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The work develops, characterizes, and validates two new FAP-targeted optical probes for near-infrared fluorescence imaging in vitro and in vivo. IRDye800CW and FNIRTag heptamethine cyanines were conjugated to the NH precursor of FAPI-46. The dyes were assessed for physicochemical properties, biodistribution, and imaging performance in a breast cancer model. FAPI-FNIRTag showed stronger fluorescence and higher photostability than FAPI-IRDye800CW, with both compounds achieving high tumor accumulation in TUBO-bearing mice at 24 h, supporting fluorescence-guided surgery potential.",{"@graph":69,"@context":123},[70,84,106],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":35,"@type":76,"position":81},"https://docshare.wps.com/document/healthcare/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/novel-fap-targeted-heptamethine-cyanines-for-nirf-imaging-applications/375889/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/novel-fap-targeted-heptamethine-cyanines-for-nirf-imaging-applications/375889.png","ImageObject",300,407,{"name":92,"@type":93},"Sophia Brooks","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-11-03","2026-09-24",true,{"@type":102,"interactionType":103,"userInteractionCount":105},"InteractionCounter",{"@type":104},"ViewAction",15,{"@type":107,"mainEntity":108},"FAQPage",[109,115,119],{"name":110,"@type":111,"acceptedAnswer":112},"What is the goal of developing the two FAP-targeted probes in this work?","Question",{"text":113,"@type":114},"To develop, characterize, and validate two novel FAP-targeted optical imaging probes for near-infrared fluorescence imaging, tested in vitro and in vivo.","Answer",{"name":116,"@type":111,"acceptedAnswer":117},"How are the probes constructed and what fluorophores are used?",{"text":118,"@type":114},"The heptamethine cyanines IRDye800CW and FNIRTag are conjugated to the NH precursor of the FAP inhibitor FAPI-46.",{"name":120,"@type":111,"acceptedAnswer":121},"Which probe performs better and what results support further use?",{"text":122,"@type":114},"FAPI-FNIRTag shows stronger fluorescence and higher photostability than FAPI-IRDye800CW. Both compounds show strong tumor accumulation in TUBO breast cancer-bearing mice 24 h post-administration, suggesting potential for fluorescence-guided surgery.","https://schema.org",{"og:url":83,"og:type":125,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":127,"canonical":83},"index,follow",{"doc_id":129,"site_id":62},375889,1790467647,{"code":4,"msg":5,"data":132},{"doc_id":129,"user_id":133,"nickname":92,"user_avatar":134,"doc_module":4,"category_id":34,"category_name":35,"doc_title":65,"doc_description":67,"doc_content":135,"file_id":136,"file_url":137,"file_type":138,"file_size":139,"view_count":105,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":140,"language":141,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":142,"faqs":143,"seo_title":144,"seo_description":67,"update_tm":145,"read_time":146},962084925636,"https://ap-avatar.wpscdn.com/davatar_994ba38a5ba835b3df7d355c54d3ed8d","This article is licensed under CC-BY 4.0   \n[pubs.acs.org/molecularpharmaceutics](pubs.acs.org/molecularpharmaceutics)  Article   \nNovel FAP-Targeted Heptamethine Cyanines for NIRF Imaging Applications  \nRebecca Rizzo, Martina Capozza, Laura Conti, Lidia Avalle, Valeria Poli, and Enzo Terreno*  \n Cite This: Mol. Pharmaceutics 2025, 22, 1518−1528  \nRead Online  \n\n|  |  |  |  |  |  |\n| --- | --- | --- | --- | --- | --- |\n| ACCESS   | Metrics & More |  |  Article Recommendations |  | *sı Supporting Information |\n\nABSTRACT: Fibroblast activation protein (FAP) is a pan-cancer target that is useful for imaging, ideally all epithelial cancers. This work aimed to develop, characterize, and validate two novel FAPtargeted probes for optical imaging, both in vitro and in vivo. IRDye800CW and FNIRTag heptamethine cyanines were conjugated to the NH precursor of the well-known FAP inhibitor FAPI-46, which is widely employed in nuclear medicine. In addition to synthesis, the dyes were characterized in terms of physicochemical properties, biodistribution, and imaging performances in a breast cancer tumor model. FAPI-FNIRTag showed a stronger fluorescence and higher photostability compared to FAPIIRDye800CW. Notably, both compounds exhibited strong tumor accumulation in TUBO breast cancer-bearing mice 24 h  \npostadministration, suggesting potential for further investigation as fluorescence-guided surgery (FGS) agents. KEYWORDS: FAP, near-infrared fluorescence imaging, breast cancer, heptamethine cyanines, optical imaging  \n■ INTRODUCTION  \nFibroblast activation protein (FAP) is a leading theranostic biomarker because of its crucial role in angiogenesis, growth, and progression in cancer.1 FAP is a transmembrane serine protease overexpressed by cancer-associated fibroblasts (CAFs) in over 90% of epithelial cancers,2 including breast,3,4 colon,4,5 and pancreatic4,6 tumors. Thus, FAP has been considered as a pan-cancer target in several preclinical approaches and clinical trials. Considering that, the development of diagnostic approaches by targeting FAP would be of great importance. Optical imaging is a noninvasive technique based on the interaction of light with tissues that guides the clinician’s decision-making in real-time. For instance, in surgery, intraoperative fluorescence imaging represents a key player in improving cancer surgical outcomes.7 Surgical intervention remains a primary treatment for patients with solid tumors, but incomplete resections or unnecessary removal of healthy tissues can significantly affect the prognosis of patients. In breast cancers, for example, many of which are nonpalpable, margin positivity rates range from 5 to 49%.8 Indeed, among the factors that influence local recurrence, margin resection is one of the few modifiable risk factors, which prompts surgeons to seek new approaches to reduce positive surgical margin (PSM) rates.9 Tumor-targeted, nearinfrared fluorescent (NIRF) imaging is an emerging field of real-time intraoperative cancer imaging based on tumortargeted NIRF dyes that have become relevant in breast cancer, as demonstrated by literature studies primarily in  \nphases 1 and 2.10 Besides undeniable advantages such as thenoninvasive nature, the immediate response during surgery intervention, the tunability of probes to obtain functional and molecular information, and the use of nonionizing radiation, optical imaging is affected by some criticisms. Among these, fluorophore conjugation often alters the properties of both the fluorophore and the molecule to which it is conjugated.11 Specifically, important parameters such as brightness, target binding, in vivo stability, and pharmacokinetics (PK) are often impacted.12 Thus, the development of novel tumor-targeted NIRF dyes has increased interest in the fluorescence-guided surgery (FGS) field. To identify a pan-tumor marker for use in the imaging of solid tumors, some research groups have investigated FAP-targeting ligands for fluorescence imaging. Ne","cbCaiphqKARLkpAs","https://ap.wps.com/l/cbCaiphqKARLkpAs","pdf",7320613,11,"English","# ABSTRACT\n# INTRODUCTION\n# EXPERIMENTAL SECTION","[{\"question\":\"What is the goal of developing the two FAP-targeted probes in this work?\",\"answer\":\"To develop, characterize, and validate two novel FAP-targeted optical imaging probes for near-infrared fluorescence imaging, tested in vitro and in vivo.\"},{\"question\":\"How are the probes constructed and what fluorophores are used?\",\"answer\":\"The heptamethine cyanines IRDye800CW and FNIRTag are conjugated to the NH precursor of the FAP inhibitor FAPI-46.\"},{\"question\":\"Which probe performs better and what results support further use?\",\"answer\":\"FAPI-FNIRTag shows stronger fluorescence and higher photostability than FAPI-IRDye800CW. Both compounds show strong tumor accumulation in TUBO breast cancer-bearing mice 24 h post-administration, suggesting potential for fluorescence-guided surgery.\"}]","Novel FAP-Targeted Heptamethine Cyanines for NIRF Imaging Applications | PDF",1790216520,28]