64Cu core-labeled nanoparticles with high specific activity via metal-free click chemistry

Dexing Zeng, Nam S. Lee, Yongjian Liu, Dong Zhou, Carmen S. Dence, Karen L. Wooley, John A. Katzenellenbogen, Michael J. Welch

Research output: Contribution to journalArticlepeer-review


Figure Persented: A novel strategy based on metal-free "click" chemistry was developed for the copper-64 radiolabeling of the core in shell-cross-linked nanoparticles (SCK-NPs). Compared with Cu(I)-catalyzed click chemistry, this metal-free strategy provides the following advantages for Cu-64 labeling of the core of SCK-NPs: (1) elimination of copper exchange between nonradioactive Cu in the catalyst and DOTA-chelated Cu-64; (2) elimination of the internal click reactions between the azide and acetylene groups in the same NPs; and (3) increased efficiency of the click reaction because water-soluble Cu(I) does not need to reach the hydrophobic core of the NPs. When 50 mCi Cu-64 was used for the radiolabeling, the specific activity of the radiolabeled product was 975 Ci/μmol at the end of synthesis, which represents the attachment of ca. 500 Cu-64 atoms per SCK-NP, giving in essence a 500-fold amplification of specific activity of the NP over that of the Cu-64 chelate. To the best of our knowledge, this is the highest specific activity obtained for Cu-64-labeled nanoparticles.

Original languageEnglish (US)
Pages (from-to)5209-5219
Number of pages11
JournalACS Nano
Issue number6
StatePublished - Jun 26 2012


  • copper-64 radiolabeling
  • high specific activity
  • metal-free click chemistry
  • shell-cross-linked nanoparticles
  • specific activity amplification

ASJC Scopus subject areas

  • General Materials Science
  • General Engineering
  • General Physics and Astronomy


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