Cyclo (-RGDfK)

Catalog No.S7834

For research use only.

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

Cyclo (-RGDfK) Chemical Structure

CAS No. 500577-51-5

Selleck's Cyclo (-RGDfK) has been cited by 7 Publications

Purity & Quality Control

Choose Selective Integrin Inhibitors

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]

Protocol (from reference)

Kinase Assay:[6]
  • 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

Chemical Information

Molecular Weight 717.69


CAS No. 500577-51-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from, updated on 2022-01-17)

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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