Imaging drug <68>Ga-NOTA-IF7 targeting Anxa1 in tumor blood vessels and preparation method thereof
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A technology of NOTA-IF7 and 68ga-nota-if7, applied in material separation, instruments, analytical materials, etc., can solve problems such as high negative predictive value, and achieve the effects of short time consumption, simple preparation process and stable markers
Inactive Publication Date: 2014-06-04
JIANGSU INST OF NUCLEAR MEDICINE
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However, the uptake of FDG is not unique to tumor tissues, and can also be concentrated in normal tissues such as the heart and brain. In addition, inflammation, sarcoid tumors, tuberculosis, and urinary tracts also have more FDG concentrations, so there are also certain false positives. but have a high negative predictive value
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Embodiment 1
[0033] Example 1 68 Ga leaching
[0034] Use a 5mL syringe to take 5mL of 0.05mol / L HCl to rinse the germanium-gallium generator at a rate of 1-2mL / min, and collect the eluent at the same time, 1mL per bottle. Take the vial with the highest radioactivity for labeling.
Embodiment 2
[0035] Example 2 68 Labeling of Ga-NOTA-IF7
[0036] Dissolve NOTA-IF7 with DMSO, take 30μL NOTA-IF7 (10μg~100μg), add 300μL freshly rinsed 68 Ga (7.4~740MBq), adjust the pH to 3.5~4.5 with 1mol / L Hepes buffer, shake and mix gently, and react in a water bath at 50~100°C for 10~20min to obtain the product radioactivity 68 Ga-NOTA-IF7.
[0037] A preparation method targeting tumor blood vessel Anxa1 labeled precursor NOTA-IF 7, the steps are as follows:
[0038] (1) Dissolution: Weigh 8 mg of p-SCN-Bn-NOTA and dissolve in 50 μL dimethyl sulfoxide DMSO to obtain solution a; weigh 20 mg IF 7 and dissolve in 300 μL dimethylformamide DMF to obtain solution b;
[0039] (2) Preparation of NOTA-IF 7: Add solution a and solution b prepared in step (1) into a glass bottle according to the mass ratio of NOTA:IF7 1-2:1, and then add 50 μL of diisopropylethylamine DIEA , react at 40°C for 2 h; cool to room temperature, add 30 μL of acetic acid to the reaction solution to terminate the rea...
Embodiment 3
[0043] Embodiment 3 quality control
[0044] 68 Radioactivity purity of Ga-NOTA-IF7 was determined by HPLC.
[0045] HPLC analysis conditions: chromatographic analysis column is C18 column (4.6×250mm), injection volume is 10μL, mobile phase A is pure water containing 0.1% TFA, B is acetonitrile containing 0.1% TFA, flow rate is 1mL / min, gradient wash The stripping condition was 95% A and 5% B at 5 minutes, increased to 35% A and 65% B at 30 minutes, and the detection wavelength was 218nm. For radioactivity detection, use a special radioactive detector for HPLC, see the results figure 1 .
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Abstract
The invention belongs to the fields of radiopharmaceuticals and nuclear medicine and provides an imaging drug <68>Ga-NOTA-IF7 targeting Anxa1 in tumor blood vessels and a preparation method thereof. The drug <68>Ga-NOTA-IF7 is used for differential diagnosis and periodization of tumors, accurate positioning of focuses and curative effect monitoring. According to the invention, the tumor imaging drug <68>Ga-NOTA-IF7 is prepared through leaching of <68>Ga and <68>Ga-NOTA-IF7 labeling. The preparation method has the advantages of simple preparation technology, convenient operation, small consumption of time, a high labeling rate and a stable marker and facilitates further application of the drug in clinical practice, scientific research and medicinal development. The invention also provides a novel positive electron tumor imaging agent. The novel positive electron tumor imaging agent has good targeting to tumors, so tumor imaging effects are improved, and a visual tool is provided for differential diagnosis and periodization of tumors, accurate positioning of focuses and curative effect monitoring. <68>Ga-NOTA-IF7 is a labeled compound belonging to polypeptide and has the advantages of small molecular weight, low immunogenicity, good tissue penetrability, high tumor tissue affinity and good application prospects.
Description
technical field [0001] An imaging drug targeting tumor blood vessels Anxa1 68 Ga-NOTA-IF7 and a preparation method thereof are used for differential diagnosis, staging, precise location of lesion and curative effect monitoring of tumors, and belong to the fields of radiopharmaceuticals and nuclear medicine. Background technique [0002] In recent years, with the penetration of molecular biology into the field of nuclear medicine and the development of PET / CT technology, but due to the lag in the development of radiopharmaceuticals, the bottleneck of PET / CT application has become prominent. At present, in all the examinations of PET imaging in my country, more than 95% of PET drugs are 18 F-labeled 2-fluorodeoxyglucose ( 18 F-FDG), greatly limiting the potential functions and effects of PET. Therefore, the study of new positron radionuclides and their labeled radiopharmaceuticals has become a hot spot in the development of nuclear medicine. [0003] The application of rad...
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