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

Citation:
Ibrahim, I. T., M. T. El-Kolaly, M. H. Aboumanei, and A. Abdelbary, "(125)I labeling of clomiphene and biodistribution studies for possible use as a model in breast cancer imaging.", Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine, vol. 115, pp. 37-44, 2016 Sep.

Abstract:

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