期刊
ACS NANO
卷 6, 期 6, 页码 5209-5219出版社
AMER CHEMICAL SOC
DOI: 10.1021/nn300974s
关键词
copper-64 radiolabeling; shell-cross-linked nanoparticles; high specific activity; specific activity amplification; metal-free click chemistry
类别
资金
- Office of Science U.S. Dept. of Energy [ER64671]
- GlaxoSmithKline
- National Heart, Lung and Blood Institute of the National Institutes of Health [HHSN268201000046C]
- Welch Foundation through the W. T. Doherty-Welch Chair in Chemistry [A-0001]
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(l)-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(l) 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/mu mol 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.
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