biostudies-literatureBeinat CNIH NINDS Research Education GrantBen and Catherine Ivy FoundationNINDS NIH HHSNCI NIH HHSNIH NCI6467-6478https://www.ebi.ac.uk/biostudies/studies/S-EPMC8639752biostudies-literatureUnknown27(23)<h4>Purpose</h4>Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[¹⁸F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([¹⁸F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM.<h4>Experimental design</h4>[¹⁸F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [¹⁸F]DASA-23 in GBM cell culture and human GBM xenografts implanted Clinical cancer research : an official journal of the American Association for Cancer ResearchA Clinical PET Imaging Tracer ([¹⁸F]DASA-23) to Monitor Pyruvate Kinase M2-Induced Glycolytic Reprogramming in Glioblastoma.PMC8639752R01 CA216054–01R01 CA2160545R25NS065741–07R25 NS065741F30 CA228215F30CA228215Murty SLiu DDGranucci MRecht LDMassoud TFShen BJames MLGandhi HHe JQHalbert KWarnock GIDavidzon GThomas RBeinat CPatel CBHayden-Gephart MJohnson EGambhir SSCastillo JBWeissman IUchida NChu PPark JHHaywood TBuccino PBorn DENagpal SHolley DPhillips MNaya LSinha RKoran MEIIagaru AReyes STKhalighi MAlam ISfalseA Clinical PET Imaging Tracer ([¹⁸F]DASA-23) to Monitor Pyruvate Kinase M2-Induced Glycolytic Reprogramming in Glioblastoma.<h4>Purpose</h4>Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[¹⁸F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([¹⁸F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM.<h4>Experimental design</h4>[¹⁸F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [¹⁸F]DASA-23 in GBM cell culture and human GBM xenografts implanted 2021-01-01T00:00:00Z2021 Dec2026-05-09T20:13:43.802Z2025-02-19T00:56:33.785ZS-EPMC86397523447510110.1158/1078-0432.CCR-21-054410.1158/1078-0432.ccr-21-0544