[11C]Choline as a PET biomarker for assessment of prostate cancer tumor models

Qi-Huang Zheng, Thomas Gardner, Sudhanshu Raikwar, Chinghai Kao, K. Lee Stone, Tanya D. Martinez, Bruce H. Mock, Xiangshu Fei, Ji Quan Wang, Gary Hutchins

Research output: Contribution to journalArticle

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Abstract

[11C]Choline has been evaluated as a positron emission tomography (PET) biomarker for assessment of established human prostate cancer tumor models. [11C]Choline was prepared by the reaction of [ 11C]methyl triflate with 2-dimethylaminoethanol (DMAE) and isolated and purified by solid-phase extraction (SPE) method in 60-85% yield based on [11C]CO2, 15-20min overall synthesis time from end of bombardment (EOB), 95-99% radiochemical purity and specific activity >0.8Ci/μmol at end of synthesis (EOS). The biodistribution of [ 11C]choline was determined at 30min post iv injection in prostate cancer tumor models C4-2, PC-3, CWR22rv, and LNCaP tumor-bearing athymic mice. The results showed the accumulation of [11C]choline in these tumors was 1.0% dose/g in C4-2 mouse, 0.4% dose/g in PC-3 mice, 3.2% dose/g in CWR22rv mice, and 1.4% dose/g in LNCaP mice; the ratios of tumor/muscle (T/M) and tumor/blood (T/B) were 2.3 (T/M, C4-2), 1.4 (T/M, PC-3), 2.5 (T/M, CWR22rv), 1.2 (T/M, LNCaP) and 2.6 (T/B, C4-2), 2.6 (T/B, PC-3), 7.8 (T/B, CWR22rv), 3.2 (T/B, LNCaP), respectively. The micro-PET imaging of [11C]choline in prostate cancer tumor models was acquired from a C4-2, PC-3, CWR22rv, or LNCaP implanted mouse at 30min post iv injection of 1mCi of the tracer using a dedicated high resolution (<3mm full-width at half-maximum) small FOV (field-of-view) PET imaging system, IndyPET-II scanner, developed in our laboratory, which showed the accumulation of [11C]choline in C4-2, PC-3, CWR22rv, or LNCaP tumor implanted in a nude athymic mouse. The initial dynamic micro-PET imaging data indicated the average T/M ratios were approximately 3.0 (C4-2), 2.1 (PC-3), 3.5 (CWR22rv), and 3.3 (LNCaP), respectively, which showed the tumor accumulation of [11C]choline in all four tumor models is high. These results suggest that there are significant differences in [11C]choline accumulation between these different tumor types, and these differences might offer some useful measure of tumor biological process.

Original languageEnglish
Pages (from-to)2887-2893
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number11
DOIs
StatePublished - Jun 1 2004

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Positron emission tomography
Biomarkers
Choline
Positron-Emission Tomography
Tumors
Prostatic Neoplasms
Neoplasms
Muscle
Blood
Muscles
Nude Mice
Bearings (structural)
Deanol
Biological Phenomena
Imaging techniques

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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[11C]Choline as a PET biomarker for assessment of prostate cancer tumor models. / Zheng, Qi-Huang; Gardner, Thomas; Raikwar, Sudhanshu; Kao, Chinghai; Stone, K. Lee; Martinez, Tanya D.; Mock, Bruce H.; Fei, Xiangshu; Wang, Ji Quan; Hutchins, Gary.

In: Bioorganic and Medicinal Chemistry, Vol. 12, No. 11, 01.06.2004, p. 2887-2893.

Research output: Contribution to journalArticle

Zheng, Qi-Huang ; Gardner, Thomas ; Raikwar, Sudhanshu ; Kao, Chinghai ; Stone, K. Lee ; Martinez, Tanya D. ; Mock, Bruce H. ; Fei, Xiangshu ; Wang, Ji Quan ; Hutchins, Gary. / [11C]Choline as a PET biomarker for assessment of prostate cancer tumor models. In: Bioorganic and Medicinal Chemistry. 2004 ; Vol. 12, No. 11. pp. 2887-2893.
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abstract = "[11C]Choline has been evaluated as a positron emission tomography (PET) biomarker for assessment of established human prostate cancer tumor models. [11C]Choline was prepared by the reaction of [ 11C]methyl triflate with 2-dimethylaminoethanol (DMAE) and isolated and purified by solid-phase extraction (SPE) method in 60-85{\%} yield based on [11C]CO2, 15-20min overall synthesis time from end of bombardment (EOB), 95-99{\%} radiochemical purity and specific activity >0.8Ci/μmol at end of synthesis (EOS). The biodistribution of [ 11C]choline was determined at 30min post iv injection in prostate cancer tumor models C4-2, PC-3, CWR22rv, and LNCaP tumor-bearing athymic mice. The results showed the accumulation of [11C]choline in these tumors was 1.0{\%} dose/g in C4-2 mouse, 0.4{\%} dose/g in PC-3 mice, 3.2{\%} dose/g in CWR22rv mice, and 1.4{\%} dose/g in LNCaP mice; the ratios of tumor/muscle (T/M) and tumor/blood (T/B) were 2.3 (T/M, C4-2), 1.4 (T/M, PC-3), 2.5 (T/M, CWR22rv), 1.2 (T/M, LNCaP) and 2.6 (T/B, C4-2), 2.6 (T/B, PC-3), 7.8 (T/B, CWR22rv), 3.2 (T/B, LNCaP), respectively. The micro-PET imaging of [11C]choline in prostate cancer tumor models was acquired from a C4-2, PC-3, CWR22rv, or LNCaP implanted mouse at 30min post iv injection of 1mCi of the tracer using a dedicated high resolution (<3mm full-width at half-maximum) small FOV (field-of-view) PET imaging system, IndyPET-II scanner, developed in our laboratory, which showed the accumulation of [11C]choline in C4-2, PC-3, CWR22rv, or LNCaP tumor implanted in a nude athymic mouse. The initial dynamic micro-PET imaging data indicated the average T/M ratios were approximately 3.0 (C4-2), 2.1 (PC-3), 3.5 (CWR22rv), and 3.3 (LNCaP), respectively, which showed the tumor accumulation of [11C]choline in all four tumor models is high. These results suggest that there are significant differences in [11C]choline accumulation between these different tumor types, and these differences might offer some useful measure of tumor biological process.",
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T1 - [11C]Choline as a PET biomarker for assessment of prostate cancer tumor models

AU - Zheng, Qi-Huang

AU - Gardner, Thomas

AU - Raikwar, Sudhanshu

AU - Kao, Chinghai

AU - Stone, K. Lee

AU - Martinez, Tanya D.

AU - Mock, Bruce H.

AU - Fei, Xiangshu

AU - Wang, Ji Quan

AU - Hutchins, Gary

PY - 2004/6/1

Y1 - 2004/6/1

N2 - [11C]Choline has been evaluated as a positron emission tomography (PET) biomarker for assessment of established human prostate cancer tumor models. [11C]Choline was prepared by the reaction of [ 11C]methyl triflate with 2-dimethylaminoethanol (DMAE) and isolated and purified by solid-phase extraction (SPE) method in 60-85% yield based on [11C]CO2, 15-20min overall synthesis time from end of bombardment (EOB), 95-99% radiochemical purity and specific activity >0.8Ci/μmol at end of synthesis (EOS). The biodistribution of [ 11C]choline was determined at 30min post iv injection in prostate cancer tumor models C4-2, PC-3, CWR22rv, and LNCaP tumor-bearing athymic mice. The results showed the accumulation of [11C]choline in these tumors was 1.0% dose/g in C4-2 mouse, 0.4% dose/g in PC-3 mice, 3.2% dose/g in CWR22rv mice, and 1.4% dose/g in LNCaP mice; the ratios of tumor/muscle (T/M) and tumor/blood (T/B) were 2.3 (T/M, C4-2), 1.4 (T/M, PC-3), 2.5 (T/M, CWR22rv), 1.2 (T/M, LNCaP) and 2.6 (T/B, C4-2), 2.6 (T/B, PC-3), 7.8 (T/B, CWR22rv), 3.2 (T/B, LNCaP), respectively. The micro-PET imaging of [11C]choline in prostate cancer tumor models was acquired from a C4-2, PC-3, CWR22rv, or LNCaP implanted mouse at 30min post iv injection of 1mCi of the tracer using a dedicated high resolution (<3mm full-width at half-maximum) small FOV (field-of-view) PET imaging system, IndyPET-II scanner, developed in our laboratory, which showed the accumulation of [11C]choline in C4-2, PC-3, CWR22rv, or LNCaP tumor implanted in a nude athymic mouse. The initial dynamic micro-PET imaging data indicated the average T/M ratios were approximately 3.0 (C4-2), 2.1 (PC-3), 3.5 (CWR22rv), and 3.3 (LNCaP), respectively, which showed the tumor accumulation of [11C]choline in all four tumor models is high. These results suggest that there are significant differences in [11C]choline accumulation between these different tumor types, and these differences might offer some useful measure of tumor biological process.

AB - [11C]Choline has been evaluated as a positron emission tomography (PET) biomarker for assessment of established human prostate cancer tumor models. [11C]Choline was prepared by the reaction of [ 11C]methyl triflate with 2-dimethylaminoethanol (DMAE) and isolated and purified by solid-phase extraction (SPE) method in 60-85% yield based on [11C]CO2, 15-20min overall synthesis time from end of bombardment (EOB), 95-99% radiochemical purity and specific activity >0.8Ci/μmol at end of synthesis (EOS). The biodistribution of [ 11C]choline was determined at 30min post iv injection in prostate cancer tumor models C4-2, PC-3, CWR22rv, and LNCaP tumor-bearing athymic mice. The results showed the accumulation of [11C]choline in these tumors was 1.0% dose/g in C4-2 mouse, 0.4% dose/g in PC-3 mice, 3.2% dose/g in CWR22rv mice, and 1.4% dose/g in LNCaP mice; the ratios of tumor/muscle (T/M) and tumor/blood (T/B) were 2.3 (T/M, C4-2), 1.4 (T/M, PC-3), 2.5 (T/M, CWR22rv), 1.2 (T/M, LNCaP) and 2.6 (T/B, C4-2), 2.6 (T/B, PC-3), 7.8 (T/B, CWR22rv), 3.2 (T/B, LNCaP), respectively. The micro-PET imaging of [11C]choline in prostate cancer tumor models was acquired from a C4-2, PC-3, CWR22rv, or LNCaP implanted mouse at 30min post iv injection of 1mCi of the tracer using a dedicated high resolution (<3mm full-width at half-maximum) small FOV (field-of-view) PET imaging system, IndyPET-II scanner, developed in our laboratory, which showed the accumulation of [11C]choline in C4-2, PC-3, CWR22rv, or LNCaP tumor implanted in a nude athymic mouse. The initial dynamic micro-PET imaging data indicated the average T/M ratios were approximately 3.0 (C4-2), 2.1 (PC-3), 3.5 (CWR22rv), and 3.3 (LNCaP), respectively, which showed the tumor accumulation of [11C]choline in all four tumor models is high. These results suggest that there are significant differences in [11C]choline accumulation between these different tumor types, and these differences might offer some useful measure of tumor biological process.

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