title: A multifunctional heptamethine near-infrared dye for cancer theranosis.
abstract: Personalized oncology significantly relies on the development of cancer theranostic agents to integrate cancer therapeutics and diagnostics. Current most common strategy for development of such multifunctional agents requires multistep chemical conjugation with cancer targeted ligands, contrast agents and therapeutic agents. Here we report the chemical synthesis and biological characterization of a new heptamethine dye, termed as IR-808DB, natively with multifunctional characteristics of cancer targeting, near-infrared fluorescence imaging, and efficient anticancer activity. The tumor inhibition effect of IR-808DB is higher than that of cyclophosphamide (CTX) toward a broad spectrum of tumor xenograft models. These findings provide IR-808DB a promising prospect as a new cancer theranostic agent that would enable integration of cancer targeted therapeutics and diagnostics without requirement of multi-component chemical conjugation.
authors.affiliation: Institute of Combined Injury, State Key Laboratory of Trauma, Burns and Combined Injury, Chongqing Engineering Research Center for Nanomedicine, College of Preventive Medicine, Third Military Medical University, Chongqing 400038, China.
authors.forename: Shenglin
authors.initials: S
authors.lastname: Luo
authors.forename: Xu
authors.initials: X
authors.lastname: Tan
authors.forename: Qingrong
authors.initials: Q
authors.lastname: Qi
authors.forename: Qinyuan
authors.initials: Q
authors.lastname: Guo
authors.forename: Xinze
authors.initials: X
authors.lastname: Ran
authors.forename: Lilong
authors.initials: L
authors.lastname: Zhang
authors.forename: Erlong
authors.initials: E
authors.lastname: Zhang
authors.forename: Yufeng
authors.initials: Y
authors.lastname: Liang
authors.forename: Lingling
authors.initials: L
authors.lastname: Weng
authors.forename: Hu
authors.initials: H
authors.lastname: Zheng
authors.forename: Tianmin
authors.initials: T
authors.lastname: Cheng
authors.forename: Yongping
authors.initials: Y
authors.lastname: Su
authors.forename: Chunmeng
authors.initials: C
authors.lastname: Shi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002232:Carbocyanines / Q000737:chemistry / Q000627:therapeutic use*; D002478:Cells, Cultured; D003287:Contrast Media / Q000737:chemistry / Q000627:therapeutic use; D003952:Diagnostic Imaging / Q000379:methods*; D005456:Fluorescent Dyes / Q000737:chemistry / Q000627:therapeutic use*; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008819:Mice, Nude; D009369:Neoplasms / Q000175:diagnosis*; D051381:Rats; D017207:Rats, Sprague-Dawley; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D002232:Carbocyanines; D003287:Contrast Media; D005456:Fluorescent Dyes; C582290:IR-808DB; D007211:Indoles