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<p>To evaluate the suitability of <sup>47</sup>Sc for SPECT imaging and therapeutic effect, a fibroblast activation protein (FAP) inhibitor FAPI-46 was used for cancer theranostics in preclinical setting. <sup>47</sup>Sc was successfully produced via thermal neutron irradiation of <sup>46</sup>Ca 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 <sup>47</sup>Sc-FAPI-46. Biodistribution and SPECT/CT imaging indicated specific uptake of <sup>47</sup>Sc-FAPI-46 in PANC-2 pancreatic tumors. Therapeutic experiments revealed an effective anti-tumor ability with negligible toxicity of <sup>47</sup>Sc-FAPI-46 in xenografted tumor mice.</p>

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

  • 期刊论文

  • 发表日期：

    2025年7月31日

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

摘要

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.