MEMORIAL SLOAN KETTERING CANCER CENTER;RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
发明人:
LEWIS, JASON S.,DERI, MELISSA,FRANCESCONI, LYNN,PONNALA, SHASHIKANTH
申请号：
CA2998420
公开号：
CA2998420A1
申请日:
2016.09.09
申请国别(地区):
CA
年份:
2017
代理人:
摘要：
Described herein is a chelator for radiolabels (e.g., 89Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator for 89Zr 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., 89Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG. 4 and FIG. 5. Such a bifunctional ligand can eliminate (e.g., 89Zr) 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.
