CYCLO (ARG-GLY-ASP-D-PHE-LYS) Chemical Properties

Melting point:

191℃ (decomposition)

Density 

1.47±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥30.19 mg/mL in DMSO; insoluble in EtOH; ≥59.2 mg/mL in H2O

form 

Powder

pka

4.01±0.10(Predicted)

color 

White to off-white

Sequence

Cyclo(Arg-Gly-Asp-Phe-Lys)

InChIKey

NVHPXYIRNJFKTE-HAGHYFMRSA-N

SMILES

[C@@H]1(NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC1=O)CC1C=CC=CC=1

CYCLO (ARG-GLY-ASP-D-PHE-LYS) Usage And Synthesis

Uses

Cyclo (-RGDfK) Trifluoroacetic Acid Salt is a potent inhibitor of αvβ3 integrin. Used in tumor therapy due to the targeting of the VEGFR2 gene by sRNA.

Biological Activity

in one study where this peptide was labeled with 125i, it was found to bind specifically and with high affinity to αvβ3 receptors on neovascular blood vessel sections of different major human cancers. the integrin alpha(iib)beta(3)-specific cyclic hexapeptide contains an arg-gly-asp (rgd) sequence.

target

Integrin

IC 50

αvβ3: 0.94 nM (IC₅₀)