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Cyclo(-RGDfK) TFA

Catalog No.S7834 Purity:99.94%

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

Cyclo(-RGDfK) TFA Chemical Structure

CAS No. 500577-51-5

Purity & Quality Control

Batch: Purity: 99.94%

99.94

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Signaling Pathway

Integrin Signaling Pathway

Biological Activity

Description

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

Targets

αvβ3 integrin ^[1]

In vitro
In vitro	The constant of affinity (K_D) 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.
Kinase Assay	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 CaCl_{2, 1 mM MgCl_{2,10 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05314543	Recruiting	Healthy Volunteers\|Performance	Centre Hospitalier Universitaire de Saint Etienne	November 29 2021	Not Applicable

References
[1] Dai XD, et al. Tetrahedron Letters. 2000, 41(33), 6295–6298. [2] Sancey L, et al. Mol Ther. 2009, 17(5), 837-843. [3] Jin ZH, et al. Mol Cancer. 2007, 6(41), 1-9. [4] Zhou D, et al. J Control Release. 2013, 169(3), 204-210. [5] Vilchis-Juárez A, et al. J Biomed Nanotechnol. 2014, 10(3), 393-404 [6] Haubner R, et al. J Nucl Med. 1999, 40(6), 1061-1071. + Expand

References

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Chemical Information & Solubility

Molecular Weight	717.69	Formula	C₂₉H₄₂F₃N₉O₉
CAS No.	500577-51-5	SDF	Download Cyclo(-RGDfK) TFA 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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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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.
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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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