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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
658552
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
175178-82-2C₁₆H₁₄ClN₃O₂

Products

Catalogue NumberPackaging Qty/Pack
658552-5MG Plastic ampoule 5 mg
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
Catalogue Number GTIN
658552-5MG 07790788052232

Documentation

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

Title

Safety Data Sheet (SDS) 

AG 1478 - CAS 175178-82-2 - Calbiochem 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 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.
    		•