Cilengitide

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Chemical Structure| 188968-51-6 同义名 : EMD 121974; EMD-85189; EMD-12192
CAS号 : 188968-51-6
货号 : A142071
分子式 : C27H40N8O7
纯度 : 99%+
分子量 : 588.66
MDL号 : MFCD04307743
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Integrins are heterodimeric transmembrane receptors involved in a wide range of cancer cell activities. Cilengitide is a selective and potent inhibitor of αv integrins that blocks the ligation of αvβ3 and αvβ5 integrins to provisional matrix proteins[5]. The IC50 values of cilengitide against αvβ3 and αvβ5 are 4.1 nM and 79 nM, respectively[6]. In primary human brain capillary endothelial cells (BCECs), incubation with 1 μg/mL cilengitide for 1h decreased cell adhesion to vitronectin. When cilengitide was added 1h after the attachment of BCECs to vitronectin, the detachment occurred in a dose-dependent manner, and the significant detachment was observed at the concentration of 10 μg/mL or higher. In αv-integrin-expressing tumor cell lines U87MG and DAOY, the exposure of 25 μg/ml cilengitide for 24h led to a significant increase in apoptosis compared to cells treated with control peptide. In a mouse xenograft model established by injecting αv-positive melanoma cells into the forebrain, Cilengitide treatment resulted in an average survival of 36.5 days compared to 17.3 days in the control peptide-treated animals[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.49mL

1.70mL

0.85mL

16.99mL

3.40mL

1.70mL
参考文献

[1]Dolgos H, Freisleben A, et al. In vitro and in vivo drug disposition of cilengitide in animals and human. Pharmacol Res Perspect. 2016 Mar 17;4(2):e00217.

[2]Wilisch-Neumann A, Kliese N, et al. The integrin inhibitor cilengitide affects meningioma cell motility and invasion. Clin Cancer Res. 2013 Oct 1;19(19):5402-12.

[3]Reardon DA, Cheresh D. Cilengitide: a prototypic integrin inhibitor for the treatment of glioblastoma and other malignancies. Genes Cancer. 2011 Dec;2(12):1159-65. doi: 10.1177/1947601912450586. PMID: 22866207; PMCID: PMC3411133.

[4]Nisato RE, Tille JC, Jonczyk A, Goodman SL, Pepper MS. alphav beta 3 and alphav beta 5 integrin antagonists inhibit angiogenesis in vitro. Angiogenesis. 2003;6(2):105-19. doi: 10.1023/B:AGEN.0000011801.98187.f2. PMID: 14739617.

[5]Taga T, Suzuki A, Gonzalez-Gomez I, Gilles FH, Stins M, Shimada H, Barsky L, Weinberg KI, Laug WE. alpha v-Integrin antagonist EMD 121974 induces apoptosis in brain tumor cells growing on vitronectin and tenascin. Int J Cancer. 2002 Apr 10;98(5):690-7. doi: 10.1002/ijc.10265. PMID: 11920637.