CAS:250612-42-1Cyclo(RGDyK)

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Cyclo(RGDyK) is a highly potent and selective inhibitor for the αvβ3 integrin with a IC50 of 0.94 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

250612-42-1

储存条件

分子式

C31H43F6N9O12

运输

蓝冰

分子量

847.72

别名

溶解度

DMSO	100.0 mg/mL (118.0 mM)
Ethanol	20.0 mg/mL (23.6 mM)

动物实验配方

生物活性

靶点 Integrin αvβ3

IC50:20nM
描述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. 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. In apoE^-/- mice, the intravenous injection of 1nmol cyclo(RGDyK)-Cy5.5 inhibited the increase of αvβ3 integrin expression in atherosclerotic carotid artery.