Eribulin (E7389) 是靶向微管 (microtubule) 的抗癌剂，其用于研究转移性乳腺癌。Eribulin 通过结合微管蛋白和微管来抑制癌细胞的增殖。
| 生物活性 | Eribulin (E7389) is amicrotubuletargeting agent that is used for the research of metastatic breastcancer. Eribulin inhibits the proliferation ofcancercells by binding microtubule proteins and microtubules. |
体外研究
(In Vitro) | Eribulin (1-100 nM; 72 h) inhibits cells proliferation, with IC50s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively[1].
Eribulin (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells[1].
Eribulin (10-50 nM; 12-72 h) induces G2/M arrest by 12 h treatment with at the dose of 50 nM, but not by long-term treatment (72 h) with 10 nM in LM8 cells[1].
Eribulin (1-50 nM; 12 h) does not induce senescence in LM8 cells[1].
Eribulin (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells[1].
Cell Proliferation Assay[1] | Cell Line: | LM8 cells and Dunn cells | | Concentration: | 0, 1, 10, 100 nM | | Incubation Time: | 72 hours | | Result: | Inhibited cells proliferation in a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | LM8 cells | | Concentration: | 0, 10, 50 nM | | Incubation Time: | 12, 24, 48, 72 hours | | Result: | Induced early apoptosis after 12 h at the concentration of 50 nM.
Not detected apoptosis at the concentration of 10 nM. |
Cell Cycle Analysis[1] | Cell Line: | LM8 cells | | Concentration: | 0, 10, 50 nM | | Incubation Time: | 12, 24, 48, 72 hours | | Result: | Induced G2/M arrest by 12 h treatment with 50 nM.
No G2/M arrest was induced by10 nM treatment. |
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体内研究
(In Vivo) | Eribulin (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice[1].
Eribulin (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase[1].
| Animal Model: | C3H/HeN mice (4-week-old) are injected LM8 cells[1] | | Dosage: | 1 mg/kg | | Administration: | I.v. once a week for 2 weeks | | Result: | Suppressed primary tumor growth and induced apoptosis in tumor cells.
Reduced lung metastasis.
Decreased the body weights. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(274.01 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3701 mL | 6.8503 mL | 13.7005 mL | | 5 mM | 0.2740 mL | 1.3701 mL | 2.7401 mL | | 10 mM | 0.1370 mL | 0.6850 mL | 1.3701 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 (protect from light, stored under nitrogen)。-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: ≥ 5 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (6.85 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.85 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 50.0 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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