IR 780

IR 780 is a heptacyanine fluorescent probe for in vivo imaging of tumor cells with a large absorption spectrum of 750-830nm.It is also a powerful and stable nanotheranostic agent[1,2]. The hydrophobic properties of IR-780 enable it to be encapsulated in the bilayer of liposome with high encapsulation efficiency. IR-780 has high singlet oxygen (1O2) quantum yield, photostability and fluorescence intensity [3], For IR-780, the 1O2 quantum yield could reach 0.127[4].

IR-780(0-160 µM;24h) induced dose-dependent inhibition of PC-3, LNCaP, and RWPE-1 cells proliferation [5].IR-780 can be efficiently taken up by RCC cells through the organic anion-transporting polypeptide (OATP) superfamily transporters, which enables the diagnosis of even small lesions through tumor tissue-specific imaging [6]. Uptake of IR-780(4 µM, 10 µM or 16 µM ;1-4h) is dose and time-dependent in 4T1 cancer cells. When these cancer cells were treated with IR-780 and US irradiation, survival was significantly reduced and necrotic/apoptotic cells increased [7].

IR-780(0.334 mg/kg and 3.334 mg/kg; i.p.; daily for 1 month) (10 times imaging dose) staining for 1 month had no significant effect on physical activity weight and histology of BABL/C mice. High signal-to-background ratios of xenografts were achieved in athymic nude mice models (IR-780 dye application in prostate cancer detection) 24 h after NIRF dyes administration [6]. Using intracranial glioma xenograft in nude mice and administration of ILs (including IR-780) by convection enhanced delivery (CED) to overcome blood-brain barrier, liposomal IR-780(0.8 g/L IR-780) could be specifically delivered to the brain tumor [8].

References:
[1]. Li S, Zhou S, et,al. Exceptionally High Payload of the IR780 Iodide on Folic Acid-Functionalized Graphene Quantum Dots for Targeted Photothermal Therapy. ACS Appl Mater Interfaces. 2017 Jul 12;9(27):22332-22341. doi: 10.1021/acsami.7b07267. Epub 2017 Jun 28. Erratum in: ACS Appl Mater Interfaces. 2020 Jun 17;12(24):27819-27820. PMID: 28643511.
[2]. Wang K, Zhang Y, et,al. Self-assembled IR780-loaded transferrin nanoparticles as an imaging, targeting and PDT/PTT agent for cancer therapy. Sci Rep. 2016 Jun 6;6:27421. doi: 10.1038/srep27421. PMID: 27263444; PMCID: PMC4899881.
[3]. Zhang L, Wang D, Yang K, Sheng D, Tan B, Wang Z, Ran H, Yi H, Zhong Y, Lin H, Chen Y. Mitochondria-Targeted Artificial "Nano-RBCs" for Amplified Synergistic Cancer Phototherapy by a Single NIR Irradiation. Adv Sci (Weinh). 2018 May 21;5(8):1800049. doi: 10.1002/advs.201800049. PMID: 30128231; PMCID: PMC6097143.
[4]. Ren H, Liu J, et,al. Relighting Photosensitizers by Synergistic Integration of Albumin and Perfluorocarbon for Enhanced Photodynamic Therapy. ACS Appl Mater Interfaces. 2017 Feb 1;9(4):3463-3473. doi: 10.1021/acsami.6b14885. Epub 2017 Jan 18. PMID: 28067039.
[5]. Yi X, Yan F, et,al. IR-780 dye for near-infrared fluorescence imaging in prostate cancer. Med Sci Monit. 2015 Feb 16;21:511-7. doi: 10.12659/MSM.892437. PMID: 25686161; PMCID: PMC4335586.
[6]. Yang X, Shao C, et,al. Optical imaging of kidney cancer with novel near infrared heptamethine carbocyanine fluorescent dyes. J Urol. 2013 Feb;189(2):702-710. doi: 10.1016/j.juro.2012.09.056. Epub 2012 Sep 20. PMID: 23000848; PMCID: PMC4120709.
[7]. Li Y, Zhou Q, et,al. IR-780 Dye as a Sonosensitizer for Sonodynamic Therapy of Breast Tumor. Sci Rep. 2016 May 13;6:25968. doi: 10.1038/srep25968. PMID: 27174006; PMCID: PMC4865802.
[8]. Lu YJ, S AT, et,al. Liposomal IR-780 as a Highly Stable Nanotheranostic Agent for Improved Photothermal/Photodynamic Therapy of Brain Tumors by Convection-Enhanced Delivery. Cancers (Basel). 2021 Jul 22;13(15):3690. doi: 10.3390/cancers13153690. PMID: 34359590; PMCID: PMC8345063.