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A fluorescent quenching probe targeting EGFR and its preparation method and application

A fluorescence quenching and targeting technology, applied in the field of fluorescence quenching probes and their preparation, can solve the problem of inability to achieve accurate diagnosis of lung cancer

Active Publication Date: 2021-04-13
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0008] In order to solve the technical problem that the precise diagnosis of lung cancer cannot be realized in the prior art, the inventors learned during the research process that the fluorescent group is introduced into the targeted drug molecule, and a bioactive fluorescent probe with target specificity is designed and synthesized. , to facilitate the study of the physiological / pathological functions of target molecules, and to explore the mechanism of action of drug molecules

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  • A fluorescent quenching probe targeting EGFR and its preparation method and application
  • A fluorescent quenching probe targeting EGFR and its preparation method and application
  • A fluorescent quenching probe targeting EGFR and its preparation method and application

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Embodiment Construction

[0077] In order to make the object, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments. It should be understood that the specific implementation cases described here are only used to explain the present invention, and are not intended to limit the present invention.

[0078] The present invention provides a fluorescent quenching probe targeting EGFR, the structural formula of which is as follows:

[0079]

[0080] Its preparation method includes:

[0081] Step 1: preparing the first intermediate;

[0082] The molecular formula of the first intermediate is:

[0083] Specifically, ethyl glycolate (8.4 g, 80.8 mmol) was added to a solution of sodium carbonate (16.8 g, 158.4 mol) in tetrahydrofuran (50 mL). The reaction mixture was stirred at room temperature. After the reaction continued for 1 h, the reaction material 1-bromo-2,4-d...

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Abstract

The invention relates to the technical field of molecular probes, and discloses a fluorescence quenching probe targeting EGFR and its preparation method and application. The structure of the fluorescence quenching probe includes a drug-effective skeleton structure, a fluorescence quenching group and A fluorescent labeling group, the fluorescent labeling group is selected from BODIPY FL dye; the fluorescent quenching group is selected from 2,4-dinitrophenol. Among them, the pharmacodynamic skeleton structure can be targetedly combined with the EGFR protein, and the quencher group in the molecular probe leaves, and the fluorescent labeling group can be specifically traced and imaged; molecular imaging can be used to detect specific cells Real-time observation of the expression process of molecules and molecules, and tracking of target targets, so as to realize the evaluation of disease development at the molecular pathological level and the precise detection of EGFR mutation typing in lung cancer patients.

Description

technical field [0001] The invention belongs to the technical field of molecular probes, and in particular relates to a fluorescence quenching probe targeting EGFR and its preparation method and application. Background technique [0002] In recent years, small molecule targeted drugs have been widely used, and the emergence of targeted drugs is one of the major breakthroughs in clinical tumor treatment. For example, gefitinib (Iressa) and erlotinib (Tarceva) are two targeted drugs for the treatment of non-small cell lung cancer, which belong to the epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI ). [0003] However, the key to using targeted drugs in the treatment of lung cancer is to accurately detect the EGFR mutation type of lung cancer. [0004] Clinically, before using TKI-targeted drugs in patients with non-small cell lung cancer, it is necessary to detect the EGFR gene mutation status. However, it is difficult to achieve accurate detection of E...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F5/02C09K11/06G01N21/64
CPCC07F5/022C09K11/06C09K2211/1007C09K2211/1044C09K2211/1055G01N21/6428G01N2021/6432
Inventor 邓慧雷倩李为民
Owner WEST CHINA HOSPITAL SICHUAN UNIV