A radioactive c-met targeting affinity small molecule compound and its application

Abstract

The invention especially relates to a radioactive C-MET-targeted affinity micromolecular compound and application thereof, belonging to the field of medical diagnosis and treatment. According to the invention, in-vivo tracking and imaging of diseases like tumors is realized through radiolabeling of a C-MET receptor antagonist. The radioactive C-MET-targeted affinity micromolecular compound can be used for monitoring the characteristics of biochemical changes of a hepatocyte growth factor receptor, visually displays the distribution and quantity of C-MET and is applicable to specific detection of a plurality of cancers including glioma, lung cancer, prostatic cancer, breast cancer, esophagus cancer, stomach cancer, liver cancer, pancreas cancer, ovarian cancer, rectal cancer and cervical cancer. The radioactive C-MET-targeted affinity micromolecular compound also has certain anticancer activity and has wide clinical application prospect.

Description

technical field [0001] The invention belongs to the field of medical diagnosis and treatment, in particular to a radioactive C-MET targeting affinity small molecular compound and its application. Background technique [0002] The encoded product of the proto-oncogene hepatocyte growth factor receptor (c-MET) is the cell membrane receptor of hepatocyte growth factor (HGF), which belongs to the tyrosine kinase receptor. The body dimerization leads to the activation of a series of signaling pathways, which lead to tumor angiogenesis, proliferation, enhanced cell motility and invasion, and finally metastasis. Therefore, the interaction between C-MET and its ligand HGF is closely related to the occurrence of various human tumors. , development related. Existing studies have found that C-MET receptors are highly expressed in a variety of tumors, including glioma, lung cancer, prostate cancer, breast cancer, esophageal cancer, gastric cancer, liver cancer, pancreatic cancer, ovari...

AI Technical Summary

Problems solved by technology

Although in vitro detection methods can judge and analyze the expression level of C-MET in cells or tissues, there are certain limitations in terms of technical analysis: ① Specimens need to be obtained through cell culture, biopsy or autopsy, and cannot be directly applied to the human body ;②The results of in vitro experiments may not be consistent with the real situation in the living body: In vitro experiments are greatly affected by experimental conditions, experimental equipment, and experimental methods. During the processing of samples, some important components may be lost, resulting in large errors , so that the experimental results are inconsistent with the real situation in the living body; ③ in vitro experiments are not conducive to dynamic research: in vitro experiments need to kill experimental animals at different time points to obtain tissues or repeated biopsies, and can only observe a certain stage of the disease, and cannot Realizing real dynamic research in the same animal body, it is not easy to get accurate conclusions in the whole process of such a complicated and progressive disease; ④The operation is complicated, time-consuming and expensive, and the randomness is great

However, the obtained image has poor contrast

So far, there are few reports on molecular imaging probes based on peptides and small molecular compounds, and there is an urgent need to develop methods for in vivo detection and quantitative C-MET based on small molecular substances

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