RGD Optical Probe
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IRDye® 800CW RGD Optical Probe is a BrightSite™ near-infrared (NIR) fluorescently-labeled RGD imaging agent specifically designed to target the overexpression of integrins on tumors. Integrins are cell surface heterodimeric glycoproteins involved in cell-to-cell and cell-to-matrix interactions.
Integrins are cell surface heterodimeric glycoproteins involved in cell-to-cell and cell-to-matrix interactions. The recognition motif, RGD (Arg-Gly-Asp), is a tripeptide sequence used to bind integrin receptors including αvβ3. Interest in using a labeled RGD peptide ligand for the study and/or monitoring of diseases related to the αvβ3 receptor over-expression is increasing. Several groups have labeled RGD successfully with fluorescent dyes for in vitro and in vivo imaging.
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Figure 1. An athymic nude mouse bearing a subcutaneous tumor, U87 (right; arrow), was imaged 24 h post intravenous injection of IRDye 680RD RGD (2 nmol). Image was captured on the Pearl® Imager; 700nm signal is presented in pseudocolor overlaid on a white light image of the mouse.
Figure 2: A) The On-Cell Western cell-based assay was used to evaluate binding affinity of IRDye 800CW RGD to U87 (glioblastoma) and 22Rv1 (prostate carcinoma) tumor cell lines. B) Binding of the IRDye 800CW RGD peptide was blocked by unlabeled RGD but not by a non-specific RAD peptide in U87 tumor cells. Nude mice bearing subcutaneous tumors, U87 (left hip) and A431(right hip), were imaged 24 hours post intravenous injection of IRDye 800CW RGD (1 nmole; C) or IRDye 800CW RGD (1 nmole) following a pre-injection 1 hour prior to an injection of unlabeled RGD peptide (100 nmoles; D) Images were captured on the Pearl Imager; 800nm signal is presented in pseudo-color overlaid on a white light image of the mouse. The images are normalized to the same look-up-table.