Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof

A technology containing isonitriles and derivatives, which is applied in the field of FAPI derivatives and its preparation, and can solve problems such as short half-life

Active Publication Date: 2021-02-26
BEIJING NORMAL UNIVERSITY
View PDF6 Cites 11 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Currently, a 68 Ga-labeled FAPI imaging agent [ 68 Ga]Ga-FAPI-04 has received extensive attention, and preclinical studies have shown that it has a high tumor-non-target tissue ratio and rapid clearance, but it is due to 68 The half-life of Ga is short (68min), 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
  • Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof
  • Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof
  • Technetium-99m labeled isonitrile-containing FAPI derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0035] The present invention is described in detail below by way of examples: a technetium-99m labeled isonitrile-containing FAPI derivative, the general structural formula of which is [ 99m Tc-(CN-FAPI) 6 ] + , its structural formula is as follows:

[0036]

[0037] In the structural formula: with 99m Tc + The core is the central core, and the carbon atoms of the isonitrile in the CN-FAPI ligand molecule and 99m Tc(I) coordinates to form a six-coordinated [ 99m Tc-(CN-FAPI) 6 ] + Complexes. n is an integer greater than or equal to 2.

[0038] The preparation method of the FAPI derivative containing isocyanide of technetium-99m label, its preparation steps are as follows:

[0039] a: Synthesis of ligand CN-FAPI:

[0040] Weigh an appropriate amount of FAPI into a round bottom flask, add an appropriate amount of DMF to dissolve, then add an appropriate amount of triethylamine and compound 1, and react at room temperature. After the reaction, the solvent was distil...

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

PropertyMeasurementUnit
purityaaaaaaaaaa
purityaaaaaaaaaa
Login to View More

Abstract

The invention discloses a technetium-99m labeled isocyanide-containing FAPI derivative with a structural general formula of [99mTc-(CN-FAPI) 6] < + > and a preparation method and an application thereof. The [99mTc (CNFAPI) 6] < + > complex is obtained through two steps of synthesis of a ligand CN-FAPI and preparation of [99mTc-(CNFAPI) 6] < + >. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has relatively high uptake and good retention at tumor parts of tumor-bearing mice, has specificity in tumor uptake, and is a novel tumor imaging agentwith popularization and application values.

Description

technical field [0001] The invention belongs to the field of radiopharmaceuticals, in particular to a technetium-99m-labeled isonitrile-containing FAPI derivative, a preparation method and application. Background technique [0002] The tumor microenvironment plays an extremely important role in the occurrence and development of tumors. Tumor-associated fibroblasts are an important part of the tumor microenvironment. They have strong proliferation, migration, secretion and synthesis capabilities, and play an important role in the proliferation, migration, immune escape, radiochemotherapy resistance and energy metabolism of tumor cells. Role. Fibroblast activation protein (FAP) is an important molecular marker on the surface of tumor-associated fibroblasts, because it is selectively expressed on the cell membrane of fibroblasts in most solid tumor stroma, and it can promote the proliferation of tumor cells, cell The degradation and reconstruction of extracellular matrix, the...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
CPCA61K51/0482C07B2200/05C07F13/00
Inventor 张俊波阮晴张旭冉冯俊红王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
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