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EJNMMI Research

Table 1 Comparison of the lipophilicity and the in vitro CXCR4 targeting characteristics of [68Ga]NOTA-pentixafor and [68Ga]pentixafor

From: Preclinical evaluation of [68Ga]NOTA-pentixafor for PET imaging of CXCR4 expression in vivo — a comparison to [68Ga]pentixafor

Compound

logP

IC50 (nM)

Total cellular activity 1 h (%)

Internalized activity 1 h (%)

NOTA-pentixafor

–

253 ± 49

–

–

[68Ga]NOTA-pentixafor

−2.36

17.8 ± 7.7

2.45 ± 0.02

0.43 ± 0.07

Pentixafor

–

102 ± 17

–

–

[68Ga]pentixafor

−2.90

24.8 ± 2.5

6.36 ± 0.46

3.39 ± 0.16

  1. Competitive binding studies (IC50) were carried out using Jurkat T cells and [125I]FC131 as the radioligand. For internalization studies, CXCR4+ Chem-1 cells were used
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