Cyclo(-RGDfK) TFACyclo(-RGDfK) TFA
MedChemExpress (MCE)
HY-P0023A
500577-51-5
99.82%
Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
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].
αvβ3 0.94 nM (IC50)
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[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. [Content Brief]
[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. [Content Brief]