Cyclo (-RGDfK)

Catalog No.S7834 Batch:S783404

Technical Data

Formula	C₂₉H₄₂F₃N₉O₉
Molecular Weight	717.69	CAS No.	500577-51-5
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (139.33 mM)
		Water	100 mg/mL (139.33 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (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]

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 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.}}

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 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.}}

References

+ Expand

Selleck's Cyclo (-RGDfK) has been cited by 10 publications

SPARC Aggravates Blood-Brain Barrier Disruption via Integrin [ Oxidative Medicine and Cellular Longevity, 2021, 10.1155/2021/9739977]	PubMed: None
SPARC Aggravates Blood-Brain Barrier Disruption via Integrin αVβ3/MAPKs/MMP-9 Signaling Pathway after Subarachnoid Hemorrhage [ Oxid Med Cell Longev, 2021, 2021:9739977]	PubMed: 34804372
Integrin αv and Vitronectin Prime Macrophage-Related Inflammation and Contribute the Development of Dry Eye Disease [ Int J Mol Sci, 2021, 22(16)8410]	PubMed: 34445121
MOB2 suppresses GBM cell migration and invasion via regulation of FAK/Akt and cAMP/PKA signaling. [ Cell Death Dis, 2020, 14;11(4):230]	PubMed: 32286266
MiR-30 family prevents uPAR-ITGB3 signaling activation through calcineurin-NFATC pathway to protect podocytes [ Cell Death Dis, 2019, 10(6):401]	PubMed: 31127093
CCN1 interlinks integrin and hippo pathway to autoregulate tip cell activity. [ Elife, 2019, 8]	PubMed: 31429823
Tension enhances cell proliferation and collagen synthesis by upregulating expressions of integrin αvβ3 in human keloid-derived mesenchymal stem cells [Song H Life Sci, 2019, 219:272-282]	PubMed: 30597173
Acquired Resistance to EGFR TKIs Mediated by TGFβ1/Integrin β3 Signaling in EGFR-Mutant Lung Cancer [ Mol Cancer Ther, 2019, 18(12):2357-2367]	PubMed: 31501278
Acquired resistance to EGFR TKIs mediated by TGF-beta1/integrin beta3 signaling in EGFR-mutant lung cancer. [ Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0181]	PubMed: 31501278
Spontaneous Extracellular Matrix Accumulation in a Human in vitro Model of Renal Fibrosis Is Mediated by αV Integrins [ Nephron, 2019, 10.1159/000499506]	PubMed: 31048591

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