Cyclo(RGDyK) is a highly potent and selective inhibitor for the αvβ3integrin with a IC50 of 0.94 nM.
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HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International
Integrins are heterodimeric transmembrane glycoproteins that play key roles in cell matrix interactions during angiogenesis and tumor invasion. Cyclo(RGDyK) is a potent and selective inhibitor of αvβ3 integrin with an IC50 value of 20 nM. The inhibitory activity of cyclo(RGDyK) against αIIbβ3 and αvβ5 were much lower with IC50 values of 3 μM and 4 μM, respectively[3]. The conjugation of cyclo(RGDyK) to PEG-b-PLAG micelles (TPM) facilitated the uptake of Dil into murine melanoma cells B16-F10 and human umbilical vein endothelial cells (HUVECs) through integrin-mediated endocytosis, as compared to cyclo(RGDyK)-free micelles (NPM). Also, paclitaxel-loaded TPM showed higher cytotoxicity and antiproliferation activities against both cell lines in vitro compared to paclitaxel-loaded NPM. The IC50 values of paclitaxel-loaded TPM against B16-F10 cells and HUVECs were 29.28 nM and 1.217 nM, respectively[4]. In apoE-/- mice, the intravenous injection of 1nmol cyclo(RGDyK)-Cy5.5 inhibited the increase of αvβ3 integrin expression in atherosclerotic carotid arteryYao Y, Jiang Y, Sheng Z, Zhang Y, An Y, Yan F, Ma G, Liu N, Teng G, Cheng Z. Analysis of in situ and ex vivo αVβ3 integrin expression during experimental carotid atherogenesis. Int J Nanomedicine. 2012;7:641-9. doi: 10.2147/IJN.S28065. Epub 2012 Feb 8. PMID: 22334786; PMCID: PMC3278228..
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