Iressa

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Cat.No. 3000 - Iressa | C22H24ClFN4O3 | CAS No. 184475-35-2
Description: Orally active, selective EGFR inhibitor
Alternative Names: Gefitinib, ZD 1839
Chemical Name: N-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
Purity: ≥98% (HPLC)
Datasheet
Citations (11)
Literature

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

Compound Libraries

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.

Technical Data

M. Wt 446.9
Formula C22H24ClFN4O3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 184475-35-2
PubChem ID 123631
InChI Key XGALLCVXEZPNRQ-UHFFFAOYSA-N
Smiles FC(C=C3)=C(Cl)C=C3NC2=NC=NC1=CC(OC)=C(OCCCN4CCOCC4)C=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.69 100
ethanol 4.47 10

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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.

View Related Products by Product Action

View all EGFR Inhibitors

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:

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

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


Do you know of a great paper that uses Iressa from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Schizophrenia

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster highlights the targets and pathways representing the most promising strategies to pursue for novel drug development.

Pathways for Iressa

Protocols

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