125I labeling of clomiphene and biodistribution studies for possible use as a model in breast cancer imaging

Clomiphene has growth-inhibitory effects of breast cancer cells, clomiphene was successfully labeled with 125I via direct electrophilic substitution reaction with labeling yield 97%. It was obtained at optimum substrate amount of 0.5 mg, Chloramine-T was used as an oxidizing agent at optimum amount of 25 µg. Labeling reactions was done at pH 5 at ambient temperature. This study showed good in vitro and in vivo stability of the 125I-clomiphene. The radiolabeled compound showed high ascetic fluid uptake of 18.12±0.27% at 30 min post-injection. Solid tumor uptake of 125I-clomiphene was 12.48±0.32% at 30 min post-injection. This data revealed the localization of tracer in tumor tissue with high percent sufficient to use 125I-clomiphene as a promising tool for the diagnosis of breast cancer.