开发了极性 BODIPY-四嗪染料，并在体内点击到预积累的反式环辛烯修饰的抗 TAG72 单克隆抗体 CC49 (CC49-TCO)。使用内部开发的离体阻断测定来评估体内点击性能。所有测试的极性 BODIPY 结构都表现出出色的体内结合，证实开启四嗪染料在体内成功点击到预靶向的 CC49-TCO。荧光成像显示肿瘤与肌肉的比例高达 4:1。这项概念验证研究表明，基于开启探针的预靶向概念可用于癌症治疗，例如光动力疗法或热疗法。© 2024 作者。由美国化学会出版。

Polar BODIPY-tetrazine dyes were developed and clicked in vivo to a preaccumulated trans-cyclooctene-modified anti-TAG72 monoclonal antibody CC49 (CC49-TCO). The in vivo click performance was evaluated using an in-house developed ex vivo blocking assay. All tested polar BODIPY structures exhibited excellent in vivo binding, confirming that the turn-on tetrazine dyes successfully clicked in vivo to pretargeted CC49-TCO. Fluorescence imaging showed high tumor-to-muscle ratios of 4:1. This proof-of-concept study indicates that the pretargeting concept based on turn-on probes could be used for cancer treatments, such as photodynamic or -thermal therapy.© 2024 The Authors. Published by American Chemical Society.