Cat. No. 3000

Iressa C22H24ClFN4O3 [184475-35-2]

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Special Conditions

No more than 1 g per individual per year to be sold without prior permission from the license holder.

Alternative 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.

Licensing Information

Sold for research purposes only under agreement from AstraZeneca

Technical Data

Soluble to 100 mM in DMSO and to 10 mM in ethanol
>98 %
Store at RT

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

McKillop et al (2005) Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Mol.Cancer Ther. 4 641. PMID: 15827338.

Baselga et al (2000) ZD1839 ('Iressa'), as an anticancer agent. Drugs 60 (Suppl. 1) 33. PMID: 11129170.

Ciardiello et al (2000) 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. Clin.Cancer Res. 6 2053. PMID: 10815932.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Iressa include:

Kurimoto et al (2016) 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. Oncol Rep 48 1825. PMID: 26984042.

Bill et al (2015) ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer. PLoS One 6 9173. PMID: 25823819.

Curran et al (2015) Architecture of Chimeric Spheroids Controls Drug Transport. Cancer Microenviron 8 101. PMID: 26239082.

Kleczko et al (2015) An Inducible TGF-β2-TGFβR Pathway Modulates the Sensitivity of HNSCC Cells to Tyrosine Kinase Inhibitors Targeting Dominant Receptor Tyrosine Kinases. Life Sci 10 e0123600. PMID: 25946135.

Lindholm et al (2015) Monocyte-Induced Prostate Cancer Cell Invasion is Mediated by Chemokine ligand 2 and Nuclear Factor-κB Activity. J Clin Cell Immunol 6. PMID: 26317041.

Wang et al (2015) Ad-p53 enhances the sensitivity of triple-negative breast cancer MDA-MB-468 cells to the EGFR inhibitor gefitinib. Oncotarget 33 526. PMID: 25501339.

Joannes et al (2014) Fhit regulates EMT targets through an EGFR/Src/ERK/Slug signaling axis in human bronchial cells. J Biol Chem 12 775. PMID: 24464917.

Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. Mol Cancer Res 100 25. PMID: 24496038.

Qawasmi et al (2014) Interactions of ABCG2 (BCRP) with epidermal growth factor receptor kinase inhibitors developed for molecular imaging. Front Pharmacol 5 257. PMID: 25484865.

Kitazono et al (2013) Effect of metformin on residual cells after chemotherapy in a human lung adenocarcinoma cell line. Int J Oncol 43 1846. PMID: 24100792.

McMellen et al (2010) Epidermal growth factor receptor signaling modulates chemokine (CXC) ligand 5 expression and is associated with villus angiogenesis after small bowel resection. Surgery 148 364. PMID: 20471049.

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Keywords: Iressa, supplier, Orally, active, selective, EGFR, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, AstraZeneca, ZD1839, Tocris Bioscience, EGFR Inhibitor products

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