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658552 AG 1478 - CAS 175178-82-2 - Calbiochem

AG 1478, CAS 175178-82-2, is a cell-permeable, potent, selective, reversible & ATP-competitive inhibitor of EGF receptor kinase (IC50 = 3 nM vs 100 µM for HER2-neu and PDGF receptor kinase).

AG 1478 - CAS 175178-82-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(3-Chloroanilino)-6,7-dimethoxyquinazoline

Primary Target: Epidermal growth factor receptor kinase
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658552
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개요

Replacement Information

주요 사양표

CAS #Empirical Formula
175178-82-2C₁₆H₁₄ClN₃O₂

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658552-5MGCN
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      		 Plastic ampoule 5 mg
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      Description
      OverviewA cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase (IC50 = 3 nM) versus HER2-neu (IC50 >100 µM) and platelet-derived growth factor receptor kinase (IC50 >100 µM). Abolishes MAP kinase (ERK) activation induced by Angiotensin II (Cat. No. 05-23-0101). Also inhibits the activation of EGFR kinase and MAP kinase by 4-hydroxynonenal. Downregulates ARF1 activity and disperses Golgi structure. A 10 mM (1 mg/317 µl) solution of AG 1478 (Cat. No. 658548) in DMSO is also available.
      Catalogue Number658552
      Brand Family Calbiochem®
      Synonyms4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
      References
      ReferencesPan, H., et al. 2008. J. Biol. Chem. 283, In press.
      Liu, W., et al. 1999. J. Cell Sci. 112, 2409.
      Eguchi, S., et al. 1998. J. Biol. Chem. 273, 8890.
      Levitzki, A., and Gazit, A. 1995. Science 267, 1782.
      Fry, D.W., et al. 1994. Science 265, 1093.
      Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047.
      Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.
      Product Information
      CAS number175178-82-2
      ATP CompetitiveY
      DeclarationSold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.
      FormPale yellow solid
      Hill FormulaC₁₆H₁₄ClN₃O₂
      Chemical formulaC₁₆H₁₄ClN₃O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationAG 1478, CAS 175178-82-2, is a cell-permeable, potent, selective, reversible & ATP-competitive inhibitor of EGF receptor kinase (IC50 = 3 nM vs 100 µM for HER2-neu and PDGF receptor kinase).
      Biological Information
      Primary TargetEpidermal growth factor receptor kinase
      Primary Target IC<sub>50</sub>3 nM against epidermal growth factor receptor kinase
      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 (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      카탈로그 번호 GTIN
      658552-5MGCN 07790788052232

      Documentation

      AG 1478 - CAS 175178-82-2 - Calbiochem MSDS

      타이틀

      물질안전보건자료(MSDS) 

      AG 1478 - CAS 175178-82-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      658552

      References

      참고문헌 보기
      Pan, H., et al. 2008. J. Biol. Chem. 283, In press.
      Liu, W., et al. 1999. J. Cell Sci. 112, 2409.
      Eguchi, S., et al. 1998. J. Biol. Chem. 273, 8890.
      Levitzki, A., and Gazit, A. 1995. Science 267, 1782.
      Fry, D.W., et al. 1994. Science 265, 1093.
      Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047.
      Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.

      Citations

      타이틀
    • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
    • Ying-Hong Feng, et al. (2005) Unconventional Homologous Internalization of the Angiotensin II Type-1 Receptor Induced by G-Protein-Independent Signals. Hypertension 46, 419-423.
    • Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.
      		•
      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
      Synonyms4-(3-Chloroanilino)-6,7-dimethoxyquinazoline
      DescriptionA cell-permeable, reversible, ATP-competitive, highly potent and specific inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (IC50 = 3 nM). Much higher concentrations are required for inhibition of the kinase activity of the closely-related HER2 (neu/erb-B2) receptor (IC50 > 100 µM), the platelet-derived growth factor (PDGF) receptor (IC50 > 100 µM), and p210Bcr-Abl (IC50 > 50 µM). Its mechanism of inhibition likely mimics that of the related compound, 4-(3-chloroanilino)quinazoline (CAQ), a competitive inhibitor with respect to ATP. Downregulates ARF1 activity and disperses Golgi structure.
      FormPale yellow solid
      CAS number175178-82-2
      Chemical formulaC₁₆H₁₄ClN₃O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml). Further dilute with aqueous buffers just prior to use.
      Storage Protect from light
      -20°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
      ReferencesPan, H., et al. 2008. J. Biol. Chem. 283, In press.
      Liu, W., et al. 1999. J. Cell Sci. 112, 2409.
      Eguchi, S., et al. 1998. J. Biol. Chem. 273, 8890.
      Levitzki, A., and Gazit, A. 1995. Science 267, 1782.
      Fry, D.W., et al. 1994. Science 265, 1093.
      Osherov, N., and Levitski, A. 1994. Eur. J. Biochem. 225, 1047.
      Ward, W.H., et al. 1994. Biochem. Pharmacol. 48, 659.
      Citation
    • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
    • Ying-Hong Feng, et al. (2005) Unconventional Homologous Internalization of the Angiotensin II Type-1 Receptor Induced by G-Protein-Independent Signals. Hypertension 46, 419-423.
    • Diane Gesty-Palmer, et al. (2005) b-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. Journal of Biological Chemistry 280, 32157-32167.
      		•