Xiu Luo, Zhe Zhang, Chao Cheng, Tao Wang, Danzhou Fang, Changjing Zuo, Gengbiao Yuan, Rou Li, Xiao Li
The so-far used Ga-68- or F-18-labelled tracers are of a relative short time window in differentiating tumor fibrosis. SPECT applicable imaging probe, 99m Tc-HYNIC-FAPI-04, was synthesized and evaluated in tumor cells and animal models of FAP-positive glioma and FAP-negative hepatoma, and then compared with 18 F-FDG or 68 Ga-FAPI-04 PET/CT. The radio-labeling rate of 99m Tc-HYNIC-FAPI-04 was greater than 90%, and the radiochemical purity was >99% after purification with sep-pak C18 column. In vitro cell uptake experiments of 99m Tc-HYNIC-FAPI-04 showed good FAP binding specificity, and the cellular uptake significantly decreased when blocked by DOTA-FAPI-04, reflecting the similar targeting mechanism of HYNIC-FAPI-04 and DOTA-FAPI-04...
March 10, 2023: Pharmaceuticals