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Synthesis and preliminary biodistribution studies of [131I]SIB-PEG4-CHC in tumor-bearing mice
Authors:Xiaobei Zheng  Feng Dong  Jing Yang  Xiaojiang Duan  Tingting Niu  Wangsuo Wu  Jianjun Wang
Affiliation:(1) Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000, China;(2) Department of Nuclear Medicine, Gansu Academy of Medical Sciences, Lanzhou, 730050, China;
Abstract:This work reports the synthesis and preliminary biodistribution results of [131I]SIB-PEG4-CHC in tumor-bearing mice. The tributylstannyl precursor ATE-PEG4-CHC was synthesized by conjugation of ATE to amino pegylated colchicine NH2-PEG4-CHC. [131I]SIB-PEG4-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. [131I]SIB-PEG4-CHC was lipophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [131I]SIB-PEG4-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.
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