Fluorine-18 Labeling of the MDM2 Inhibitor RG7388 for PET Imaging: Chemistry and Preliminary Evaluation.

ABSTRACT: RG7388 (Idasanutlin) is a potent inhibitor of oncoprotein murine double minute 2 (MDM2). Herein we investigated the feasibility of developing ¹⁸F-labeled RG7388 as a radiotracer for imaging MDM2 expression in tumors with positron emission tomography (PET). Two fluorinated analogues of RG7388, 6 and 7, were synthesized by attaching a fluoronicotinyl moiety to RG7388 via a polyethylene glycol (PEG₃) or a propyl linker. The inhibitory potency (IC₅₀) of 6 and 7 against MDM2 was determined by a fluorescence polarization (FP)-based assay. Next, compound 6 was labeled with ¹⁸F using a trimethylammonium triflate precursor to obtain [¹⁸F]FN-PEG₃-RG7388 ([¹⁸F]6), and its properties

SUBMITTER: Zhou Z 

PROVIDER: S-EPMC8775362 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature