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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $55 | In Stock | |
5 mg | $100 | In Stock | |
10 mg | $181 | In Stock | |
25 mg | $342 | In Stock | |
50 mg | $549 | In Stock | |
100 mg | $641 | In Stock | |
1 mL x 10 mM (in DMSO) | $153 | In Stock |
Description | Cyclo(-RGDfK) (Cyclo (-RGDfK)) is an effective and specific αvβ3 integrin inhibitor. |
Targets&IC50 | αvβ3:0.94 nM. |
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. |
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. |
Alias | Cyclo (-RGDfK) |
Molecular Weight | 603.67 |
Formula | C27H41N9O7 |
Cas No. | 161552-03-0 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 80 mg/mL (111.5 mM) Ethanol: 84 mg/mL (117.04 mM) DMSO: 100 mg/mL (139.33 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
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