658401 AG 490 - CAS 133550-30-8 - Calbiochem

658401
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₄N₂O₃ 133550-30-8

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      658401-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.
          Catalogue Number658401
          Brand Family Calbiochem®
          Synonymsα-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
          References
          ReferencesJaleel, M., et al. 2004. Biochemistry 43, 8247.
          Eriksen, K.W., et al. 2001. Leukemia 15, 787.
          Kirken, R.A., et al. 1999. Leukoc. Biol. 65, 891.
          Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
          Meydan, N., et al. 1996. Nature 379, 645.
          Gazit, A., et al. 1991. J. Med. Chem. 34, 1896.
          Levitzki, A. 1990. Biochem. Pharmacol. 40, 913.
          Product Information
          CAS number133550-30-8
          ATP CompetitiveN
          FormYellow solid
          Hill FormulaC₁₇H₁₄N₂O₃
          Chemical formulaC₁₇H₁₄N₂O₃
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targetepidermal growth factor receptor kinase autophosphorylation
          Primary Target IC<sub>50</sub>100 nM against epidermal growth factor receptor kinase autophosphorylation
          Purity≥98% 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 -20°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
          Packaging Information
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          AG 490 - CAS 133550-30-8 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          AG 490 - CAS 133550-30-8 - Calbiochem Certificates of Analysis

          TitleLot Number
          658401

          References

          Reference overview
          Jaleel, M., et al. 2004. Biochemistry 43, 8247.
          Eriksen, K.W., et al. 2001. Leukemia 15, 787.
          Kirken, R.A., et al. 1999. Leukoc. Biol. 65, 891.
          Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
          Meydan, N., et al. 1996. Nature 379, 645.
          Gazit, A., et al. 1991. J. Med. Chem. 34, 1896.
          Levitzki, A. 1990. Biochem. Pharmacol. 40, 913.

          Citations

          Title
        • Yona Goldshmit, et al. (2004) SOCS2 Induces Neurite Outgrowth by Regulation of Epidermal Growth Factor Receptor Activation. Journal of Biological Chemistry 279, 16349-16355.
        • 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.

          Revision12-January-2010 RFH
          Synonymsα-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
          DescriptionA cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Jak family tyrosine kinase inhibitor. Inhibition of Jak2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal haematopoiesis. Inhibits the constitutive activation of STAT-3 and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. Also reported to inhibit guanylyl cyclase.
          FormYellow solid
          CAS number133550-30-8
          Chemical formulaC₁₇H₁₄N₂O₃
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
          Toxicity Standard Handling
          ReferencesJaleel, M., et al. 2004. Biochemistry 43, 8247.
          Eriksen, K.W., et al. 2001. Leukemia 15, 787.
          Kirken, R.A., et al. 1999. Leukoc. Biol. 65, 891.
          Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
          Meydan, N., et al. 1996. Nature 379, 645.
          Gazit, A., et al. 1991. J. Med. Chem. 34, 1896.
          Levitzki, A. 1990. Biochem. Pharmacol. 40, 913.
          Citation
        • Yona Goldshmit, et al. (2004) SOCS2 Induces Neurite Outgrowth by Regulation of Epidermal Growth Factor Receptor Activation. Journal of Biological Chemistry 279, 16349-16355.