同位素2024，Vol.37Issue(2)：97-105,9.DOI:10.7538/tws.2024.37.02.0097
FAPα靶向标记化合物131I-FAPI-03的合成及初步体内外实验研究
Synthesis and Preliminary Evaluation of FAPα Targeted Tracer 131I-FAPI-03
摘要
Abstract
Using N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine)as scaffold,we prolonged the linker with serine to obtain a FAPI derivative ATE-FAPI-03,which was subsequently labeled with 131I by electrophilic substitution.Then the in vitro stability,Log P value,binding affinity,targeting properties and biodistribution behavior of 131I-FAPI-03 was evaluated.Results show that 131I-FAPI-03 was lipophilic and stable in vitro,capable of specifically binding to FAPα-positive U87MG cells fast with a major proportion trapped intracellularly.After 10 min of incubation,131I-FAPI-03 showed a specific binding rate of(22.00±0.35)%,and the binding rate increased with the incubation time,to a peak of(37.5±0.83)%at 180 min.However,the FAPα-negative MCF-7 cells exhibited very low uptake of 131I-FAPI-03 at any time point.The IC50 measured by the competition assay indicated significant binding property of 131I-FAPI-03.Biodistribution studies revealed that 131I-FAPI-03 could rapidly accumulate in tumor sites with an uptake of(14.90±3.21)%ID/g at 5 min post injection.At 2 h post injection,131I-FAPI-03 displayed the highest tumor-to-muscle ratio of 43.7±16.7.All above results provided important reference for the development of novel FAPα-targeting tracers.关键词
FAPα/131I/FAPI/胶质瘤Key words
FAPα/131I/FAPI/glioma分类
能源科技引用本文复制引用
马欢,廖家莉,杨远友,刘宁,李飞泽..FAPα靶向标记化合物131I-FAPI-03的合成及初步体内外实验研究[J].同位素,2024,37(2):97-105,9.基金项目
中央高校基本科研业务费专项资金资助(2023SCU12132) （2023SCU12132）
四川省医学科学院.四川省人民医院青年人才基金(2022QN32) （2022QN32）
