RESUMO
Carbon-14 labeled linker molecule, N-succinimidyl-3-maleimidopropionate was prepared for disposition studies of PEGylated biologics. Our new route started with 100 mCi of carbon-14 labeled Potassium cyanide (KCN) to prepare 55 mCi of [1-(14)C]N-succinimidyl-3-maleimidopropionate, 6 in five steps. This represents a multiple of 5.5× improvement in the yield of the desired labeled product compared with our previous synthesis.
Assuntos
Maleimidas/síntese química , Compostos Radiofarmacêuticos/síntese química , Succinimidas/síntese química , Radioisótopos de Carbono/química , Maleimidas/química , Polietilenoglicóis/química , Compostos Radiofarmacêuticos/química , Succinimidas/químicaRESUMO
Adnectins™ are novel fibronectin-based proteins containing domains engineered to bind to targets of therapeutic interest. The molecular weights of adnectins are less than conventional monoclonal antibodies but larger than traditional small molecules. Until now, there has been no information on the placental transfer of adnectins. To assess placental permeability to adnectins in pregnant guinea pigs, a radiolabeled adnectin, ATI-1072, bound to polyethylene glycol through a [(14) C]Maleimide linker, was synthesized from [1,4-(14) C]Maleic acid. This publication describes the synthesis and analysis of PEG-[(14) C]Maleimide-adnectin ([(14) C]ATI-1072).