Novel dual-function near-infrared II fluorescence and PET probe for tumor delineation and image-guided surgeryElectronic supplementary information (ESI) available. See DOI: 10.1039/c7sc04774f

• Main Authors: Sun, Yao, Zeng, Xiaodong, Xiao, Yuling, Liu, Changhao, Zhu, Hua, Zhou, Hui, Chen, Ziyang, Xu, Fuchun, Wang, Jule, Zhu, Mengyue, Wu, Junzhu, Tian, Mei, Zhang, Hong, Deng, Zixin, Cheng, Zhen, Hong, Xuechuan
• Format: Article
• Language: English
• ISSN: 2041-6520; 2041-6539
• DOI: 10.1039/c7sc04774f

Accurate tumor identification is essential in cancer management. Incomplete excision of tumor tissue, however, negatively affects the prognosis of the patient. To accomplish radical excision of tumor tissue, radiotracers can be used that target tumor tissue and can be detected using a gamma probe during surgery. Intraoperative fluorescence imaging could allow accurate real-time tumor delineation. Herein, a novel dual-modal imaging platform using base-catalyzed double addition of thiols into a propiolamide scaffold has been developed, allowing for the highly efficient and selective assembly of various thiol units in a protecting-group-free manner. The first small-molecule based αvβ 3 -targeted NIR-II/PET probe 68 Ga-SCH2 was concisely generated via this strategy and subsequently evaluated in mice bearing the U87MG xenograft. Excellent imaging properties such as good tumor uptake, high tumor contrast and specificity, tumor delineation and image-guided surgery were achieved in the small animal models. These attractive results of 68 Ga-SCH2 allow it to be a promising αvβ 3 -targeted NIR-II/PET probe for clinical translation. The first small-molecule based αvβ 3 -targeted NIR-II/PET dual-modal probes via base-catalyzed thiol-addition chemistry were concisely assembled and evaluated.