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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
658401
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
133550-30-8C₁₇H₁₄N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
658401-5MG Plastic ampoule 5 mg
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 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.

Brochure

Title
An Introduction to Inhibitors and Their Biological Applications - 1st Edition
Caspases and other Apoptosis Related Tools Brochure

Posters

Title
Human Kinome & InhibitorSelect™ Libraries

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.
    		•