Radiosynthesis and biological evaluation of [¹⁸F]AG-120 for PET imaging of the mutant isocitrate dehydrogenase 1 in glioma.

ABSTRACT: Glioma are clinically challenging tumors due to their location and invasiveness nature, which often hinder complete surgical resection. The evaluation of the isocitrate dehydrogenase mutation status has become crucial for effective patient stratification. Through a transdisciplinary approach, we have developed an ¹⁸F-labeled ligand for non-invasive assessment of the IDH1R132H variant by using positron emission tomography (PET) imaging. In this study, we have successfully prepared diastereomerically pure [¹⁸F]AG-120 by copper-mediated radiofluorination of the stannyl precursor 6 on a TRACERlab FX2 N radiosynthesis module. In vitro internalization studies demonstrated significantly higher uptake of [¹⁸F]AG-120 in U251 human high-grade glioma cells with stable

SUBMITTER: Lai TH 

PROVIDER: S-EPMC10881675 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature