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A kind of fluorescent molecular probe targeting EGFR and its preparation method and application

A fluorescent molecular probe, targeting technology, applied in fluorescence/phosphorescence, chemical instruments and methods, material analysis by optical means, etc. Solve problems such as the inability to directly obtain the mutation of the primary tumor

Active Publication Date: 2021-07-06
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Abstract
  • Description
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Problems solved by technology

[0005] 2) Secondly, the existing EGFR mutation detection methods all have certain limitations. For example, the use of molecular pathology to detect EGFR mutations has poor reproducibility and cannot overcome spatial heterogeneity. Relatively speaking, molecular detection is more convenient and reproducible , but the disadvantage is that the mutation status of the primary tumor cannot be obtained directly, and the problem of heterogeneity within the primary tumor and metastases of lung cancer cannot be solved
[0006] In addition, traditional imaging methods such as CT and MRI cannot reflect the information of EGFR molecular typing at the molecular level.

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  • A kind of fluorescent molecular probe targeting EGFR and its preparation method and application
  • A kind of fluorescent molecular probe targeting EGFR and its preparation method and application
  • A kind of fluorescent molecular probe targeting EGFR and its preparation method and application

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Embodiment Construction

[0065] 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 embodiments described here are only used to explain the present invention, not to limit the present invention.

[0066] The present invention provides a fluorescent molecular probe targeting EGFR, the structural formula of which is as follows:

[0067]

[0068] Its preparation method includes:

[0069] Step 1: reacting the first reactant with the second reactant to obtain the first intermediate;

[0070] Wherein, the structural formula of the first reactant is as follows:

[0071] The structural formula of the second reactant is as follows:

[0072] The structural formula of the first intermediate is as follows:

[0073] Specifically, the first reactant (15.0g, 49.9mmol) and the second reactant (...

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Abstract

The invention relates to the technical field of molecular probes, and discloses a fluorescent molecular probe targeting EGFR and its preparation method and application. The fluorescent molecular probe includes a fluorescent labeling group, a linking group and a reactive group; the reactive group The group can be targetedly combined with the EGFR protein, and can be specifically labeled, traced, and imaged through the fluorescent labeling group; the expression process of specific cells and molecules can be observed in real time by using molecular imaging, and the target site can be detected. Tracking, 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, in particular to a fluorescent molecular probe targeting EGFR and its preparation method and application. Background technique [0002] In recent years, molecular targeted drugs have been widely used, which 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 ). Accurate detection of EGFR mutation typing in lung cancer is the key to the use of molecular targeted drugs in the treatment of lung cancer. [0003] 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 EGFR mutation typing in lung cancer patients with exi...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/12C09K11/06G01N21/64
CPCC07D413/12C09K11/06C09K2211/1044C09K2211/1048G01N21/6428G01N21/6456G01N2021/6439
Inventor 邓慧雷倩李为民
Owner WEST CHINA HOSPITAL SICHUAN UNIV