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Cyclo(-Arg-Gly-Asp-D-Phe-Lys) trifluoroacetate salt

Names

[ CAS No. ]:
161552-03-0

[ Name ]:
Cyclo(-Arg-Gly-Asp-D-Phe-Lys) trifluoroacetate salt

[Synonym ]:
Cyclo (-RGDfK)
c(D-Phe-Lys-Arg-Gly-Asp)
A8164
Cyclo(L-arginylglycyl-L-α-aspartyl-D-phenylalanyl-L-lysyl)
cyclo-[Arg-Gly-Asp-D-Phe-Lys]
Cyclo[L-α-aspartyl-D-phenylalanyl-L-lysyl-N-(diaminomethylene)-L-ornithylglycyl]
cyclic-RGD peptide
cyclo[RGD-{D-F}-K]
cyclo(RGDfK)
Cyclo-RGDfK

Biological Activity

[Description]:

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Sequence: Cyclo(Arg-Gly-Asp-Phe-Lys).

[Related Catalog]:

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

[Target]

IC50: 0.94 nM (αvβ3 integrin)[1].


[In Vitro]

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with a IC50 of 0.94 nM[1]. [(66)Ga]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.


[Related Small Molecules]

Cilengitide | Arg-Gly-Asp-Ser | CWHM-12 | OSU-T315 | E 7820 | GLPG 0187 | Firategrast | ATN-161 trifluoroacetate salt | Cucurbitacin B | Eptifibatide acetate salt | iRGD peptide | Lifitegrast | Zaurategrast | Integrin Antagonist 1 (hydrochloride) | TR 14035

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C27H41N9O7

[ Molecular Weight ]:
603.670

[ Exact Mass ]:
603.312866

[ PSA ]:
288.17000

[ LogP ]:
-3.10

[ Index of Refraction ]:
1.666

[ Storage condition ]:
-20°C

Synthetic Route

Click to get detail synthetic route

Related Compounds

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