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<68>Ga labeled compound for nano positron imaging agent, and preparation and application of <68>Ga labeled compound

A compound, 68ga technology, applied in the field of 68Ga-labeled compounds and their preparation, can solve the problems of low uptake rate and low targeting, and achieve the effects of good imaging effect, short reaction time and easy synthesis

Pending Publication Date: 2021-01-08
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The technical problem to be solved by the present invention is that the nano-PET imaging agent in the prior art needs to be prepared in vitro, has a low uptake rate in the body, and has low targeting. The compound of tropism nano-PET imaging agent, its preparation method, and the application of compound

Method used

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  • &lt;68&gt;Ga labeled compound for nano positron imaging agent, and preparation and application of &lt;68&gt;Ga labeled compound
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  • &lt;68&gt;Ga labeled compound for nano positron imaging agent, and preparation and application of &lt;68&gt;Ga labeled compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Embodiment 1: Ac-RVRRCK ( 68 Synthesis of Ga-NODAGA)-CBT

[0056] In this example, Ac-RVRRCK (NODAGA)-CBT was first synthesized, and the synthesis method was as follows:

[0057] Ac-RVRRCKCBT (66mg, 0.06mmol), tri-tert-butoxy-1,4,7-triazacyclononane-1,4-diacetate-7-carboxyethyl acetate (NODAGA (OtBu) 3 ) (33mg, 0.06mmol), O-benzotriazole-tetramethyluronium hexafluorophosphate (HBTU, 22.8mg, 0.06mmol), DIPEA (18μl, 0.09mmol) were dissolved in 2mL of DMF, and the reaction was stirred at room temperature Overnight, HPLC separation and purification to obtain the compound Ac-RVRRCK (NODAGA (OtBu) 3 )-CBT (25 mg, 0.015 mmol, yield: 25%). Ac-RVRRCK (NODAGA (OtBu) 3 )-CBT dissolved in CH containing 1% (v / v) triisopropylsilane, 95% (v / v) TFA 2 Cl 2 solution (3mL), stirred at room temperature for 3h, hydrolyzed the protecting group, separated and purified by HPLC to obtain the labeled precursor Ac-RVRRCK(NODAGA)-CBT (16mg, 0.011mmol, yield: 73%), according to the mass spect...

Embodiment 2

[0059] Embodiment 2: Ac-RVRRCK ( 68 Synthesis of Ga-NODAGA)-CBT

[0060] In this example, Ac-RVRRCK ( 68 The preparation method of Ga-NODAGA)-CBT is as follows: rinse with 0.05mol / LHCl 4mL solution 68 Ge- 68 Ga generator, take eluent 1.2mL (8mCi 68 GaCl 3 ), add 200 μL 0.5N sodium acetate solution to adjust the pH to 4-5. Add 10 μL of 3 mg / mL Ac-RVRRCK (NODAGA)-CBT water / acetonitrile (5:1 by volume) solution, and react at 30°C for 10 min. After the reaction, the reaction solution was collected, and the purity of the reaction solution was detected by HPLC to be 97%, without further purification. The HPLC operating parameters are the same as in Example 1.

Embodiment 3

[0061] Embodiment 3: the synthesis of Ac-RVRRCK (Ga-NODAGA)-CBT

[0062] Ac-RVRRCK (NODAGA)-CBT 29mg (0.02mmoL) and 34mg GaCl 3 (0.2mmoL), dissolved in 2mL of 0.2M ammonium acetate solution (pH 5), reacted at 95°C for 25min, prepared and purified by HPLC, and lyophilized to obtain the complex product Ac-RVRRCK(Ga-NODAGA)-CBT 28mg (0.018mmol, Yield 90.0%). Product HPLC chart see image 3 , The HPLC process is detected with the ultraviolet detector in Example 1, and the ultraviolet detection wavelength is 320nm. According to the results of mass spectrometry, it can be known that the structure of the generated compound is

[0063]

[0064] [M+H] + =1527.6051, molecular formula is C 61 h 97 N 22 o 14 S 3 Ga, mass spectrum see Figure 4.

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Abstract

A compound A disclosed by the invention is a small molecular compound, has furin targeting property, has relatively good cell permeability, can be taken in by tumor cells with the high expression of furin, carries out a condensation reaction at a tumor part to form nanoparticles, improves the local concentration of biological tissues, has relatively high tumor targeting property, high imaging sensitivity and good imaging effect, and avoids problems of low uptake rate and poor targeting property caused by directly adopting a macromolecule. According to the compound A disclosed by the invention,<68>Ga is used as a labeling part for imaging. <68>Ga does not need to be generated by an expensive cyclotron or synthesized by a synthesizer, only an appropriate eluent is needed to elute <68>Ga outfrom a commercial <68>Ge-<68>Ga generator, <68>Ga is uniformly mixed with a labeling precursor, and is combined with the labeling precursor through a complexation reaction, the synthesis is simple and convenient, the reaction time is short, a labeling rate is up to 95% or above, thereby a production amount can be determined by an amount of nuclide required, the use cost is relatively low, and large equipment and place are not needed.

Description

technical field [0001] The invention belongs to the field of nano-imaging agents, in particular to a nano-PET imaging agent 68 Ga-labeled compound and its preparation method and application. Background technique [0002] Early diagnosis of tumor is a key factor in treating tumor and improving survival rate. Among the clinical diagnostic methods of tumors, positron emission tomography (PET) is one of the most advanced medical imaging diagnostic methods. PET is a nuclear medical imaging technology that uses bioactive substances labeled with isotopes of natural elements that emit positrons as imaging agents. PET can perform three-dimensional whole-body scanning, quickly obtain multi-level tomographic images, and three-dimensional quantitative results, which are earlier, more sensitive, and more accurate. Diagnose tumors, guide treatment, and monitor outcomes more accurately. [0003] With the increase in the number of PET inspections, the demand for PET drugs is also increas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K51/12C07K7/06C07K1/13A61K103/00
CPCA61K51/08A61K51/121C07K7/06
Inventor 刘娅灵王洪勇邹霈吴昊吴军韩国庆
Owner JIANGSU INST OF NUCLEAR MEDICINE
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