product name Cyclo(RGDyK)
Description: Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 NM. 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.
References: J Nucl Med. 2001 Feb;42(2):326-36; J Drug Target. 2011 Jan;19(1):25-36.
847.72
Formula
C31H43F6N9O12
CAS No.
250612-42-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (118.0 mM)
Water: 100 mg/mL (118.0 mM)
Ethanol: 20 mg/mL (23.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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: 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. |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Nucl Med. 2001 Feb;42(2):326-36; J Drug Target. 2011 Jan;19(1):25-36. |
