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New Bifunctional Chelator for Cu-64-Immuno-Positron Emission Tomography

New Bifunctional Chelator for Cu-64-Immuno-Positron Emission Tomography
Pandya, DN[Pandya, Darpan N.]Bhatt, N[Bhatt, Nikunj]Dale, AV[Dale, Ajit V.]Kim, JY[Kim, Jung Young]Lee, H[Lee, Hochun]Ha, YS[Ha, Yeong Su]Lee, JE[Lee, Ji-Eun]An, GI[An, Gwang Il]Yoo, J[Yoo, Jeongsoo]
DGIST Authors
Lee, H[Lee, Hochun]
Issued Date
Article Type
1,8-N,N′-Bis-(Carboxymethyl)-4-N″-(4′-Isothiocyanatophenethyl)-1,4,8,11-TetraazacyclotetradecaneAnimalAnimal ExperimentAnimal ModelAnimaliaAnimalsAntibodies, MonoclonalAtomBreast NeoplasmsBreast TumorCarboxylic AcidCell Line, TumorChelating AgentChelating AgentsChemical AnalysisChemistryConjugationControlled StudyCopperCopper 64Copper ComplexCopper RadioisotopesCupric IonCyclic PotentiometryDiagnostic UseDrug SynthesisFemaleFunctional GroupGeometryHeterocyclic Compounds, 1-RingImmunologyIsothiocyanatesIsothiocyanic Acid DerivativeMacrocyclic CompoundMiceMonoclonal AntibodyMouseNitrogenNon-HumanOxygenPentetic AcidPositron-Emission TomographyPositron-Emission Tomography (PET)ProceduresRoom-TemperatureScintiscanningSingle Heterocyclic RingsTetraxetanTrastuzumabTumor Cell LineX Ray Crystallography
A new tetraazamacrocyclic bifunctional chelator, TE2A-Bn-NCS, was synthesized in high overall yield from cyclam. An extra functional group (NCS) was introduced to the N-atom of TE2A for specific conjugation with antibody. The Cu complex of TE2A-Bn-NCS showed high kinetic stability in acidic decomplexation and cyclic voltammetry studies. X-ray structure determination of the Cu-TE2A-Bn-NH2 complex confirmed octahedral geometry, in which copper atom is strongly coordinated by four macrocyclic nitrogens in equatorial positions and two carboxylate oxygen atoms occupy the elongated axial positions. Trastuzumab was conjugated with TE2A-Bn-NCS and then radiolabeled with 64Cu quantitatively at room temperature within 10 min. Biodistribution studies showed that the 64Cu-labeled TE2A-Bn-NCS-trastuzumab conjugates maintain high stability in physiological conditions, and NIH3T6.7 tumors were clearly visualized up to 3 days by 64Cu-immuno-positron emission tomography imaging in animal models. © 2013 American Chemical Society.
American Chemical Society
Related Researcher
  • 이호춘 Lee, Hochun 에너지공학과
  • Research Interests Lithium-ion batteries; Novel Materials for rechargeable batteries; Novel energy conversion;storage systems; Electrochemistry; 리튬이차전지; 이차전지용 신규 전극 및 전해액; 신규 에너지변환 및 저장 시스템; 전기화학
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Department of Energy Science and Engineering Electrochemistry Laboratory for Sustainable Energy(ELSE) 1. Journal Articles


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