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Tenatumomab (ST2146) is a murine monoclonal antibody against tenascin-C. And tenascin-C, the large extracellular glycoprotein, is overexpressed in cancer. Tenatumomab has been used for Pretargeted Antibody Guided Radioimmunoresearch (PAGRIT), and delivering radionuclides to tumors via PAGRIT and direct 131Iodine labeling approach[1][2]. | [in vivo]
Tenatumomab (4 μg/mouse; i.v.; single dose) shows a biodistribution associated with low and high tenascin expression in nude mice transplanted with human HT-29 colon carcinoma and/or human U-118MG glioblastoma cells, respectively[2].
| [References]
[1] Giannini G, et al. Synthesis and preliminary in vitro evaluation of DOTA-Tenatumomab conjugates for theranostic applications in tenascin expressing tumors. Bioorg Med Chem. 2019 Aug 1;27(15):3248-3253. DOI:10.1016/j.bmc.2019.05.047
[2] De Santis R, et al. Low and high tenascin-expressing tumors are efficiently targeted by ST2146 monoclonal antibody. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2191-6. DOI:10.1158/1078-0432.CCR-05-2526 |
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