Cyclo (-RGDfK)

For research use only.

Catalog No.S7834

5 publications

Cyclo (-RGDfK) Chemical Structure

CAS No. 500577-51-5

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

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Biological Activity

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

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
Formula

C29H42F3N9O9

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
NCT04041297 Recruiting Other: Preoperative Pulmonary Rehabilitation Non Small Cell Lung Cancer ADIR Association July 16 2019 --

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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.

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Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID