Home Cytoskeletal Signaling Integrin inhibitor Cyclo (-RGDfK) For research use only.

Cyclo (-RGDfK)

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

Cyclo (-RGDfK) Chemical Structure

Cyclo (-RGDfK) Chemical Structure

CAS: 500577-51-5

Selleck's Cyclo (-RGDfK) has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

Cyclo (-RGDfK) Related Products

Signaling Pathway

Integrin Signaling Pathways

Integrin Signaling Pathway

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Biological Activity

Description Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor.
Targets
αvβ3 integrin [1]
In vitro
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]
Kinase Assay 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.
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05314543 Recruiting
Healthy Volunteers|Performance
Centre Hospitalier Universitaire de Saint Etienne
 November 29 2021 Not Applicable
NCT04680793 Completed
Ehlers-Danlos Syndrome
Hakimi Adrien|Clinique de la Mitterie
 September 22 2020 Not Applicable

Chemical Information & Solubility

Molecular Weight 717.69 Formula

C29H42F3N9O9
CAS No. 500577-51-5 SDF Download Cyclo (-RGDfK) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (139.33 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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