Tumor PET imaging agent <68>Ga-NOTA-ADG and preparation method and application thereof

A PET imaging agent, 68ga-nota-adg technology, applied in the field of tumor PET imaging agent 68Ga-NOTA-ADG and its preparation, can solve the problems of huge cost and initial investment, and achieve high radiochemical purity and short synthesis time Short, simple and fast preparation method

Pending Publication Date: 2021-12-31
ZHONGSHAN HOSPITAL FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the production of F-18 nuclides requires a positron cyclotron and advanced shielding fields, and the cost and initial investment are huge, reaching millions of dollars

Method used

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  • Tumor PET imaging agent &lt;68&gt;Ga-NOTA-ADG and preparation method and application thereof
  • Tumor PET imaging agent &lt;68&gt;Ga-NOTA-ADG and preparation method and application thereof
  • Tumor PET imaging agent &lt;68&gt;Ga-NOTA-ADG and preparation method and application thereof

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Experimental program
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Embodiment 1

[0031] Synthesis of precursor NOTA-Amino-DG:

[0032] To a solution (1 mL) of 2-amino-2-deoxy-D-glucose (10 mg, 46.4 μmol, 4.3 equiv) and HEPES sodium salt (30 mg, 115 μmol) was added p-SCN-Bn-NOTA 3HCl ( 6 mg, 10.7 μmol, 1.0 equiv). The solution was incubated at room temperature for 10 h and then stored at -20 °C for use, the reaction formula is as follows:

[0033]

[0034] Target compound PET probe 68 Synthesis of Ga-NOTA-ADG:

[0035] 50 μl of precursor solution was added in NaOAc solution (0.25M, 950 μl). Add to this solution 68 GaCl 3 (eluent 0.05M HCl, 0.70-0.74GBq, 4mL). That is, after the precursor is dissolved in the sodium acetate solution, the Ge / Ga generator is rinsed with 0.05M HCl, and the rinse solution is directly added to a sterile bottle of the sodium acetate solution containing the precursor.

[0036] The reaction mixture was incubated at room temperature for 5 minutes. The product does not need to be further purified, and its radiochemical purit...

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Abstract

The invention relates to a tumor positron emission tomography(PET) imaging agent <68>Ga-NOTA-ADG and a preparation method and application thereof, and relates to synthesis of a labeling precursor of the PET imaging agent <68>Ga-NOTA-ADG and radiosynthesis of the <68>Ga-NOTA-ADG, wherein the precursor is used for labeling the <68>Ga-NOTA-ADG for the first time, and a result shows that the radiochemical yield of the preparation method is close to 100%. The positron imaging agent <68>Ga-NOTA-ADG provided by the invention can be used as a PET imaging probe for targeting tumors. Therefore, the <68>Ga-NOTA-ADG becomes a PET candidate imaging probe for the tumors. According to the invention, the radioactive chemical synthesis of the <68>Ga-NOTA-ADG is carried out for the first time, the preparation method is simple and rapid, and a foundation is laid for scientific research and clinical application of the <68>Ga-NOTA-ADG.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceutical chemistry, in particular to a tumor PET imaging agent 68 Ga-NOTA-ADG and its preparation method and application. Background technique [0002] Recently, the World Health Organization's International Agency for Research on Cancer (IARC) released the latest data on the global burden of cancer in 2020, estimating the latest incidence, mortality and cancer development trends in 36 of 185 countries around the world. According to the latest estimates, there will be 19.29 million new cancer cases in the world in 2020, including 10.06 million men and 9.23 million women; by 2020, 9.96 million people will die of cancer worldwide, including 5.53 million men and 4.43 million female. One of the important reasons why so many people die of cancer every year is that cancer has not been diagnosed and treated in time. [0003] 18 F-FDG, as a molecular probe reflecting glucose metabolism in tumor tis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H23/00C07H1/00A61K51/04
CPCC07H23/00C07H1/00A61K51/0491A61K51/0482C07B2200/05
Inventor 程登峰林卿玉石洪成
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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