[tyr3]octreotate

[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.

Tyr3-Octreotate acetate is a somatostatin analogue with a high tumor uptake rate that can be labeled with radioactive metals, thus exhibiting antitumor activity. It is utilized in the synthesis and study of radiolabeled conjugate drugs (RDC).

PEN-221 is a Somatostatin receptor 2 (SSTR2)-targeting cytotoxic conjugate with an IC50 of 10 nM. PEN-221 is a conjugate consisting of microtubule-targeting agent DM1 linked to the C-terminal side chain of Tyr3-octreotate.