Filanesib (ARRY-520) 是一种选择性的，非竞争性的纺锤体驱动蛋白 (KSP) 抑制剂，对人 KSP 作用的IC50值为 6 nM。Filanesib 在体外能通过诱导自噬 (apoptosis) 导致细胞死亡。Filanesib 具有高效的抗增生活性。
| 生物活性 | Filanesib (ARRY-520) is a selective and noncompetitivekinesinspindle protein (KSP) inhibitor, with anIC50of 6 nM for human KSP. Filanesib induces cell death byapoptosisin vitro. Filanesib has potent anti-proliferative activity[1]. |
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体外研究
(In Vitro) | Filanesib induces mitotic arrest in multiple cell lines[1].
Filanesib exhibits anti-proliferative against a broad range of human and rodent tumor cell lines, including a variety of leukemias and solid tumors, with EC50s between 0.4 nM and 14.4 nM[1].
Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells[1].
Filanesib (3.13-6.25 nM; 44 hours) causes accumulation of cells in the G2/M phase of the cell cycle in a dose-dependent manner in HeLa cells[1].
Filanesib potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells[2].
Filanesib (3 μM; 6-24 hours) is able to induce caspase-2 activation[3].
Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells[3].
Apoptosis Analysis[1] | Cell Line: | Hela cells | | Concentration: | 0.01-0.1 nM | | Incubation Time: | 36 hours | | Result: | Induced the formation of nucleosomes and activation of caspases-3 and 7. |
Cell Cycle Analysis[1] | Cell Line: | HeLa cells | | Concentration: | 0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM | | Incubation Time: | 44 hours | | Result: | Resulted in G2/M arrest. |
Western Blot Analysis[3] | Cell Line: | Type II EOC cells | | Concentration: | 3 μM | | Incubation Time: | 6 hours, 12 hours, 24 hours | | Result: | Induced caspase-2 activation in a time-dependent manner. |
Cell Cytotoxicity Assay[3] | Cell Line: | Type II EOC cell lines (A2780, CP70, 01-28) | | Concentration: | 0.003 μM, 0.03 μM, 0.3μM, 3 μM | | Incubation Time: | 24 hours , 48 hours | | Result: | Effectively decreased cell viability in a time-dependent manner in the Type II EOC cell lines. |
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体内研究
(In Vivo) | Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo[3].
| Animal Model: | Female nude mice, EOC mice xenograft model[3] | | Dosage: | 20 mg/kg, 30 mg/kg | | Administration: | Intraperitoneal injection, q4dx3 | | Result: | Induced a decrease in tumor kinetics in a dose-dependent manner. |
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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 : ≥ 100 mg/mL(237.82 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.3782 mL | 11.8912 mL | 23.7823 mL | | 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL | | 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.95 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 25.0 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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