Cyclo(-RGDfK) | CAS:161552-03-0

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Name:Cyclo(-RGDfK); Cyclo(RGDfK) peptide; Cyclic RGDfK peptide
Cat. No. :CS-4203
CAS No. :161552-03-0
Formula:C27H41N9O7
M. Wt. : 603.67
Solubility:DMSO: ≥ 150 mg/mL

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin.IC50 value:Target: αvβ3 integrin inhibitorin vitro: NOPO-c(RGDfK) and its Ga(III) and Cu(II) complexes showed high affinity to αvβ3 integrin (IC50 = 0.94 ± 0.06, 1.02 ± 0.09, and 0.51 ± 0.06 nM, respectively) [1]. [(66)Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μmol), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation [2].

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. Kim YS, et al. Synthesis and characterization of gadolinium-Peptidomimetic complex as an αvβ3 integrin targeted MR contrast agent. Bioorg Med Chem Lett. 2015 May 15;25(10):2056-9. 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.