Cyclo (-RGDfK)

For research use only.

Catalog No.S7834

6 publications

Cyclo (-RGDfK) Chemical Structure

CAS No. 500577-51-5

Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor.

Selleck's Cyclo (-RGDfK) has been cited by 6 publications

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Biological Activity

Description Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor.
αvβ3 integrin [1]
In vitro

The constant of affinity (KD) of Cyclo (-RGDfK-) for purified integrin is 41.70 nM.[2] Cyclo (-RGDfK) is reacting with HEK293(β3) cells moderately.[3] Cyclo(-RGDfK-) modified micelles shows strong affinity to T-24 cells and strong inhibitory effect on the proliferation of T-24 cells.[4]

In vivo In athymic mice bearing α(v)β(3)-integrin-positive C6 gliomas, Cyclo (-RGDfK-) modification induces less tumor progression, less tumor metabolic activity, fewer intratumoral vessels.[5]


Kinase Assay:[6]
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Isolated Integrin Binding Assays.:

Purified integrin (1 μg/mL; 4℃) is used to coat 96-well microtitre plates, which are then blocked with bovine serum albumin (BSA) (3% in 1 mM CaCl2, 1 mM MgCl2,10 pM MnCl2, 100 mM NaC1,50 mM trishydroxymethyl-aminomethane; pH 7.4), and incubated (3 h at 30 ℃) with biotinylated ligands (1 pg/mL in binding buffer: 0.1% BSA, 1 mM CaCl2,1 mM MgCl2, 10 μM MnCl2, 100 mM NaCl, 50 mM trishydroxymethyl-aminomethane; pH 7.4) in the presence or absence of serially diluted peptides. After washing (3×5 min with binding buffer), bound biotinylated ligand is detected with alkaline-phosphatase conjugated goat antibiotin antibodies (1 μg/mL; 1 h, 37℃), using p-nitrophenyl phosphate as chromogen. Cyclo (-RGDfK) binding in the absence of competitor is defined as 100% signal; binding to blocked wells in the absence of integrin is defined as 0%. Concentrations of Cyclo (-RGDfK) required for 50% inhibition of signal (IC50 values) are estimated graphically.

Solubility (25°C)

In vitro DMSO 100 mg/mL (139.33 mM)
Water 84 mg/mL (117.04 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 717.69


CAS No. 500577-51-5
Storage powder
in solvent
Synonyms N/A
Smiles C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CCCCN)CC2=CC=CC=C2)CC(=O)O.C(=O)(C(F)(F)F)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04680793 Enrolling by invitation Other: Rehabilitation Ehlers-Danlos Syndrome Hakimi Adrien|Clinique de la Mitterie September 22 2020 Not Applicable

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Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID