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Tyrphostin AG 1478

A Potent EGF Receptor Tyrosine Kinase Inhibitor

Cat #: T-320
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 315.76
    Purity: >99%
    Effective concentration 0.5-50 µM.
    Structure
    Chemical name N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine.
    Molecular formula C16H14ClN3O2.
    CAS No.: 153436-53-4
    Activity Tyrphostin AG 1478 is a reversible, highly potent and selective blocker of EGF receptor tyrosine kinase (IC50 = 3 nM)1. At higher concentrations, it also inhibits KV1.5 K+ channels in an EGF receptor-independent manner (IC50 = 9.8 µM)2.
    References-Activity
    1. Zhu, X.F. et al. (2001) Cancer Lett. 169, 27.
    2. Choi, B.H. et al. (2002) Am. J. Physiol. 282, C1461.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Protect from light.
    Our bioassay
    • Alomone Labs Tyrphostin AG 1478 inhibits EGF receptor activation in 3T3-L1 cells.
      Alomone Labs Tyrphostin AG 1478 inhibits EGF receptor activation in 3T3-L1 cells.
      Cells were serum-starved for 3 h. The cells were then incubated for 2 h with various concentrations of Tyrphostin AG 1478 (#T-320) and stimulated with 200 ng/ml EGF for 10 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-EGFr (upper panel) and with anti-phospho ERK1/2 (lower panel).
    References - Scientific background
    1. Zhu, X.F. et al. (2001) Cancer Lett169, 27.
    2. Kauh, J.S. et al. (2003) Georgetown University Hospital, Washington, DC; Georgetown University, Washington, DC 2003 ASCO annual Meeting Proc Am Soc Clin Oncol 22, 876 (abstr 3520).
    3. Johns, T.G. et al. (2003) Proc. Natl. Acad. Sci. U.S.A. 100, 15871.
    4. Choi, B.H. et al. (2002) Am. J. Physiol. 282, C1461.
    Scientific background

    Tyrphostin AG 1478 (AG 1478) is a reversible, highly potent (IC50 = 3 nM) and selective inhibitor of EGFR tyrosine kinase activity, commonly used as an EGF signaling blocker.1

    AG 1478 inhibits cell proliferation and arrests the cell cycle in tumor cells with overexpression of EGFR.2,3

    AG1478 also directly blocks (IC50 = 9.8 µM) the rat brain KV1.5 K+ channel in vitro in a non-protein-tyrosine-kinase-mediated manner.4

    Last update: 13/10/2022

    Tyrphostin AG 1478 (#T-320) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Product citations
    1. Rayego Mateos, S. et al. (2013) J. Mol. Cell Biol. 5, 323.

    Specifications

    Scientific Background

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