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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| IC50& Target[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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| Clinical Trial |
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| 分子量 |
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| 性状 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
| Powder |
-20°C |
3 years |
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4°C |
2 years |
| In solvent |
-80°C |
6 months |
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-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 |
*
请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 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
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1.
请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% 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。
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2.
请依序添加每种溶剂： 10% DMSO90% (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% DMSO90%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。
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以上所有助溶剂都可在本网站选购。
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