Soochow University

Haibin Shi

Yinjia Gao

Shuyue Ye

The present invention discloses HOresponsive crosslinking NIR molecular probe for tumor microenvironment and application therefor. The preparation method includes the following steps: the amide condensation of 2-propynylamine and Fmoc-Lys(Boc)-OH to obtain compound A01-01; removing protecting groups from compound A01-01, to obtain compound C1-2; reacting compound C1-2 and NHS-activated (3-carboxypropyl)triphenylphosphonium bromide, to obtain compound C1-3; removing protecting groups from compound C1-3, to obtain compound C1-4; reacting compound C1-4 with NHS-activated 3,5-dioxocyclohexane carboxylic acid, to obtain a compound C1-5; and reacting compound C1-5 with NIR dye, to obtain a HOresponsive crosslinking NIR molecular probe for tumor microenvironment. The probe itself uses HOin a tumor microenvironment for crosslinking on a tumor site, achieving the goal of a long-term retention, thereby improving a result of tumor imaging, and providing a novel strategy and means for improving long-term retention of a NIR molecular probe at a tumor site.

HO-responsive crosslinking near-infrared molecular probe for tumor microenvironment and use therefor

The present invention disclosed a red-light-mediated nucleic acid anchoring fluorescent probe and its preparation method and application. The fluorescent probe has the capability of taking a crosslinking reaction with RNA in cytoplasm under singlet oxygen mediation, and imaging of tumor tissues in a long window period is achieved. Moreover, it is found that by means of the probe, after crosslinking of RNA, a severe apoptosis phenomenon of tumor cells occurs, and the integration of diagnosis and treatment of tumors is achieved.

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Suzhou, China

Haibin Shi