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E[c(RGDfK)]c(RGDfK)
Nom chimique: H-Glu[cyclo(-Arg-Gly-Asp-D-Phe-Lys)]-cyclo(-Arg-Gly-Asp-D-Phe-Lys) // Synonymes: E[cyclo(RGDfK)]2, bis[cyclo[arginyl-glycyl-aspartyl-D-phenylalanyl-lysyl]] glutamate
- n° Art.:LS-3980
- n° CAS:250612-47-6
- Formule:C59H87N19O16
- Storage temperature:-20°C
- Masse moléculaire:1318,44 g/mol
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description
This cyclic RGD peptide shows high tumor targeting properties. It is an integrin inhibitor and gained interest non-small-cell lung cancer treatment. It can be easily conjugated to dyes (see for example LS 3950: ICG-E[c(RGDfK)]2), drug molecules, or chelators, like DOTA and NOTA.
references
1. Tumor targeting with radiolabeled alpha(v)beta(3) integrin binding peptides in a nude mouse model. Marcel L. Janssen, Wim J. Oyen, Ingrid Dijkgraaf, Leon F. Massuger, Cathelijne Frielink, D. Scott Edwards, Milind Rajopadhye, Henk Boonstra, Frans H. Corstens and Otto C. Boerman; Cancer Res. 2002; 62(21): 6146-6151.
2. microPET imaging of glioma integrin {alpha}v{beta}3 expression using (64)Cu-labeled tetrameric RGD peptide. Yun Wu, Xianzhong Zhang, Zhengming Xiong, Zhen Cheng, Darrell R. Fisher, Shuang Liu, Sanjiv S. Gambhir, and Xiaoyuan Chen; J. Nucl. Med. 2005; 46(10): 1707-1718.
References for similar peptides:
1. Radiolabeled Cyclic RGD Peptides as Radiotracers for Imaging Tumors and Thrombosis by SPECT. Yang Zhou, Sudipta Chakraborty, and Shuang Liu;
Theranostics 2011; 1: 58–82.
2. Jytte Oxboel et al., Comparison of two new angiogenesis PET tracers 68Ga-NODAGA-E[c(RGDyK)]2 and 64Cu-NODAGA-E[c(RGDyK)]2; in vivo imaging studies in human xenograft tumors, Comparison of two new angiogenesis PET tracers 68Ga-NODAGA-E[c(RGDyK)]2 and (64)Cu-NODAGA-E[c(RGDyK)]2; in vivo imaging studies in human xenograft tumors. Jytte Oxboela, Malene Brandt-Larsen, Christina Schjoeth-Eskesen, Rebecca Myschetzky, Henrik H. El-Ali, Jacob Madsen, Andreas Kjaer; Nuclear Medicine and Biology 2014; 41(3): 259-267.
DOI: 10.1016/j.nucmedbio.2013.12.003.
3. Stability Analysis of Glutamic Acid Linked Peptides Coupled to NOTA through Different Chemical Linkages. Lixin Lang, Ying Ma, Dale O. Kiesewetter, and Xiaoyuan Chen; Mol. Pharm. 2014; 11(11): 3867–3874. DOI: 10.1021/mp400706q.
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