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Table 1 Inhibition constants (Ki in nM) and internalization values (%IA = % internalized activity) of [nat/68Ga]Ga-PSMA-11, [nat/68Ga]Ga-, [nat/44Sc]Sc-, [nat/177Lu]Lu-DOTA-PSMA-617 and [nat/68Ga]Ga-, [nat/44Sc]Sc-, [nat/177Lu]Lu-AAZTA5-PSMA-617

From: 68Ga, 44Sc and 177Lu-labeled AAZTA5-PSMA-617: synthesis, radiolabeling, stability and cell binding compared to DOTA-PSMA-617 analogues

derivative

Ki ± SD

/ nM

 

Internalization ± SD

/ %IA/106 cells

 

[nat/68Ga]Ga-PSMA-11

12.0 ± 2.8

(Eder et al. 2012a)

9.5 ± 2.6

(Benešová et al. 2015)

[nat/68Ga]Ga-PSMA-617

6.4 ± 1.0

(Benešová et al. 2015)

17.7 ± 4.4

(Benešová et al. 2015)

[nat/68Ga]Ga-AAZTA5-PSMA

8.7 ± 0.9

 

13.0 ± 0.2

 

[nat/44Sc]Sc-PSMA-617

4.7 ± 0.8

(Eppard et al. 2017)

15.8 ± 2.1

(Eppard et al. 2017)

[nat/44Sc]Sc-AAZTA5-PSMA

30.6 ± 11.5

 

20.0 ± 0.9

 

[nat/177Lu]Lu-PSMA-617

6.9 ± 1.3

(Benešová et al. 2015)

17.5 ± 3.1

(Benešová et al. 2015)

[nat/177Lu]Lu-AAZTA5-PSMA

26.6 ± 11.1

 

18.0 ± 2.0