Development and Preliminary Evaluations of a Novel 18F-Labeled Tracer for Detection of BRAFV600E Mutant Status in Animal Models of Melanoma.

Abstract excerpt

The BRAFV600E mutation is a well-established oncogenic driver, and several oral inhibitors have achieved clinical success. However, radiolabeled tracers for the non-invasive imaging of this mutation remain limited. N-(2-Chloro-3-((3,5-dimethyl-4-oxo-3,4-dihydroquinazolin-6-yl)oxy)-5-fluorophenyl)propane-1-sulfonamide (74) is a novel oral inhibitor targeting BRAFV600E with high inhibitory potency. Here, we report...

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