Cyclo(-RGDfK) TFA

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Chemical Structure| 500577-51-5 同义名 : Cyclo
CAS号 : 500577-51-5
货号 : A239927
分子式 : C29H42F3N9O9
纯度 : 99%+
分子量 : 717.69
MDL号 : MFCD20488083
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(146.3 mM)，配合低频超声助溶，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: 30 mg/mL(41.8 mM)，配合低频超声助溶
生物活性
靶点

  • Integrin
描述 Integrins are membrane-spanning heterodimers that mediate cell-extracellular matrix adhesion. Cyclo(-RGDfK) Trifluoroacetate is a potent and selective inhibitor of purified αvβ3 integrin with a KD value of 41.70 nM. In HEK293 (β3) cells, incubation with 2 μM Cyclo(-RGDfK) trifluoroacetate decreased the αvβ3 intergrin lateral mobility compared to the control group. When HEK293 (β3) cells were starved for 30 min and incubated with 1 μM Cyclo(-RGDfK) trifluoroacetate-Cy5 for 10 min at room temperature, the αvβ3 integrin internalization was less extensive than that in cells treated with regioselectively addressable functionalized template-arginine-alanine-aspartic acid (RAFT-RGD). Additionally, the internalization of αvβ3 integrin in HEK293 (β3) was dose-dependently induced by RAFT-RGD, and reached 79% increase versus control group at the dose of 1 μM. On the contrary, increasing doses of cyclo(-RGDfK) trifluoroacetate (0.1 - 4 μM) did not affect the integrin internalization as compared to the control cells[3]. In athymic mice bearing αvβ3-integrin-positive C6 gliomas, administration of cyclo(-RGDfK) trifluoroacetate conjugated to 177Lu-gold nanoparticles (2MBq/0.05 mL, four times from day 1 to 21) suppressed tumor progression, tumor metabolic activity, the number of intratumoral vessels and VEGF gene expression compared to mice treated with other radiopharmaceuticals[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.97mL

1.39mL

0.70mL

13.93mL

2.79mL

1.39mL
参考文献

[1]Sancey L, Garanger E, et al. Clustering and internalization of integrin alphavbeta3 with a tetrameric RGD-synthetic peptide. Mol Ther. 2009 May;17(5):837-43.

[2]Jin ZH, Josserand V, Foillard S, Boturyn D, Dumy P, Favrot MC, Coll JL. In vivo optical imaging of integrin alphaV-beta3 in mice using multivalent or monovalent cRGD targeting vectors. Mol Cancer. 2007 Jun 12;6:41.

[3]Sancey L, Lucie S, Garanger E, Elisabeth G, Foillard S, Stéphanie F, Schoehn G, Guy S, Hurbin A, Amandine H, Albiges-Rizo C, Corinne AR, Boturyn D, Didier B, Souchier C, Catherine S, Grichine A, Alexeï G, Dumy P, Pascal D, Coll JL, Jean-Luc C. Clustering and internalization of integrin alphavbeta3 with a tetrameric RGD-synthetic peptide. Mol Ther. 2009 May;17(5):837-43. doi: 10.1038/mt.2009.29. Epub 2009 Mar 3. Erratum in: Mol Ther. 2009 Jul;17(7):1301. [multipe author names corrected]. Erratum in: Mol Ther. 2009 Jul;17(7):1301. PMID: 19259068; PMCID: PMC2760123.

[4]Vilchis-Juárez A, Ferro-Flores G, Santos-Cuevas C, Morales-Avila E, Ocampo-García B, Díaz-Nieto L, Luna-Gutiérrez M, Jiménez-Mancilla N, Pedraza-López M, Gómez-Oliván L. Molecular targeting radiotherapy with cyclo-RGDFK(C) peptides conjugated to 177Lu-labeled gold nanoparticles in tumor-bearing mice. J Biomed Nanotechnol. 2014 Mar;10(3):393-404. doi: 10.1166/jbn.2014.1721. PMID: 24730235.