Labeling of EGFR inhibitor to prepare a potential SPECT agent for molecular imaging of breast cancer via iodine-bromine exchange

Abstract

A simple method was developed for labeling N-{4-[(3-chloro-4-fluorophenyl)amino]quinazolin-6-yl}-3-bromopropionamide, an EGFR inhibitor, with radioactive iodine via nucleophilic iododebromination. The factors affecting the radiochemical yield of 125I-EGFR such as reaction medium, substrate concentration, CuCl concentration, and temperature were examined. Reducing agents such as ascorbic acid, SnCl2, and Na2S2O5 were used to prevent disproportionation. The radiochemical yield and purity of the labeled product were determined by TLC and HPLC.