Memorial Sloan Kettering Cancer Center

The City University of New York

Lynn Francesconi

Jason S Lewis

Melissa Deri

Shashikanth Ponnala

Described herein is a chelator for radiolabels (e.g.,Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator forZr 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., the HOPO is an octadentate chelator that stabilizes chelation of radiolabels (e.g.,Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG.and FIG.. Such a bifunctional ligand can eliminate (e.g.,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.

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Bridgewater, NJ, United States of America

Lynn Francesconi