47sc标记FAPI-46的合成及初步评价

IF 1.6 3区化学 Q3 CHEMISTRY, ANALYTICAL

Journal of Radioanalytical and Nuclear Chemistry Pub Date : 2025-07-31 DOI:10.1007/s10967-025-10281-1

Dongping Su, Yuhao Liao, Jieru Wang, Ruomeng Liu, Huawei Cai, Xiaojie Yin, Zhi Qin, Jinsong Zhang, Zeen Yao, Bo Li

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引用次数: 0

摘要

为了评估47Sc在SPECT成像中的适用性和治疗效果，在临床前将成纤维细胞活化蛋白（FAP）抑制剂FAPI-46用于癌症治疗。47Sc通过46Ca的热中子辐照制备成功，然后与FAPI-46偶联，获得了超过98%的高放射化学纯度。体外实验证实了FAP介导47Sc-FAPI-46与MG-63细胞特异性结合。生物分布和SPECT/CT成像显示PANC-2胰腺肿瘤中47Sc-FAPI-46的特异性摄取。治疗实验显示47Sc-FAPI-46对异种移植瘤小鼠具有有效的抗肿瘤能力，毒性可忽略不计。

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Synthesis and preliminary evaluation of 47Sc-labeled FAPI-46 for cancer theranostics

To evaluate the suitability of ⁴⁷Sc for SPECT imaging and therapeutic effect, a fibroblast activation protein (FAP) inhibitor FAPI-46 was used for cancer theranostics in preclinical setting. ⁴⁷Sc was successfully produced via thermal neutron irradiation of ⁴⁶Ca and then conjugated with FAPI-46, achieving a high radiochemical purity over 98%. In vitro experiments confirmed the FAP mediated specific binding to MG-63 cells for ⁴⁷Sc-FAPI-46. Biodistribution and SPECT/CT imaging indicated specific uptake of ⁴⁷Sc-FAPI-46 in PANC-2 pancreatic tumors. Therapeutic experiments revealed an effective anti-tumor ability with negligible toxicity of ⁴⁷Sc-FAPI-46 in xenografted tumor mice.

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来源期刊

Journal of Radioanalytical and Nuclear Chemistry 化学-分析化学

CiteScore

2.80

自引率

18.80%

发文量

504

审稿时长

2.2 months

期刊介绍： An international periodical publishing original papers, letters, review papers and short communications on nuclear chemistry. The subjects covered include: Nuclear chemistry, Radiochemistry, Radiation chemistry, Radiobiological chemistry, Environmental radiochemistry, Production and control of radioisotopes and labelled compounds, Nuclear power plant chemistry, Nuclear fuel chemistry, Radioanalytical chemistry, Radiation detection and measurement, Nuclear instrumentation and automation, etc.