PEN-221

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.

C[C@]12[C@@](O1)([C@H](C)[C@@]3(C[C@](O)([C@H](OC)/C=C/C=C(\C)/CC4=CC(N(C)C(=O)C[C@@H]2OC([C@@H](N(C(CCSSC[C@H](NC(=O)[C@H]5NC(=O)[C@]([C@@H](C)O)(NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=6C=7C(NC6)=CC=CC7)NC(=O)[C@H](CC8=CC=C(O)C=C8)NC(=O)[C@@H](NC([C@@H](CC9=CC=CC=C9)N)=O)CSSC5)[H])C(N)=O)=O)C)C)=O)=C(Cl)C(OC)=C4)NC(=O)O3)[H])[H]