Chloramine-T in high-specific-activity radioiodination of antibodies using N-succinimidyl-3-(trimethylstannyl)benzoate as an intermediate.
Monoclonal antibodies C215 and MOv18 have been radiohalogenated, using a single-batch method employing N-succinimidyl-3-(trimethylstannyl)benzoate, m-MeATE. Labelling to the stannyl ester was optimized using chloramine-T as oxidizing agent. The results show that the stannyl ester is effectively labelled with short reaction times giving reproducible yields from 85% to 95%. Subsequent antibody conjugation, 10 to 80 microg MAb, resulted in biologically active, labelled antibodies with overall radiochemical yields of 50% to 80%, with corresponding specific activities of 490-50 kBq(125I)/microg.
Lindegren
S
S
Department of Nuclear Chemistry, Chalmers University of Technology, Sahlgrenska University Hospital, Göteborg, Sweden. sture.lindegren@radfys.gu.se
Skarnemark
G
G
Jacobsson
L
L
Karlsson
B
B
D000906:Antibodies / Q000737:chemistry*; D000911:Antibodies, Monoclonal / Q000737:chemistry / Q000378:metabolism; D000915:Antibody Affinity; D001565:Benzoates / Q000737:chemistry*; D002700:Chloramines / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D007457:Iodine Radioisotopes / Q000737:chemistry*; D009947:Organotin Compounds / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D014105:Tosyl Compounds / Q000737:chemistry*; D014298:Trimethyltin Compounds / Q000737:chemistry*; D014407:Tumor Cells, Cultured / Q000276:immunology
D000906:Antibodies; D000911:Antibodies, Monoclonal; D001565:Benzoates; D002700:Chloramines; D007457:Iodine Radioisotopes; D009947:Organotin Compounds; D019275:Radiopharmaceuticals; D014105:Tosyl Compounds; D014298:Trimethyltin Compounds; C016300:chloramine-T; C061345:N-succinimidyl 3-(trimethylstannyl)benzoate