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。 |
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