Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Cyclo(RGDyK) TFA, the trifluoroacetate (TFA) salt of Cyclo(RGDyK) which is a glycosylated RGD-containing peptide (RGD-peptide), is a potent and selective αVβ3 integrin inhibitor with potential antineoplastic activity. It inhibits αVβ3 integrin with an IC50 of 20 nM. Cyclo(RGDyK) showed high affinity and selectivity for alpha(v)beta3 in vitro (50% inhibitory concentration = 40 nmol/L). Cyclo(RGDyK) conjugation facilitated intracellular drug delivery of polymeric micelles to neovasculature (HUVECs) and tumor cells in which integrin is overexpressed. Cyclo(RGDyK) showed high affinity and selectivity for αVβ3 integrin over αVβ5 and αIIbβ3. In vivo, Cyclo(RGDyK) (1 nM, i.v. injection) blocked the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery of apoE-/- mice. The favorable biokinetics make the glycosylated RGD-peptide a promising lead structure for tracers to quantify the alpha(v)beta3 expression using PET.
ln Vitro |
High affinity and selectivity for αVβ3 are demonstrated by Cyclo(RGDyK) (c(RGDyK(SAA)) over αVβ5 (IC50=4000 nM) and αIIbβ3 (IC50=3000 nM)[1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Haubner R, et al. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001 Feb;42(2):326-36.
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Molecular Formula |
C31H43F6N9O12
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Molecular Weight |
847.72
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CAS # |
250612-42-1
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Related CAS # |
Cyclo(RGDyK);217099-14-4
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SMILES |
O=C(N[ C@H](C(N[ C@H]1CCCNC(N)=N)=O)CCCCN)[ C@H](NC([C@@H](NC(CNC1=O)=O)CC(O)=O)=O) CC2=CC=C(O)C=C2.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.1796 mL | 5.8982 mL | 11.7963 mL | |
5 mM | 0.2359 mL | 1.1796 mL | 2.3593 mL | |
10 mM | 0.1180 mL | 0.5898 mL | 1.1796 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.