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PD 153035

A Potent EGF Receptor Tyrosine Kinase Inhibitor

Cat #: P-360
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 360.21
    Purity: >99%
    Effective concentration 10-500 nM.
    Structure
    Chemical name 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline.
    Molecular formula C16H14BrN3O2.
    CAS No.: 153436-54-5
    Activity PD 153035 is a potent inhibitor of the epidermal growth factor receptor (EGFR), (IC50 = 50 pM)1.
    References-Activity
    1. Fry, D. et al. (1994) Science 2665, 1093.
    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 or ethanol. 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.
    Our bioassay
    • Alomone Labs PD 153035 inhibits EGF receptor activation in 3T3-L1 cells.
      Alomone Labs PD 153035 inhibits EGF receptor activation in 3T3-L1 cells.
      Cells were serum starved for 3 h and preincubated with different concentrations of PD 153035 (#P-360) for 2 h. The cells were then stimulated with 200 ng/ml EGF for 10 minutes. 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. Fry, D.W. et al. (1994) Science 265, 1093.
    2. Kunkel, M.W. et al. (1996) Invest. New Drugs 13, 295.
    3. Bridges, A.J. et al. (1996) J. Med. Chem. 39, 267.
    4. Bos, M. et al. (1997) Clin. Cancer Res3, 2099.
    5. Goossens, J.F. et al. (2001) Biochemistry 40, 4663.
    6. Faust, R.A. et al. (1999) Oral Oncol35 290.
    7. Kunkel, M.W. et al. (1996) Invest New Drugs13. 295.
    8. Fredriksson, A. et al. (1999) Life Sci65, 165.
    Scientific background

    PD 153035 is a small molecule derived from brominated anilinoquinazoline which inhibits tyrosine kinase activity of the EGFR by competition at the ATP binding site. PD 153035 is a highly potent inhibitor for auto and hetro tyrosine kinase activity of EGF receptor (ERB2) at sub nM concentrations and inhibits other purified tyrosine kinases only at micromolar or higher concentrations.1-3

    PD 153053 abolished all growth effects mediated by the addition of exogenous EGF in a receptor number-dependent manner and shows a remarkable apoptotic and cytotoxic activity against several types of tumor cell lines that overexpress the EGF receptor in vitro and in vivo .4-8

    Last update: 11/04/2021

    PD 153035 (#P-360) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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