Overview

  • Product name

    PD 153035, EGFR inhibitor
  • Description

    Highly potent and selective EGFR inhibitor
  • Biological description

    Highly potent and selective EGFR inhibitor (IC50 = 25 pM). Antiproliferative and antitumor effects in vivo.
  • Purity

    > 99%
  • CAS Number

    153436-54-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine
  • Molecular weight

    360.21
  • Molecular formula

    C16H14BrN3O2
  • PubChem identifier

    4705
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in DMSO to 10 mM (with warming)
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC
  • Source

    Synthetic

  • Research areas

Images

  • 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 (ab141839) 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

This product has been referenced in:

  • Swanson CD  et al. Inhibition of epidermal growth factor receptor tyrosine kinase ameliorates collagen-induced arthritis. J Immunol 188:3513-21 (2012). Read more (PubMed: 22393153) »
  • Ge H  et al. Therapeutic and preventive effects of an epidermal growth factor receptor inhibitor on oral squamous cell carcinoma. J Int Med Res 40:455-66 (2012). Read more (PubMed: 22613406) »
  • Bridges AJ  et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem 39:267-76 (1996). Read more (PubMed: 8568816) »

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