4.7 Article

New cross-bridged cyclam derivative CB-TE1K1P, an improved bifunctional chelator for copper radionuclides

Journal

CHEMICAL COMMUNICATIONS
Volume 50, Issue 1, Pages 43-45

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c3cc45928d

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Funding

  1. NCI [R01CA093375]

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A new cross-bridged cyclam chelator, CB-TE1K1P, was developed for copper-based radiopharmaceuticals, and this chelator can be labelled with Cu-64 under mild conditions in high specific activity. DBCO-PEG(4)-CB- TE1K1P was synthesized for conjugation to proteins, while Dde-CB- TE1K1P(Bu-t(2))-OH was synthesized for solid-phase peptide synthesis. Examples of the conjugation chemistry, radiolabelling and serum stability of each are presented.

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