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.
理化性质和储存条件
| Molecular Weight (MW) | 847.72 |
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| Formula | C31H43F6N9O12 |
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| CAS No. | 250612-42-1 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 100 mg/mL (118.0 mM) |
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| Water: 100 mg/mL (118.0 mM) |
| Ethanol: 20 mg/mL (23.6 mM) |
| 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 | Cyclo(RGDyK) trifluoroacetate |
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实验参考方法
| In Vitro | In vitro activity: Cyclo(RGDyK), a glycosylated RGD-containing peptide (RGD-peptide), is a potent and selective αVβ3 integrin inhibitor with 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. Cyclo(RGDyK) shows high affinity and selectivity for αVβ3 over αVβ5 and αIIbβ3. Cyclo(RGDyK)-conjugated micelles (TPM) facilitated the cell-specific uptake of DiI into B16-F10 cells and HUVECs via integrin-mediated endocytosis compared with Cyclo(RGDyK) -free micelles (NPM).
Kinase Assay: yclo(RGDyK) (c(RGDyK(SAA)) shows high affinity and selectivity for αVβ3 over αVβ5 (IC50=4000 nM) and αIIbβ3 (IC50=3000 nM)
Cell Assay: Cyclo(RGDyK) conjugation facilitated intracellular drug delivery of polymeric micelles to neovasculature (HUVECs) and tumor cells in which integrin is overexpressed. In addition, Cyclo(RGDyK) showed high affinity and selectivity for αVβ3 integrin over αVβ5 and αIIbβ3. |
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| In Vivo | In apoE–/– mice, Cyclo(RGDyK) (1 nmol, i.v.) inhibits the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery. |
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| Animal model | apoE–/– mice |
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| Formulation & Dosage | 1 nmol, i.v. |
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| References | J Nucl Med. 2001 Feb;42(2):326-36; J Drug Target. 2011 Jan;19(1):25-36. |
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