Preliminary research of preparation of <sup>64</sup>Cu-ATSM and its small animal scanning

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Preliminary research of preparation of ⁶⁴Cu-ATSM and its small animal scanning

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- Preliminary research of preparation of ⁶⁴Cu-ATSM and its small animal scanning
- Vol. 25, Issue 3, Pages: 267-271(2016)
- 作者机构：
  
  1. 上海市质子重离子医院核医学科,上海,201321
  2. 复旦大学附属肿瘤医院核医学科，复旦大学上海医学院肿瘤学系,上海,200032
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Online First：02 November 2016，
  
  Published：02 November 2016
- 稿件说明：
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孙筠,李自立,许晓平,等. ⁶⁴Cu-ATSM乏氧分子影像探针及其荷人乳腺癌小动物PET/CT显像的初步研究[J]. 肿瘤影像学, 2016, 25(3): 267-271
DOI：

孙筠,李自立,许晓平,等. ⁶⁴Cu-ATSM乏氧分子影像探针及其荷人乳腺癌小动物PET/CT显像的初步研究[J]. 肿瘤影像学, 2016, 25(3): 267-271 DOI：

摘要

目的：

64

Cu有半衰期较长、化学反应温和的优势，本研究合成新型乏氧分子影像学探针

64

Cu-ATSM，并与

18

F-氟硝基咪唑(

18

F-fluoromisonidazole，

18

F-FMISO)进行初步比较。

方法：

使用SIEMENS Eclipse HP 11 MeV小型医用回旋加速器系统，Comecer ALCEO EDL、PRF、TADDEO放射性模块和定制铂金靶盘进行

64

Ni电镀、

64

Cu纯化和

64

Cu-ATSM合成。用伽马能谱仪和高效液相色谱(high performance liquid chromatography，HPLC)进行放射核纯度、放化纯度和稳定性检测。在荷人乳腺癌MDB-MA-231模型中进行小动物PET/CT显像并与自制的

18

F-FMISO进行比较。

结果：

实现了

64

Cu-ATSM的自动化生产，产率60%，放射性核纯度＞99%，放化纯度＞95%，标记物稳定性＞6 h。与

18

F-FMISO一样能反映肿瘤乏氧情况，且注射1 h后T/M值即能达5.28。

结论：

成功用11 MeV SIEMENS回旋加速器和Comecer ALCEO模块合成了

64

Cu-ATSM，荷人乳腺癌小动物PET/CT乏氧显像靶/本比高。

Abstract

Objective:

To investigate the synthesis and application of

64

Cu-ATSM in hypoxia imaging of xenografted MDBMA-231 breast cancer.

Methods:

64

CuCl2 was prepared by SIEMENS Eclipse HP 11 MeV cyclotron

Comecer ALCEO EDL

PRF and TADDEO pharmaceutical modules

and the modified platinum target plate. And then the prepared

64

CuCl2 and synthesized

64

Cu-ATSM were mon

itored by energy spectroscopy and high performance liquid chromatography (HPLC) for detection of radioactive purity

radiochemical purity and stability.

64

Cu-ATSM was intravenously injected into MDB-MA-231 cells xenografted nude mouse and then imaged by microPET/CT. The results were compared with that of

18

F-fluoromisonidazole (

18

F-FMISO) injected 4 d after

64

Cu-ATSM imaging.

Results:

The automatic production of

64

Cu-ATSM with a productivity of 60% without radioactive and radiochemical impurity was achieved.

64

Cu-ATSM was stable at 6 h after synthesis. Both

64

Cu-ATSM and

18

F-FMISO could demonstrate the hypoxic degree of MDB-MA-231 cell xenografted tumor. And the tumor/muscle (T/M) ratio of

64

Cu-ATSM was 5.28

which was significantly higher than that of

18

F-FMISO (1.88). Nevertheless

three hours after injection

the T/M ratios of the two probes were similar.

Conclusion:

The synthesized

64

Cu-ATSM could image the hypoxic condition of MDB-MA-231 xenografted tumor.

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