A fluorescently labeled molecular probe targeting ephrinb2 and its preparation method and application

A fluorescent labeling and molecular probe technology, applied in the field of biomedicine, can solve the problems of no EphrinB2 tracer analysis and drug-receptor interaction fluorescent probes, and achieve important application value and market prospects

Inactive Publication Date: 2018-10-30
XI AN JIAOTONG UNIV
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Problems solved by technology

[0004] The object of the present invention is to provide a fluorescently labeled molecular probe targeting EphrinB2 and its preparation method and application, so as to solve the problem that there are no fluorescent probes available for EphrinB2 tracer analysis and drug-receptor interaction

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  • A fluorescently labeled molecular probe targeting ephrinb2 and its preparation method and application
  • A fluorescently labeled molecular probe targeting ephrinb2 and its preparation method and application
  • A fluorescently labeled molecular probe targeting ephrinb2 and its preparation method and application

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Embodiment Construction

[0042] The present invention provides a fluorescently labeled molecular probe targeting EphrinB2, which is denoted as CY5-SU. The probe has the function of specifically targeting EphrinB2, can compete with EphB4 to combine with EphrinB2 and inhibit the activity of tumor cells, and can be widely used. For drug-receptor interaction analysis and drug mechanism research. The present invention will be further described in detail below in conjunction with specific embodiments and accompanying drawings.

[0043] The synthetic route of targeting EphrinB2 fluorescently labeled molecular probe provided by the present invention is as follows: figure 1 As shown, it specifically includes the following steps:

[0044] (1) Synthesis of Intermediate 1:

[0045] Under nitrogen protection, a solution of benzyloxycarbonyl succinimide (2.42g, 9.71mmol) in -40°C in 60mL of anhydrous dichloromethane was slowly added dropwise to -40°C N-ethylethylenediamine (0.88g or 1.05mL, 10.0mmol) in 60mL of ...

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Abstract

The invention discloses a fluorescent marker molecular probe for targeting EphrinB2 and a preparation method and an application thereof. The fluorescent marker molecular probe is characterized in that a medicine of Sunitinib is connected with a fluorescent molecule CY5, and the inhibition function of original function molecule on proliferation of tumor cells is remained. The fluorescent marker molecular probe has the advantages that the selection and identification function on Ephrinb2 target protein is high; under the radiation of 647+ / -5nm absorbing light, the protein cell of an EphrinB2 receptor can be efficiently marked, and a red fluorescent signal is sent out; the molecular probe is used as a targeting tool molecule, and can directly act on the tumor cells; the important application value and broad application prospect are realized in the targeting identification field, analysis of mutual action of medicines, and study of medicine action mechanism.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a fluorescently labeled molecular probe targeting EphrinB2 and its preparation method and application. Background technique [0002] The incidence of tumor is increasing year by year all over the world, and it has become a killer that seriously threatens human health. Anticancer drug research is a very challenging and significant field in life science today. Receptor tyrosine kinases (RTKs) are a huge family that play a very important role in the life activities of organisms. Eph belongs to the largest known protein tyrosine kinase receptor family (RTKs) subfamily, including Eph receptors and their Ephrin ligands. EphB4 and EphrinB2 show a unique way in signal transmission, and can be activated by each other to generate "forward signal" and "reverse signal". to the signal. EphrinB2 may play a role as a general regulator in the VEGF signaling pathway and play a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/14G01N21/64C09K11/06
CPCC07D403/14C09K11/06C09K2211/1022C09K2211/1029G01N21/6486
Inventor 张彦民陈胜昔白晓光马维娜代秉玲张东东展颖转
Owner XI AN JIAOTONG UNIV
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