Radiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050

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dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorTaylor, Sen_AU
dc.contributor.authorPham, TQen_AU
dc.contributor.authorWyatt, NAen_AU
dc.contributor.authorJiang, CDen_AU
dc.contributor.authorBourdier, Ten_AU
dc.contributor.authorLoc'h, Cen_AU
dc.contributor.authorRoselt, Pen_AU
dc.contributor.authorNeels, OCen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.date.accessioned2013-12-03T00:36:06Zen_AU
dc.date.available2013-12-03T00:36:06Zen_AU
dc.date.issued2011-01-01en_AU
dc.date.statistics2013-12-03en_AU
dc.description.abstract[18F]6-Fluoro-N-[2-(diethylamino)ethyl]nicotinamide [18F]MEL050 is a novel nicotinamide-based radiotracer, designed to target random metastatic dissemination of melanoma tumours by targeting melanin. Preclinical studies suggest that [18F]MEL050 has an excellent potential to improve diagnosis and staging of melanoma. Here we report the radiochemical optimization conditions of [18F]MEL050 and its large scale automated synthesis using a GE FXFN automated radiosynthesis module for clinical, phase-1 investigation. [18F]MEL050 was prepared via a one-step synthesis using no-carrier added K[18F]F-Krytpofix® 222 (DMSO, 170°C, 5 min) followed by HPLC purification. Using 6-chloro-N-[2-(diethylamino)ethyl]nicotinamide as precursor, [18F]MEL050 was obtained in 40–46% radiochemical yield (non-decay corrected), in greater than 99.9% radiochemical purity and specific activity ranging from 240 to 325 GBq μmol–1. Total synthesis time including formulation was 40 min and [18F]MEL050 was stable (99.8%) in PBS for 6 h. © 2011, CSIRO Publishingen_AU
dc.description.sponsorshipWe thank the Commonwealth Government of Australia for their financial support to the Collaborative Research Centre for Biomedical Imaging Development.en_AU
dc.identifier.citationGreguric, I., Taylor, S., Pham, T., Wyatt, N., Jiang, C. D., Bourdier, T., Loc'h, C., Roselt, P., Neels, O. C., & Katsifis, A. (2011). Radiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050. Australian Journal of Chemistry, 64 (7), 873-879. doi:10.1071/CH11048en_AU
dc.identifier.govdoc5285en_AU
dc.identifier.issn0004-9425en_AU
dc.identifier.issue7en_AU
dc.identifier.journaltitleAustralian Journal of Chemistryen_AU
dc.identifier.pagination873-879en_AU
dc.identifier.urihttp://dx.doi.org/10.1071/CH11048en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/5058en_AU
dc.identifier.volume64en_AU
dc.language.isoenen_AU
dc.publisherCSIRO Publishingen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectMetastasesen_AU
dc.subjectMelanomasen_AU
dc.subjectSynthesisen_AU
dc.subjectRenal clearanceen_AU
dc.subjectTherapyen_AU
dc.titleRadiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050en_AU
dc.typeJournal Articleen_AU
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