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.
Sold for research purposes only under agreement from AstraZeneca
Iressa is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 446.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.24 mL||11.19 mL||22.38 mL|
|5 mM||0.45 mL||2.24 mL||4.48 mL|
|10 mM||0.22 mL||1.12 mL||2.24 mL|
|50 mM||0.04 mL||0.22 mL||0.45 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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
Baselga et al (2000) ZD1839 ('Iressa'), as an anticancer agent. Drugs 60 33 PMID: 11129170
McKillop et al (2005) Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor. Mol.Cancer Ther. 4 641 PMID: 15827338
If you know of a relevant reference for Iressa, please let us know.
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Keywords: Orally active selective EGFR inhibitors inhibits Epidermal Growth Factors Receptors ErbB Her Receptor Tyrosine Kinases RTKs AstraZeneca ZD1839 chemotherapeutics Gefitinib ZD 1839 EGFR
11 Citations for Iressa
Citations are publications that use Tocris products. Selected citations for Iressa include:
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
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
Curran et al (2015) Architecture of Chimeric Spheroids Controls Drug Transport. Cancer Microenviron 8 101 PMID: 26239082
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
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
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
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
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
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
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
Do you know of a great paper that uses Iressa from Tocris? If so please let us know.