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Title: Radiosynthesis of a novel PET fluoronicotinamide for melanoma tumour PET imaging [18F]MEL050
Authors: Greguric, I
Taylor, S
Pham, TQ
Wyatt, NA
Jiang, CD
Bourdier, T
Loc'h, C
Roselt, P
Neels, OC
Katsifis, A
Keywords: Positron computed tomography
Renal clearance
Issue Date: 1-Jan-2011
Publisher: CSIRO Publishing
Citation: Greguric, 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/CH11048
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 Publishing
Gov't Doc #: 5285
ISSN: 0004-9425
Appears in Collections:Journal Articles

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