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Meeting ReportOncology - Basic: Basic Science

Evaluation of 18F-clofarabine as a PET probe of deoxycytidine kinase in mouse and rat models of glioblastoma

C Wu, P Chan, W Chang, H Wang and R Liu
Journal of Nuclear Medicine May 2009, 50 (supplement 2) 1612;
C Wu
2National Yang-Ming University Medical School, MAGIC/NRPGM, Dept of Nuclear Medicine, Taipei, Taiwan
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P Chan
2National Yang-Ming University Medical School, MAGIC/NRPGM, Dept of Nuclear Medicine, Taipei, Taiwan
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W Chang
2National Yang-Ming University Medical School, MAGIC/NRPGM, Dept of Nuclear Medicine, Taipei, Taiwan
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H Wang
2National Yang-Ming University Medical School, MAGIC/NRPGM, Dept of Nuclear Medicine, Taipei, Taiwan
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R Liu
1Taipei Veterans General Hospital, NPCC, Dept of Nuclear Medicine, Taipei, Taiwan
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Abstract

1612

Objectives Clofarabine, 2-chloro-9-(2-deoxy-2-fluoro-b-arabinofuranosyl)-adenine, a deoxycytidine kinase (dCK) inhibitor, is a next-generation tumor treatment drug. This study aimed to evaluate the fluorinated clofarabine (18F-clo) as a PET probe for assessing dCK activity of glioblastoma.

Methods Starting from benzoate-protected arabinose triflate, 18F-clofarabine was prepared in 3.5 h via a two-step synthesis with high radiochemical purity (≧98%) and acceptable radiochemical yield (10-15%, decay corrected). NOD-SCID mice were inoculated with glioblastoma (GBM) cells in the left thigh or in the brain. F344 rats were inoculated with GBM cells in the brain. The microPET imaging of 18F-clo was performed on day 12 after tumor inoculation.

Results GBM cells exhibited the moderate cell-to-medium (C/M) ratio (21.61) during 2 h incubation compared with other cells. MicroPET imaging showed different tumor contrasts depending on tumor-bearing sites and species. The tumor-to-muscle ratio was only 1.51 in tumor-bearing mice, but the radioactivity retained in the tumor in mouse brain was higher than normal brain to achieve 12.4 of tumor-to-brain ratio due to the low dCK activity in the brain. MicroPET did not detect the tumor growth in the brain of F344 rat.

Conclusions Fluorine-18 labeled clofarabine is successfully prepared via a two-step synthesis. 18F-clo is a promising PET probe for assessing dCK activity of glioblastoma in the mouse model, but not in rat model. 18F-clo seems not to be allowed to pass through blood-brain-barrier in F344 rat.

  • © 2009 by Society of Nuclear Medicine
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Journal of Nuclear Medicine
Vol. 50, Issue supplement 2
May 2009
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Evaluation of 18F-clofarabine as a PET probe of deoxycytidine kinase in mouse and rat models of glioblastoma
C Wu, P Chan, W Chang, H Wang, R Liu
Journal of Nuclear Medicine May 2009, 50 (supplement 2) 1612;

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Evaluation of 18F-clofarabine as a PET probe of deoxycytidine kinase in mouse and rat models of glioblastoma
C Wu, P Chan, W Chang, H Wang, R Liu
Journal of Nuclear Medicine May 2009, 50 (supplement 2) 1612;
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