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Bioorg Med Chem Lett. 2006 Aug 1;16(15):4102-6. Epub 2006 May 11.

Synthesis of [11C]Iressa as a new potential PET cancer imaging agent for epidermal growth factor receptor tyrosine kinase.

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  • 1Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.


Iressa (Gefitinib) is an orally active inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TK) involved in cell signal transduction processes critical to proliferation, apoptosis, repair, and angiogenesis of cancer cells. [11C]Iressa was first designed and synthesized as a new potential positron emission tomography (PET) cancer imaging agent for EGFR-TK in 30-40% radiochemical yield with 4.0-6.0 Ci/micromol specific activity at end of bombardment (EOB).

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