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Synthesis and in vitro evaluation of [18F]BMS-754807: a potential PET ligand for IGF-1R.

Majo, Vattoly J; Arango, Victoria; Simpson, Norman R; Prabhakaran, Jaya; Kassir, Suham A; Underwood, Mark D; Bakalian, Mihran; Canoll, Peter; John Mann, J; Dileep Kumar, J S.
Bioorg Med Chem Lett; 23(14): 4191-4, 2013 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-23743281
Radiosynthesis and in vitro evaluation of [(18)F](S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide ([(18)F]BMS-754807 or [(18)F]1) a specific IGF-1R inhibitor was performed. [(18)F]1 demonstrated specific binding in vitro to human cancer tissues. Synthesis of reference standard 1 and corresponding bromo derivative (1a), the precursor for radiolabeling were achieved from 2,4-dichloropyrrolo[2,1-f][1,2,4]triazine (4) in three steps with 50% overall yield. The radioproduct was obtained in 8% yield by reacting 1a with [(18)F]TBAF in DMSO at 170°C at high radiochemical purity and specific activity (1-2Ci/µmol, N=10). The proof of concept of IGF-IR imaging with [(18)F]1 was demonstrated by in vitro autoradiography studies using pathologically identified surgically removed grade IV glioblastoma, breast cancer and pancreatic tumor tissues. These studies indicate that [(18)F]1 can be a potential PET tracer for monitoring IGF-1R.
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