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Cyclo(-RGDfK) TFA

Names

[ CAS No. ]:
500577-51-5

[ Name ]:
Cyclo(-RGDfK) TFA

[Synonym ]:
Cyclo(L-arginylglycyl-L-α-aspartyl-D-phenylalanyl-L-lysyl) trifluoroacetate (1:1)
Acetic acid, 2,2,2-trifluoro-, compd. with cyclo(L-arginylglycyl-L-α-aspartyl-D-phenylalanyl-L-lysyl) (1:1)

Biological Activity

[Description]:

Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cytoskeleton >> Integrin

[Target]

IC50: 0.94 nM (αvβ3 integrin)[1]


[In Vitro]

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin and exhibits a IC50 of 0.94 nM[1]. [66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].

[References]

[1]. Simecek J, et al. Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK). Mol Pharm. 2014 May 5;11(5):1687-95.

[2]. Lopez-Rodriguez V, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14.

[3]. V Lopez-Rodriguez, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H42F3N9O9

[ Molecular Weight ]:
717.694

[ Exact Mass ]:
717.305786

Related Compounds