Synthesis and preliminary biodistribution studies of [~(131)I]SIB- PEG_4-CHC in tumor-bearing mice

摘要

This work reports the synthesis and preliminary biodistribution results of [~(131)I]SIB-PEG_4-CHC in tumor-bearing mice. The tributylstannyl precursor ATE-PEG_4-CHC was synthesized by conjugation of ATE to amino pegylated colchicine NH_2-PEG_4-CHC. [ 131I]SIB-PEG_4-CHC was radiosynthesized by electrophilic destannylation of the precursor with a yield of ~44%. The radiochemical purity (RCP) appeared to be >95% by a Sep-Pak cartridge purification. [ ~(131)I]SIB-PEG_4-CHC was lipophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [ ~(131)I]SIB-PEG_4-CHC cleared from background rapidly, and didn't deiodinate in vivo. However, the poor tumor localization excluded it from further investigations as a tumor-targeted radiopharmaceuticals.