Catalog Number: 3000
Alternate Names: Gefitinib, ZD 1839
Chemical Name: N-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
Biological Activity
Orally active, selective inhibitor of EGFR tyrosine kinase (IC50 = 23 - 79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes only under agreement from AstraZeneca
Other Product-Specific Information:
Background References
  1. ZD1839 ('Iressa'), as an anticancer agent.
    Baselga et al.
    Drugs, 2000;60:33
  2. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor.
    Ciardiello et al.
    Clin.Cancer Res., 2000;6:2053
  3. Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor.
    McKillop et al.
    Mol.Cancer Ther., 2005;4:641

The citations listed below are publications that use Tocris products. Selected citations for Iressa include:

Showing Results 1 - 10 of 11

  1. Drug resistance originating from a TGF-β/FGF-2-driven epithelial-to-mesenchymal transition and its reversion in human lung adenocarcinoma cell lines harboring an EGFR mutation.
    Authors: Kurimoto Et al.
    Oncol Rep
  2. Architecture of Chimeric Spheroids Controls Drug Transport.
    Authors: Curran Et al.
    Cancer Microenviron
  3. ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer.
    Authors: Bill Et al.
    PLoS One
  4. Monocyte-Induced Prostate Cancer Cell Invasion is Mediated by Chemokine ligand 2 and Nuclear Factor-κB Activity.
    Authors: Lindholm Et al.
    J Clin Cell Immunol
  5. Ad-p53 enhances the sensitivity of triple-negative breast cancer MDA-MB-468 cells to the EGFR inhibitor gefitinib.
    Authors: Wang Et al.
  6. An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases.
    Authors: Kleczko Et al.
    Life Sci
  7. Interactions of ABCG2 (BCRP) with epidermal growth factor receptor kinase inhibitors developed for molecular imaging.
    Authors: Qawasmi Et al.
    Front Pharmacol
  8. Fhit regulates EMT targets through an EGFR/Src/ERK/Slug signaling axis in human bronchial cells.
    Authors: Joannes Et al.
    J Biol Chem
  9. SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner.
    Authors: Moody Et al.
    Mol Cancer Res
  10. Effect of metformin on residual cells after chemotherapy in a human lung adenocarcinoma cell line.
    Authors: Kitazono Et al.
    Int J Oncol
  11. Epidermal growth factor receptor signaling modulates chemokine (CXC) ligand 5 expression and is associated with villus angiogenesis after small bowel resection.
    Authors: McMellen Et al.
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