Radiolabeled T140 polypeptide compound, and preparing method and application thereof

A technology for radiolabeling and compounding, applied in the field of radiolabeling compounds, can solve the problems of inability to detect biochemical changes in tumor tissue, poor specificity and sensitivity, and no radioactive imaging agent, etc., to increase tumor uptake value, improve radiochemical purity, The effect of good diagnosis

Active Publication Date: 2013-09-04
厦门锐谱思科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

US and MRI techniques can be used for anatomical analysis of solid tumors, but the disadvantage of these techniques is that they cannot detect biochemical changes in tumor tissue at the molecular level, because MRI and CT techniques require tumor tissue to contain many contrast agents to contrast with normal tissue. In strong contrast, another disadvantage of these techniques is their poor specificity and sensitivity for high-incidence tumors (such as breast, gallbladder, lung, and prostate cancers), so we urgently need to develop a new tumor Specific radiotracers, which can not only be used for early diagnosis of tumors, but also can monitor tumor growth and tumor response to drug treatment
But so far there is no satisfactory radioactive imaging agent, so the development of an imaging agent with excellent performance is still in progress

Method used

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  • Radiolabeled T140 polypeptide compound, and preparing method and application thereof
  • Radiolabeled T140 polypeptide compound, and preparing method and application thereof
  • Radiolabeled T140 polypeptide compound, and preparing method and application thereof

Examples

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preparation example

[0047] 1. Preparation of Compound 1:

[0048] 1) 4-nitrophenyl-2-[ 18 F] Fluoropropionate ([ 18 F] FPA) Preparation

[0049] Use 1mL containing 15mg K222 (amino polyether) and 3.5mg K 2 CO 3 90% acetonitrile solution will 100mCi[ 18 F]F - Eluting from the separation column (CHROMAFIX), placed in a glass reaction bottle, and the solvent was removed by vacuuming to obtain anhydrous [ 18 F]F - . After cooling, add 5 mg of ethyl 2-bromopropionate dissolved in 0.5 mL of acetonitrile, and heat to 100° C. for 10 min to obtain ethyl 2-[ 18 F] Fluoropropionate. At the end of the reaction, add 125 μL of 0.2 mol / L potassium hydroxide solution and 375 μL of acetonitrile solution, and heat to 100° C. for 10 minutes to obtain ethyl 2-[ 18 F] Potassium fluoropropionate, then diluted with 1 mL of acetonitrile and dried in vacuo to remove the solvent, after which an appropriate amount of 1 mL of bis-(4-nitrophenyl)carbonate in acetonitrile (20 mg of bis-(4-nitrophenyl) Carbonate), r...

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Abstract

The present invention discloses a radiolabeled T140 polypeptide compound, and a preparing method and an application thereof. The structure of the T140 polypeptide compound labeled by radionuclide <18>F contains a radionuclide and a polypeptide (Ac-TC14012) targeting a CXCR4 receptor. According to different radiolabeling methods, the compound is grouped into two classes: a compound 1 and a compound 2. The present invention also relates to the application of the compound as an imaging agent in organs or organizations of human or animals, especially as a tumor imaging agent, and the compound has the advantages of high tumor uptake, low non-specificity uptake and higher target / non-target ratio.

Description

technical field [0001] The present invention relates to a radiolabeled compound, a process for its preparation and the use of said compound as a tumor imaging agent. Background technique [0002] According to the current trend of cancer incidence, the incidence of cancer worldwide will increase by 50% in 2020, and the number of new cancer patients in the world will reach 15 million each year (the World Health Organization (WHO) recently published the "World Cancer Report"). Early detection and early treatment are the most effective ways to reduce cancer mortality. The implementation of a screening system for bowel cancer, cervical cancer, breast cancer, etc. can reduce the number of cancer deaths worldwide by one-third. Currently in developing countries, 80% of cancer patients are only discovered at the advanced stage of the disease. [0003] Although the exact mechanism of cancer development is still unclear, if the cancer can be diagnosed at an early stage and treated wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K51/08C07K1/16A61K101/02
Inventor 张现忠陈小元牛刚
Owner 厦门锐谱思科技有限公司
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