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Cilengitide TFA

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Chemical Structure| 199807-35-7 同义名 : NSC 707544;EMD 121974;Cilengitide trifluoroacetate;EMD 121974 TFA
CAS号 : 199807-35-7
货号 : A253683
分子式 : C29H41F3N8O9
纯度 : 99%+
分子量 : 702.679
MDL号 : MFCD22665738
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 100 mg/mL(142.31 mM)
动物实验配方：

PO 0.5% CMC-Na 40 mg/mL clear

生物活性
靶点

  • Integrin

    αvβ3 receptor, IC50:4.1 nM

    αvβ5 receptor, IC50:79 nM
描述 Cilengitide (EMD 121974) is an antagonist for αvβ3 and αvβ5 integrin receptors. It effectively blocks the adhesion of human melanoma M21 and UCLA-P3 human lung carcinoma cell lines to vitronectin, demonstrating inhibitory concentrations (IC50s) of 0.4 μM for both[1]. Exposure to Cilengitide at concentrations above 1 µM induces cytotoxic effects that are both concentration- and time-dependent[2]. Exposure to Cilengitide at concentrations above 1 µM induces cytotoxic effects that are both concentration- and time-dependent[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CAL27 6.25–200 µM Growth Inhibition Assay 72 h results moderate, dose-dependent growth inhibition 24557056
CAL27 25 µM  Apoptosis Assay 48 h  induces apoptosis 24557056
FaDu 6.25–200 µM Growth Inhibition Assay 72 h results moderate, dose-dependent growth inhibition 24557056
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.42mL

0.28mL

0.14mL

7.12mL

1.42mL

0.71mL

14.23mL

2.85mL

1.42mL
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 TL, et al. The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model. Int J Cancer. 2012 Nov 13.