abstract |
Described herein is a chelator for radiolabels (e.g., 89 Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator for 89 Zr is the ligand, 3,4,3-(LI-1,2-HOPO) (“HOPO”), which exhibits equal or superior stability compared to DFO in chemical and biological assays across a period of several days in vivo. As shown in FIG. 1 , the HOPO is an octadentate chelator that stabilizes chelation of radiolabels (e.g., 89 Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG. 4 and FIG. 5 . Such a bifunctional ligand can eliminate (e.g., 89 Zr) loss from the chelate in vivo and reduce uptake in bone and non-target tissue. Therefore, the bifunctional HOPO ligand can facilitate safer and improved PET imaging with radiolabeled antibodies. |