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Isotope-substituted positron imaging agent targeting melanoma, preparation method and use thereof

An isotope and selected technology, applied in the field of PET, can solve the problems of accurate detection of unfavorable abdominal lesions, high uptake, and slow liver clearance

Active Publication Date: 2020-01-21
HTA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such probes often have the disadvantages of slow liver clearance and high uptake, which is not conducive to the accurate detection of abdominal lesions

Method used

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  • Isotope-substituted positron imaging agent targeting melanoma, preparation method and use thereof
  • Isotope-substituted positron imaging agent targeting melanoma, preparation method and use thereof
  • Isotope-substituted positron imaging agent targeting melanoma, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Compound of Example 1 18 F-PEG 3 -The synthetic route of FPN such as figure 1 shown.

[0108] 18 F-PEG 3 -The pipeline schematic diagram of the preparation process of FPN is as follows figure 2 As shown, the specific process is as follows:

[0109] 1. Preparation before automatic synthesis:

[0110] 1. Short-circuit the valve V17 and valve V15 in the pipeline.

[0111] 2. Add 1.5mL of eluent to the bottle controlled by valve V1, the eluent is mixed with 3mg K 2 CO 3 , 15mg phase transfer catalyst kryptofix.k222, 500μL sterile water and 1mL acetonitrile configuration;

[0112] Add 5 mg of the precursor previously dissolved in 600 μL of anhydrous DMSO solution to the container vial controlled by valve V3;

[0113] Add 2 mL of liquid (water / acetonitrile 50 / 50) to a vessel vial controlled by valve V6.

[0114] 2. Synthesis process

[0115] Step 1: Preparation and capture of 18F-Fˉ. With oxygen-18 abundance > 95% [ 18 O]H 2 O is used as a raw material, and th...

Embodiment 2

[0122] This embodiment examines the compound that embodiment 1 prepares 18 F-PEG 3 - The cell uptake of FPN, the specific steps are as follows: Take the B16F10 and A375m cells in the logarithmic growth phase and plate them, 1 × 10 per well 5 cells. Added to each well 18 F-PEG 3 - FPN (2μCi / well) set 4 duplicate wells in each group, incubate at 37°C for 30min, 60min and 120min respectively, absorb the radioactive medium, wash twice with polybutylene succinate (PBS) and collect in the same test tube Inside, the cells were lysed with 1N NaOH and then washed twice with polybutylene succinate (PBS) and collected in the same test tube. Finally, the radioactive counts of the supernatant and cell lysate were measured with an automatic gamma counter.

[0123] The results were expressed by cell uptake rate: cell uptake rate (%)=Counts cell lysate / (Counts cell lysate+Counts supernatant)×100%.

[0124] Cell blocking assays for analysis 18 F-PEG 3 -FPN and its standard 19 F-PEG 3...

Embodiment 3

[0128] The present invention utilizes the tumor-bearing mouse model to investigate the preparation of embodiment 1 18 F-PEG 3 - PET imaging and blocking imaging of FPN, the specific steps are as follows:

[0129] Animal tumor model construction: C57BL / 6 mice (male, 4-6 weeks old) and BALB / C nude mice (male, 4-6 weeks old) were provided by Beijing Weitong Lihua Biotechnology Co., Ltd., at Huazhong University of Science and Technology The animal experiment center is bred without special pathogen barrier system. All animals used in the experiment were approved by the Experimental Animal Use and Management Committee of Tongji Medical College, Huazhong University of Science and Technology. B16F10 cells 1×10 5 Suspended in 100 μL polybutylene succinate (PBS), planted subcutaneously in the axilla of the right upper limb of C57BL / 6 mice, A375m cells in 2×10 6 Each was suspended in 100 μL of polybutylene succinate (PBS), and subcutaneously planted in the axilla of the right upper l...

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Abstract

The invention relates to the technical field of PET (Positron Emission Tomography) and particularly relates to an isotope substituted targeted melanoma positron imaging agent and a preparation methodand an application of the isotope substituted targeted melanoma positron imaging agent. The invention provides a compound shown as in the formula I, and a preparation method and an application of thecompound. The compound is rapidly combined with a melanoma cell, the binding force is strong, the sensitivity is high, the specificity is good, and tiny lung and liver metastasis can still be sensitively detected under the condition that the uptake ratio of the compound by the liver is obviously reduced. In addition, the preparation method of the imaging agent is simple, a product is easy to get,and the stability is excellent.

Description

technical field [0001] The invention relates to the technical field of PET (Positron Emission Tomography, positron emission tomography), in particular to an isotope-substituted positron imaging agent targeting melanoma and its preparation method and application. Background technique [0002] Malignant melanoma (MM) is a malignant tumor originating from melanoma cells, which is highly malignant and highly metastatic. It can often invade the dermal tissue, spread to the lymphatic system, blood stream and other parts of the body, such as the lungs, liver, brain and bones. Its prognosis and survival rate are closely related to clinical stage. Patients with stage I and stage II melanoma can be surgically removed, and the 5-year survival rate is over 90%. However, patients with stage III and stage IV melanoma are often resistant to existing treatments, and their prognosis is very poor. The median survival period is only 6-9 months and the 3-year survival rate is only 10-15%. Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/81C07B59/00A61K51/04A61K51/06A61K101/02
Inventor 兰晓莉柳轻瑶许晓东盖永康张永学
Owner HTA CO LTD
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