An ideal positron emission tomography (PET) tracer should be highly extractable by the tumor tissue or organ that contains low toxicity and can provide high‐resolution images in vivo. In this work, the aim was to evaluate the application of Al18F‐labeled 1,4,7‐triazacyclononane‐1,4,7‐triacetic acid containing sulfonamide group (18F‐Al‐NOTA‐SN) as a potential tumor‐targeting signal‐enhanced radioactive tracer in PET. SN as a tumor‐targeting group was incorporated to NOTA to make a ligand. Subsequently, this ligand reacted with Na18F and AlCl3 to produce a compound 18F‐Al‐NOTA‐SN. This compound was further characterized and its property in regard to cell cytotoxicity assay, microPET imaging, biodistribution, cell uptake assay, and tumor selectivity in vitro and in vivo, was also investigated. 18F‐Al‐NOTA‐SN possessed low cell cytotoxicity and uptake to COS‐7 and 293T healthy cells and high cell cytotoxicity and uptake to MDA‐MB‐231, HepG2, and HeLa tumor cells in vitro. Moreover, 18F‐Al‐NOTA‐SN showed good tumor‐targeting property and high PET signal enhancement of HeLa tumors, liver, and kidneys in mice, as well as the uptake ratios of tumor to blood and tumor to muscle, were 4.98 and 3.87, respectively. 18F‐Al‐NOTA‐SN can be accepted to be kidney and liver eliminated earlier and show a potential tumor‐targeting signal‐enhanced radioactive tracer in PET.

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