Radio-synthesis, Quality Control and Micro-PET Imaging of 64Cu-DOTA-TATE†

doi:10.7503/cjcu20170520

Abstract

Abstract:

To investigate the potential of ⁶⁴Cu labeled DOTA-[Tyr3]-octreotate(DOTA-TATE) molecular probe in detecting somatostatin receptor(SSTR) positive tumors. The somatostatin analogue DOTA-TATE was radiolabeled with ⁶⁴Cu to prepare ⁶⁴Cu-DOTA-TATE. The stability of the probe was measured in 5%(volume ratio) HSA and 0.9%(volume ratio) saline solutions. After purification, 18.5 MBq of ⁶⁴Cu-DOTA-TATE was injected intravenously to nude mice bearing human pancreatic cancer via tail vein, micro-PET images were taken after radiotracer injection 1 and 10 h. After purification with 80%(volume ratio) ethanol, the radiochemical purity of ⁶⁴Cu-DOTA-TATE was over 99%, and could keep stable for 40 h in 5% HSA and 0.9% saline solutions. As shown in micro-PET imaging, tumor uptake was visualized after post injection 1 h, with the uptake increased after 10 h. ⁶⁴Cu-DOTA-TATE may be useful for imaging somatostatin receptor-positive tumors.

Key words: Somatostatin, 64Cu-DOTA-[Tyr3]-octreotate, Quality control, Neuroendocrine neoplasm

CLC Number:

O629.72
O615

TrendMD:

LIU Fei, XIE Qing, LIU Teli, XU Xiaoxia, GUO Xiaoyi, LI Nan, ZHU Hua, YANG Zhi. Radio-synthesis, Quality Control and Micro-PET Imaging of ⁶⁴Cu-DOTA-TATE^†[J]. Chem. J. Chinese Universities, 2018, 39(4): 695.

Figures/Tables 6

Scheme 1 Radiosynthesis of 64Cu-DOTA-TATE

Fig.1 MOLDI-TOF MS spectra of 64Cu-DOTA-TATE

Fig.2 In vitro stability of 64Cu-DOTA-TATE in 5% HSA(a) and 0.9% NaCl(b) solutions

Fig.3 Blood activity-time profile of 64Cu-DOTA-TATEThe profile of the curve was fitted to a two-compartment model.

Fig.4 Biodistribution of 64Cu-DOTA-TATE in percentage of injected dose per gram of organs after post-injection 1, 4 and 24 h in micea. Blood; b. heart; c. liver; d. spleen; e. kidneys; f. stomach; g. small intestine; h. large intestime; i. muscle; j. brain. Values are mean±standard deviation(n=3).

Fig.5 Micro-PET images of 64Cu-DOTA-TATE in nude mice bearing PANC-1 tumors after post-injection 1, 4 and 10 h(A) and corresponding SUV ratios of tumor to blood and muscle(B)(A) White arrows indicate the tumors. (B) a. SUV(T)/SUV(B); b. SUV(T)/SUV(M).

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Radio-synthesis, Quality Control and Micro-PET Imaging of ⁶⁴Cu-DOTA-TATE^†

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