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

658552
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₆H₁₄ClN₃O₂175178-82-2

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      658552-5MG
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          658552

          References

          Reference overview
          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

          Title
        • 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 -20°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
          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.