| Name | Cyclo(-RGDfK) |
| Description | Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface. |
| 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 Tris-hydroxymethyl-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 Tris-hydroxymethyl-aminomethane; pH 7.4) in the presence or absence of serially diluted peptides. After washing (3×5 min with binding buffer), the bound biotinylated ligand is detected with alkaline-phosphatase conjugated goat anti-biotin 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 vitro | Cyclo (-RGDfK-) has a high affinity for purified integrin (Kd: 41.70 nM). It is reacting with HEK293(β3) cells moderately. The micelles modified by Cyclo(-RGDfK-) show strong affinity to T-24 cells and strong inhibitory effect on the proliferation of T-24 cells. |
| In vivo | In athymic mice bearing α(v)β(3)-integrin-positive C6 gliomas, Cyclo (-RGDfK-) modification induces less tumor metabolic activity, less tumor progression, fewer intratumoral vessels. |
| Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (6.63 mM), Sonication is recommended.
H2O : 80 mg/mL (132.52 mM), Sonication is recommended.
Ethanol : 84 mg/mL (139.15 mM), Sonication is recommended.
DMSO : 100 mg/mL (165.65 mM), Sonication is recommended.
|
| Keywords | αVβ3 integrin | αvβ3 integrin | tumoral cell | -RGDfK | Microvasculature | ligand | Integrin | Inhibitor | inhibit | Cyclo(-RGDfK) | Cyclo(RGDfK) | Cyclo( RGDfK) | Cyclo | cancer |
| Inhibitors Related | K34c hydrochloride | E7820 | Arg-Gly-Asp TFA (99896-85-2(free base)) | Tirofiban hydrochloride monohydrate | Lifitegrast | Elarofiban TFA | Tirofiban | Bestatin hydrochloride | RO0270608 | ICAM-1-IN-1 | Cilengitide | Gantofiban |
| Related Compound Libraries | Macrocyclic Compound Library | Cyclic Peptide Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Peptide Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
