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Table 1 Affinities (IC50) of different Cu2+-labeled pentixafor derivatives, [natCu]NOTA, [natCu]NODAGA-pentixather, and the corresponding metal-free precursors to human CXCR4. FC131 and [68Ga]pentixafor are included as reference compounds. Competitive binding studies were carried out using Jurkat T-cell leukemia cells (400.000 cells/sample) and [125I]FC131 as the radioligand

From: [64Cu]NOTA-pentixather enables high resolution PET imaging of CXCR4 expression in a preclinical lymphoma model

Compound

IC50 [nM]

FC131

9.9 ± 2.4a

[natGa]pentixafor (DOTA)

24.8 ± 2.5a

[natCu]DOTAGA-pentixafor

1165 ± 220a

[natCu]NOTA-pentixafor

46.1 ± 26a

[natCu]NODAGA-pentixafor

343 ± 10a

[natCu]DTPA-pentixafor

175 ± 66a

NOTA-pentixather

27.5 ± 2.1

[natCu]NOTA-pentixather

14.9 ± 2.1

NODAGA-pentixather

64.9 ± 6.5

[natCu]NODAGA-pentixather

47.5 ± 1.8

  1. aref (Poschenrieder et al. 2016b)
  2. Data are means ± SD from a minimum of three separate determinations