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[Tyr3]Octreotate is a long peptide compound containing 8 amino acids and is a functional DOTA chelating agent with covalent bonds. [Tyr3]Octreotate binds to transmembrane receptors of SSR2-active NETs and is actively transported into cells by endocytosis, which may increase the required double-stranded DNA breaks and is a potential drug for tumor treatment.