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

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM).

AG 490 - CAS 133550-30-8 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: α-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

Primary Target: epidermal growth factor receptor kinase autophosphorylation
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658401
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
133550-30-8C₁₇H₁₄N₂O₃

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      658401-5MG 07790788052218

      Documentation

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

      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 Protect from light
      -20°C
      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.
      		•