Eribulin mesylate (E7389 mesylate) 是靶向微管 (microtubule) 的抗癌剂,其用于研究转移性乳腺癌。Eribulin mesylate 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 mesylate (E7389 mesylate) is amicrotubuletargeting agent that is used for the research of metastatic breastcancer. Eribulin mesylate 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 hour | 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 hour | 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.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -80°C, protect from light, stored under nitrogen |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(121.07 mM) Ethanol : ≥ 100 mg/mL(121.07 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.2107 mL | 6.0533 mL | 12.1065 mL | 5 mM | 0.2421 mL | 1.2107 mL | 2.4213 mL | 10 mM | 0.1211 mL | 0.6053 mL | 1.2107 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 (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 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 (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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 (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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 (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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。 4. 请依序添加每种溶剂: 10% EtOH 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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 EtOH 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。 5. 请依序添加每种溶剂: 10% EtOH 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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 EtOH 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 6. 请依序添加每种溶剂: 10% EtOH 90%corn oil Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.03 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 EtOH 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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