Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

18 F-labeling affinity type compound and preparation method and application thereof

A compound and labeling technology, which is applied in the field of 18F-labeled Affimer compounds and its preparation, can solve the problems of high liver toxicity, complicated preparation methods, and low tumor sensitivity, and achieves small toxic and side effects, short residence time, radiochemical The effect of high purity

Active Publication Date: 2016-08-24
JIANGSU INST OF NUCLEAR MEDICINE
View PDF1 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, on the one hand, tumors are 18 The uptake of F-FBEM-(ZHER2:342) is low, which leads to low tumor imaging sensitivity; on the other hand, the liver is sensitive to the above 18 The uptake of F-FBEM-(ZHER2:342) is higher, which leads to greater toxicity to the liver; in addition, the above 18 The preparation method of F-FBEM-(ZHER2:342) is complicated, which limits its clinical application to a certain extent

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 18 F-labeling affinity type compound and preparation method and application thereof
  • 18 F-labeling affinity type compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 50nmol formula (II), 12nmol aluminum trichloride, 0.5mol / L, the acetic acid- Sodium acetate buffer;

[0062] The preparation method of the medicine box comprises the following steps:

[0063] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.5 mol / L, pH 4.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0064] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.5mol / L and pH of 4.0 to obtain solution B for subsequent use;

[0065] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0066] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0067] The preparation method of the ...

Embodiment 2

[0072] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 1nmol formula (II), 1nmol aluminum trichloride, 0.4mol / L, the acetic acid- Sodium acetate buffer;

[0073] The preparation method of the medicine box comprises the following steps:

[0074] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.4mol / L, pH 5.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0075] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.4mol / L and pH of 5.0 to obtain solution B for subsequent use;

[0076] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0077] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0078] The preparation method of the com...

Embodiment 3

[0083] This embodiment is used in the kit for preparing the compound shown in formula (I), and its reagent comprises: the compound shown in 5nmol formula (II), 1nmol aluminum trichloride, 0.6mol / L, the acetic acid- Sodium acetate buffer;

[0084] The preparation method of the medicine box comprises the following steps:

[0085] (1) Dissolving the selected mole of the compound shown in formula (II) in 0.6mol / L, pH 3.0 acetic acid-sodium acetate buffer solution to obtain solution A for subsequent use;

[0086] (2) dissolving selected moles of aluminum chloride in acetic acid-sodium acetate buffer solution of 0.6mol / L and pH of 3.0 to obtain solution B for subsequent use;

[0087] (3) Mix the solution A and the solution B uniformly to obtain the solution C for subsequent use;

[0088] (4) The solution C is subjected to sterile filtration, divided into controlled antibiotic bottles, freeze-dried for 24 hours, and sealed with a stopper.

[0089] The preparation method of the com...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the field of radiopharmaceuticals, and particularly relates to an 18-labeling affinity type compound and a preparation method and application thereof. On one hand, the absorbing value of a tumor to the 18-labeling affinity type compound is high, and the tumor development sensitivity high; on the other hand, the absorbing value of the liver to the 18-labeling affinity type compound is low, and the toxic and side effect on the liver is little. Animal experiments show that the 18-labeling affinity type compound can serve as tumor PET photographic developer targeting an HER2 receiver due to the fact that the absorbing value of the tumor to the 18-labeling affinity type compound is high, the residence time is short, the target ratio / target-to-nontarget ratio is high, good pharmacokinetics characters are achieved, and the biological performance is excellent. The preparation method is low in cost, and easy, convenient and quick to operate, the labeling rate is high, the radiochemical purity of a labeled product is high, and the prepared 18-labeling affinity type compound serving as the tumor PET photographic developer tarting the HER2 receiver can be clinically applied and popularized easily.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals and nuclear medicine, and specifically relates to a 18 F-labeled affibody compound, preparation method and application. Background technique [0002] Positron emission tomography (PET) is a cutting-edge technology for biomedical research and clinical diagnosis in the 21st century. Gain insight into the activity of labeled drugs in normal or sick people. Compared with SPECT, PET has obvious advantages such as high resolution and quantitative analysis. [0003] 18 F has nearly 100% positron efficiency, low positron energy (0.64 MeV), and relatively short physical half-life (t 1 / 2 =109.7min) and other characteristics, it is an ideal PET imaging nuclide. [0004] Peptides have the advantages of rapid tissue penetration, rapid clearance in blood, and low immunogenicity. 18 Suitable carriers for F-labeled imaging agents. Human epidermal growth factor receptor-2 (human epithelial growth factor ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07K14/00C07K1/13A61K51/08A61K101/02
CPCA61K51/08C07K14/00
Inventor 杨敏徐宇平潘栋辉赵富宽严骏杰王立振杨润琳张波
Owner JIANGSU INST OF NUCLEAR MEDICINE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com