230.
      Braselmann, S., et al. 2006. J. Pharmacol. Exp. Ther. 319, 998.