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

• Published in: Radiochemistry (New York, N.Y.) Vol. 54; no. 5; pp. 497 - 500
• Main Authors: Farouk, N., Ramadan, H. E., El-Amir, M. A.
• Format: Journal Article
• Language: English
• Published: Dordrecht SP MAIK Nauka/Interperiodica 01-09-2012
• Subjects: Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Nuclear Chemistry; catalyst; chromatographic analysis; Isotope exchange; EGFR inhibitor; radiochemical yield
• ISSN: 1066-3622; 1608-3288
• DOI: 10.1134/S1066362212050141

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
125
I-EGFR such as reaction medium, substrate concentration, CuCl concentration, and temperature were examined. Reducing agents such as ascorbic acid, SnCl
2
, and Na
2
S
2
O
5
were used to prevent disproportionation. The radiochemical yield and purity of the labeled product were determined by TLC and HPLC.