Cyclo(RGDyK)

• CAT Number: I011870
• CAS Number: 250612-42-1
• Molecular Formula: C27 H41 N9 O8 . 2 C2 H F3 O2
• Molecular Weight: 847.72
• Purity: ≥95%
• Synonyms: Cyclo(RGDyK) trifluoroacetate;Cyclo(L-​arginylglycyl-​L-​α-​aspartyl-​D-​tyrosyl-​L-​lysyl)​, 2,​2,​2-​trifluoroacetate
• Target: Integrin
• Solubility: Soluble in DMSO
• Storage: RT
• Related CAS: 217099-14-4(free base)

Cyclo(RGDyK) (CAT: I011870) is a potent and selective inhibitor of the αVβ3 integrin, a cell surface receptor involved in cell adhesion and signaling processes. The peptide sequence RGDyK specifically targets and binds to the αVβ3 integrin, blocking its activity. By inhibiting the αVβ3 integrin, Cyclo(RGDyK) disrupts cellular interactions with the extracellular matrix and inhibits various integrin-mediated processes, such as cell adhesion, migration, and angiogenesis. Its high potency, with an IC50 of 20 nM, highlights its effectiveness in selectively targeting the αVβ3 integrin pathway.

Reference

1. J Drug Target. 2011 Jan;19(1):25-36. doi: 10.3109/10611861003663531. Epub 2010
Mar 16.

Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric
micelles to integrin-overexpressing tumor cells and neovasculature.

Yin J(1), Li Z, Yang T, Wang J, Zhang X, Zhang Q.

Author information:
(1)State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical
Sciences, Peking University, Beijing, People/’s Republic of China.

On the basis of the fact of the overexpression of integrins in malignant tumor
cells and neovasculature, and the advantage of polymeric micelles (PM) as the
drug carriers, a cyclic RGD peptide (cRGDyK) was anchored on the surface of
polyethylene glycol-b-poly(lactic-co-glycolic acid) (PEG-b-PLGA) micelles as a
ligand of integrins in order to enhance the intracellular delivery of
encapsulated hydrophobic drug into the tumor cells and its neovasculature. Toward
this goal, PEG-b-PLGA micelles without or with cRGDyK conjugation loaded with
paclitaxel (PTX) or DiI were prepared and characterized. The results revealed
that drug-loaded micelles were stable in solution, with small diameters (<80 nm)
and a low critical micelle concentration. Spectrophotofluorometry, confocal
microscopy, and flow cytometry showed that cRGDyK-conjugated micelles (TPM)
facilitated the cell-specific uptake of DiI into the murine melanoma B16-F10
cells and human umbilical vein endothelial cells (HUVEC) via integrin-mediated
endocytosis compared with cRGDyK-free micelles (NPM), and the uptake was
proportional to the ratio of cRGDyK modification in certain range. Meanwhile,
PTX-loaded TPM displayed higher cytotoxicity and antiproliferation activities
against both cells than PTX-loaded NPM. These results suggest that cRGDyK-coupled
PEG-b-PLGA micelles may be the promising intracellular targeting carriers for
efficient delivery of chemotherapeutic agents into tumor cells and
neovasculature.