Cilengitide

CAS号

188968-51-6

分子式

C27H40N8O7

主要靶点

Autophagy|Integrin

仅限科研使用

Cat No : CM04773

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Synonyms

inhibit|Inhibitor|Integrin|integrins|αVβ3 integrin|αVβ5 integrin|ανβ3|ανβ5|Vitronectin|西仑吉肽|Cilengitide|Autophagy|EMD 121974|EMD121974|EMD-121974



产品信息

CAS号 188968-51-6
分子式 C27H40N8O7
主要靶点 Autophagy|Integrin
主要通路 细胞骨架|自噬
分子量 588.66
纯度 99.8%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Inhibitor|Integrin|integrins|αVβ3 integrin|αVβ5 integrin|ανβ3|ανβ5|Vitronectin|西仑吉肽|Cilengitide|Autophagy|EMD 121974|EMD121974|EMD-121974

靶点活性

αvβ5:79 nM|αvβ3:4.1nM

溶解度

H2O:7.69 mg/mL (13.06 mM);DMSO:45.45 mg/mL (77.21 mM)

细胞实验

Cilengitide is supplied as an apyrogenic sterile infusion solution in physiological saline. Cilengitide is diluted in saline to a concentration of 1 mM[2]. The cytotoxicity of the two drugs, Belotecan and Cilengitide, is measured by the Cell Counting Kit-8 (CCK-8). U87 mg and U251 mg cells are seeded in 96 well plates at a density of 4×103 cells per well to allow for adhesion overnight. After this, the cells are treated with Cilengitide at a concentration of 0, 0.1, 0.5, 1, 5 and 25 μM and Belotecan at a concentration of 0, 6.25, 12.5, 25, 50 and 100 nM. All possible combinations of concentrations are used to assess the combined therapeutic effect of Cilengitide and Belotecan. After 3 days, 10 μL of the CCK-8 solution is added to each well of the plate, and the plate is incubated for 3 hr in the incubator (37°C; 5% CO2). The optical density (OD) of the sample plate is measured at 450 nm in a microplate reader. The viability of tumor cells is assessed by calculating the OD ratio of the specific OD in each sample to that of the control. Each experiment is conducted in quadruplicate. The values are averaged and normalized against the controls to generate dose-response curves[2].

参考文献

1.Hariharan S, et al. Assessment of the biological and pharmacological effects of the alpha nu beta3 and alpha nu beta5 integrinreceptor antagonist, Cilengitide (EMD 121974), in patients with advanced solid tumors. Ann Oncol. 2007 Aug;18(8):1400-7.
2.Kim YH, et al. Combination therapy of cilengitide with belotecan against experimental glioblastoma. Int J Cancer. 2013 Aug 1;133(3):749-56.
3.ten Hagen, T., Seynhaeve, A., de Wiel-Ambagtsheer, G., de Bruijn, E., van Tiel, S., & Ruegg, C. et al. (2012). The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model.?International Journal Of Cancer,?132(11), 2694-2704. doi: 10.1002/ijc.27940

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