前列腺癌（PCa）被认为是全世界男性中最常见的恶性肿瘤。阿比特龙是一种 17α-羟化酶/C17, 20-裂解酶 (CYP17) 抑制剂，已被批准用于前列腺癌患者。然而，长期使用可能会出现一些负面影响，例如耐药性、毒性以及缺乏治疗反应的实时监测。因此，开发具有特异性靶向以避免副作用的抗癌药物势在必行。在这里，我们使用MHI-148（一种七次甲基花青（HC）近红外荧光染料（NIRF））作为原型结构来合成两种治疗诊断剂Abi-DZ-1和Abi-783。新化合物Abi-DZ-1保留了MHI-148优异的光物理特性和NIRF成像特性，并且可以通过HIF1α/有机阴离子转运多肽轴优先在前列腺癌细胞中积累，而不是在正常前列腺上皮细胞中积累。使用 Abi-DZ-1 的 NIRF 成像选择性地识别携带 PCa 异种移植物的小鼠中的肿瘤。此外，Abi-DZ-1 治疗显着延缓了细胞来源的异种移植模型和患者来源的肿瘤异种移植模型中的肿瘤生长。这一发现表明，Abi-DZ-1 有望成为未来肿瘤靶向成像和精准治疗的潜在多功能治疗诊断剂。使用 NIRF 染料平台构建治疗诊断剂在准确治疗和术中导航方面具有广阔的前景。

Prostate cancer (PCa) is considered to be the most prevalent malignancy in males worldwide. Abiraterone is a 17α-hydroxylase/C17, 20-lyase (CYP17) inhibitor that has been approved for use in patients with prostate cancer. However, several negative aspects, such as drug resistance, toxicity, and lack of real-time monitoring of treatment responses, could appear with long-term use. Therefore, the development of anticancer agents with specific targeting to avoid side effects is imperative. Here, we used MHI-148, a type of heptamethine cyanine (HC) near-infrared fluorescence dye (NIRF), as a prototype structure to synthesize two theranostic agents, Abi-DZ-1 and Abi-783. The new compound Abi-DZ-1 retained the excellent photophysical characteristics and NIRF imaging property of MHI-148, and it could preferentially accumulate in prostate cancer cells but not in normal prostate epithelial cells via the HIF1α/organic anion-transporting polypeptides axis. NIRF imaging using Abi-DZ-1 selectively identified tumors in mice bearing PCa xenografts. Moreover, Abi-DZ-1 treatment significantly retarded the tumor growth in both a cell-derived xenograft model and a patient-derived tumor xenograft model. This finding demonstrated that Abi-DZ-1 may hold promise as a potential multifunctional theranostic agent for future tumor-targeted imaging and precision therapy. Constructing theranostic agents using the NIRF dye platform holds great promise in accurate therapy and intraoperative navigation.