CyAL-5 cyclic RGD Optical Probe

Data Sheet

Buy CyAL-5 cyclic RGD Products

Product Description

CyAL-5 cRGD is a fluorescence imaging agent comprising a potent cyclic RGD peptide, c(RGDfK)
designed to target integrins and a CyAL-5 dye with emission at 658 nm. This agent has been developed to target αvβ3 expression in the neovasculature as well as tumor cells, to monitor angiogenesis and growth and treatment efficacy. The integrin family is comprised of 25 identified members, which are heterodimers of 19 α- and 8 β-subunits imbedded noncovalently into the cell membrane [1]. Generally, linear RGD peptides, such as GRGDS (Gly-Arg-Gly-Asp-Ser), often have
low affinity (IC50 > 100 nM) and selectivity for αvβ3 and αIIBβ3 [2], and undergo rapid degradation in serum by a variety of proteases [3]. Cyclic RGD (cRGDfk) has shown elevated binding affinity and selectivity for αvβ3 over αIIBβ3 [2,4].

References

• [1] Desgrosellier JS, Cheresh DA (2010). Integrins in cancer: biological implications and therapeutic opportunities. Nat Rev Cancer.10:9-22.
• [2] Pfaff M, Tangemann K, Müller B et al. (1994). Selective recognition of cyclic RGD peptides of NMR defined conformation by αIIbβ3, αvβ3, and α5β1 integrins. J Biol Chem.269:20233-8.
• [3]Gottschalk KE, Kessler H (2002). The structures of integrins and integrin-ligand complexes: Implications for drug design and signal transduction. Angew Chem Int Ed Engl. 41:3767-74
• [4] Boturyn D, Dumy P (2001). A convenient access to αvβ3/αvβ5 integrin ligand conjugates: regioselective solid-phase functionalization of an RGD based peptide. Tetrahedron Lett. 42:2787-90

Storage and Handling

CyAL-5 is sold under an exclusive license from Harvard Medical School and Mass General Hospital.