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Cyclo(RGDyK) trifluoroacetate

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Chemical Structure| 250612-42-1 同义名 : Cyclo(RGDyK)
CAS号 : 250612-42-1
货号 : A193345
分子式 : C31H43F6N9O12
纯度 : 99%+
分子量 : 847.717
MDL号 : MFCD20134101
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 125 mg/mL(147.45 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(117.96 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Integrin

    αVβ3 integrin, IC50:20 nM
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[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..
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.18mL

0.24mL

0.12mL

5.90mL

1.18mL

0.59mL

11.80mL

2.36mL

1.18mL
参考文献

[1]Haubner R, Wester HJ, et al. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001 Feb;42(2):326-36.

[2]Yin J, Li Z, et al. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature. J Drug Target. 2011 Jan;19(1):25-36.

[3]Haubner R, Wester HJ, Burkhart F, Senekowitsch-Schmidtke R, Weber W, Goodman SL, Kessler H, Schwaiger M. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001 Feb;42(2):326-36. PMID: 11216533.

[4]Yin J, Li Z, Yang T, Wang J, Zhang X, Zhang Q. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature. J Drug Target. 2011 Jan;19(1):25-36. doi: 10.3109/10611861003663531. Epub 2010 Mar 16. PMID: 20233083.