500577-51-5

500577-51-5 structure

Name: Cyclo(-RGDfK) TFA
Chemical Name: Cyclo (-RGDfK) 2,2,2-Trifluoroacetic acid
CAS Number: 500577-51-5
Molecular Formula: C₂₉H₄₂F₃N₉O₉
Molecular Weight: 717.694
Catalog: Signaling Pathways Cytoskeleton Integrin
Create Date: 2019-03-10 16:17:23
Modify Date: 2024-04-02 11:28:07
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].

Name	Cyclo (-RGDfK) 2,2,2-Trifluoroacetic acid
Synonyms	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)

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.