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[68Ga]Ga-DATA5m.SA.FAPi is a radiopharmaceutical diagnostic agent developed for positron emission tomography (PET) imaging of the tumor microenvironment. It specifically targets Fibroblast Activation Protein (FAP), an enzyme highly overexpressed on cancer-associated fibroblasts (CAFs) in the stroma of most epithelial tumors. The molecule features a DATA5m (6-pentanoic acid-6-amino-1,4-diazepane-triacetate) chelator, which is a hybrid ligand that allows for rapid and efficient labeling with Gallium-68 at room temperature, facilitating a kit-like preparation process in clinical settings. The squaric acid (SA) moiety acts as a linker between the chelator and the FAP-targeting ligand. This tracer is designed to overcome the heating requirements of traditional DOTA-based FAP inhibitors, potentially improving the accessibility and ease of use for FAP-targeted imaging in oncology.
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