Synthesis and Evaluation of a ¹⁸F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET.

ABSTRACT: Mutations in the isocitrate dehydrogenase gene 1 (IDH1) are common in gliomas. Studies suggest that IDH1 mutations are early events in glioma formation and are important drivers of malignant progression. Herein, we report the synthesis and evaluation of a ¹⁸F-labeled triazinediamine analogue, [¹⁸F]1, as a candidate radiotracer for noninvasive imaging of IDH1 mutations in gliomas by positron emission tomography (PET). In vitro studies revealed good binding inhibition potency and binding affinity for [¹⁸F]1 in IDH1 mutant glioma cell lines, with a half-maximal inhibitory concentration value (IC₅₀) of 54 nM and an equilibrium dissociation constant (K_d) of 40 nM. In vivo studies using mutant IDH1 glioma x

SUBMITTER: Chitneni SK 

PROVIDER: S-EPMC6047021 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature