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

505819
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₂₃FN₆O₅ 841290-80-0

      Pricing & Availability

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      5.05819.0001
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          Glass bottle 5 mg
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          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          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 +2°C to +8°C
          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.
          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.