Fenbendazole 是一种口服有效的苯并咪唑类驱虫剂,具有广泛的抗寄生虫活性。Fenbendazole 是一种微管去稳定剂,主要通过与微管蛋白结合并破坏微管蛋白微管平衡来作用于蠕虫。Fenbendazole 稳定转录激活因子HIF-1α。Fenbendazole 具有有效的抗增殖活性并诱导细胞凋亡。Fenbendazole 导致细胞周期停滞和有丝分裂细胞死亡,并对野生型 p53 异种移植小鼠具有抗肿瘤活性。
生物活性 | Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broadantiparasiticrange. Fenbendazole is amicrotubule destabilizingagent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activatorHIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and inducesapoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1]. |
体外研究 (In Vitro) | 芬苯达唑 (1 uM; 24 小时) 在野生型 p53 的人非小细胞肺癌 (NSCLC) 的肿瘤细胞系 (H460 和 A549) 中显着抑制细胞生长[1]。 芬苯达唑 (1 uM; 24 小时) 诱导细胞凋亡并导致线粒体 p53 蛋白水平升高[1]。 芬苯达唑 (1 uM; 24 小时) 可以引起人 NSCLC 细胞的有丝分裂期细胞的周期停滞[1]。 芬苯达唑 (1 uM; 24 小时) 可以导致 A549 细胞微管网络的部分改变[1]。
Cell Cycle Analysis[1] Cell Line: | A549 cells | Concentration: | 1 uM | Incubation Time: | For 24 h | Result: | Caused an early elevation of cyclin B1/CDK1 levels (8 h as compared to 16 h in case of control untreated cells). p-histone H3 (Ser10) was found to be up-regulated at 12 and 24 h. |
Apoptosis Analysis[1] Cell Line: | A549 cells | Concentration: | 1 uM | Incubation Time: | 8, 16, 24, 32, 40, 48 h | Result: | The number of apoptotic cells increased in a time dependent manner with simultaneous decrease in cyclin B1 levels, and ~30% cells had undergone apoptosis after 32 h. |
Western Blot Analysis[1] Cell Line: | H460 cells | Concentration: | 1 uM | Incubation Time: | For 24 h | Result: | Caused an increased level of p53 protein in the mitochondrial fraction. |
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体内研究 (In Vivo) | 芬苯达唑 (1 mg; 口服; 每隔一天一次; 持续 12 天) 可显着减小肿瘤大小和重量[1]。
Animal Model: | Female athymic nu/nu mice were xenografted with A549 cells[1] | Dosage: | 1 mg/mouse | Administration: | Orally; every second day for 12 day | Result: | Led to a marked reduction in tumour size and weight. Led to a reduction in hemoglobin content in tumors signifying reduced tumor vascularity. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 10 mg/mL(33.41 mM;Need ultrasonic) H2O : 1 mg/mL(3.34 mM;ultrasonic and warming and heat to 80℃) 配制储备液 1 mM | 3.3406 mL | 16.7029 mL | 33.4057 mL | 5 mM | 0.6681 mL | 3.3406 mL | 6.6811 mL | 10 mM | 0.3341 mL | 1.6703 mL | 3.3406 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1 mg/mL (3.34 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (3.34 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1 mg/mL (3.34 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (3.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在本网站选购。 |