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Near infrared fluorescent dye with tumor specificity targeting performance and applications thereof

A tumor-specific, fluorescent dye technology, applied in the field of heptacyanine dyes, which can solve problems such as changing the specificity and affinity of target molecules

Inactive Publication Date: 2015-01-28
师长宏 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these methods have their limitations for tumor imaging, because the targeted fragments can only detect some specific tumor cells, these cells have clear surface molecular characteristics, and they are only a small part of the diverse tumor cells
Moreover, chemical binding may alter the specificity and affinity of the target molecule

Method used

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  • Near infrared fluorescent dye with tumor specificity targeting performance and applications thereof
  • Near infrared fluorescent dye with tumor specificity targeting performance and applications thereof
  • Near infrared fluorescent dye with tumor specificity targeting performance and applications thereof

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Embodiment Construction

[0044] The near-infrared fluorescent dye PC-002 with tumor-specific targeting provided by the present invention is an asymmetric near-infrared cyanine dye with dual functions of tumor-specific target molecules and imaging. The dye can be detected by tumor tissues and cells Specific absorption; through non-invasive NIR imaging, tumor tissue can be observed to specifically absorb NIR dyes. The specific binding of the dye to canine tumor cells depends on hypoxia and activation of HIF1α / OATPs signaling molecules. The present invention will be further described in detail below in conjunction with the accompanying drawings, which are explanations rather than limitations of the present invention.

[0045] 1. Synthesis of near-infrared fluorescent dye PC-002:

[0046] Carry out the synthesis of NIR dye PC-002 according to the synthesis route shown below:

[0047]

[0048] The near-infrared fluorescent dye PC-002 is based on the asymmetric cyanine dye shown in compound 4 (in the h...

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Abstract

The invention provides a near infrared fluorescent dye with a tumor specificity targeting performance and applications thereof. The near infrared fluorescent dye is NIR dye PC-002, and can be automatically absorbed and accumulated by canine tumor cells; and the dye can be specifically accumulated in the tumor parts, and will not absorbed by the normal cells, so the dye can be used for tumor specificity target molecule imaging. The NIR specific combining between the near infrared fluorescent dye and the tumor cell is achieved by activating a HIF1[alpha] / OATPs signal molecule and oxygen deficiency. Heterogeneity of tumor cells is overcome, specific target molecule conjugate with common characters can be designed according to the characteristics of oxygen deficiency and OATP high expression of tumor cells, and through the observation on specific combining between the NIR dye and other tumor cells, the near infrared imaging technology can be applied to early warning and rapid diagnosis of more tumors.

Description

technical field [0001] The invention belongs to the technical field of near-infrared fluorescent dyes, and relates to a heptamethine dye, in particular to a near-infrared fluorescent dye with tumor-specific targeting and an application thereof. Background technique [0002] Near infrared fluorescent dye (near infrared dye, NIR) is a kind of heterocyclic compound of polymethylcyanine dye, which is composed of a heterocyclic ring at both ends or in the middle, an aromatic ring and multiple methyl chains inside the molecule. The π-conjugated system has both absorption and emission spectra in the near-infrared region (700-1000nm). Its inherent characteristics include: low autofluorescence, but strong fluorescein due to the aggregation of fluorophores after combining with macromolecules in the body; it has good tissue permeability, and the absorbed near-infrared light has a relatively deep penetration depth in biological tissues. Large, and the excited fluorescence is less affec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C09B23/10C09K11/06A61K49/00
Inventor 师长宏钟维国赵海燕潘东风
Owner 师长宏
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