GLUTトランスポーターによる糖の取り込み/血管新生を検出

 

 

 

 

 

 

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Product Description:

 CyAL-5 2-deoxyglucose (CyAl-5 2-DG) is a fluorescent imaging agent designed to target a wide spectrum of cancers such as breast, glioblastoma, colon and prostate in vitro as well as in vivo. 2-DG is a glucose analog that utilizes the GLUT transporters for entry into the cell. One of the hallmarks of many cancer cells is an elevated uptake of glucose. Numerous fluorophores, including 800CW [1] and 2-NBDG [2] have been used to label 2-DG for tumor detection. FDG has been used extensively in PET imaging for diagnosis and tumor response monitoring in various types of cancer [3,4].

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 [5]. 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 [6], and undergo rapid degradation in serum by a variety of proteases [7]. Cyclic RGD (cRGDfk) has shown elevated binding affinity and selectivity for αvβ3 over αIIBβ3 [6,8].

 

 

References:
[1] Kovar JL,Volcheck W, Olive DM, Simpson MA (2007). Abstract #5527, Poster presentation, AACR Annual Meeting.
[2] Lloyd PG, Hardin CD, Sturek M (1999). Physiol Res 48:401‐410.
[3] Hicks RJ, Wahl RL (2010). PET diagnosis and response monitoring in oncology, Molecular Imaging, Principles and Practice, p875‐895.
[4] Mankoff DA (2010). PET imaging in cancer clinical trials, Molecular Imaging, Principles and Practice, p1179‐1191.

[5] Desgrosellier JS, Cheresh DA (2010). Integrins in cancer: biological implications and therapeutic opportunities. Nat Rev Cancer.10:9‐22.
[6] 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.
[7] 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
[8] 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

 

Product Name	Catalog No.	Size
CyAL-5 2DG	DG-1001	125 nmol
CyAL-5 cRGD	RG-1001	25 nmol

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