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Description: Eribulin (E-7389; Halaven; B1939; ER-086526; Eisai), a synthetic analogue of the marine-originated natural product halichondrin B, is an antitubulin/microtubule targeting agent (MTA)/mitotic/tubulin inhibitor approved for use in the treatment of metastatic breast cancer. Eribulin (E7389) inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
| ln Vitro |
Eribulin (1-100 nM; 72 h) suppresses cell growth with IC50 values of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively [1]. Eribulin (10-50 nM; 12-72 hours) significantly promotes early apoptosis in LM8 cells given at a dosage of 50 nM for 24 hours [1]. In LM8 cells, eribulin (10-50 nM; 12-72 hours) produced G2/M arrest at 50 nM for 12 hours, while long-term treatment (72 hours) at 10 nM Does not induce G2/M phase arrest[1]. Eribulin (1-50 nM; 12 hours) does not promote senescence in LM8 cells [1]. Eribulin (1-10 nM; 16 hours) produces morphological alterations and inhibits cell migration at low concentrations in LM8 cells [1].
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| ln Vivo |
Eribulin (1 mg/kg; intravenously injected once weekly for 2 weeks) inhibits initial tumor development and lung metastasis of osteosarcoma in rats [1]. At low doses, eribulin (1 mg/kg; intravenously administered once) suppresses the development of circulating tumor cells (CTCs) [1].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: LM8 cells and Dunn cells Tested Concentrations: 0, 1, 10, 100 nM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of cell proliferation in a dose-dependent manner. Apoptosis analysis [1] Cell Types: LM8 cells Tested Concentrations: 0, 10, 50 nM Incubation Duration: 12, 24, 48, 72 hrs (hours) Experimental Results: 50 nM concentration induced early apoptosis after 12 hrs (hours). No apoptosis was detected at 10 nM concentration. Cell cycle analysis[1] Cell Types: LM8 Cell Tested Concentrations: 0, 10, 50 nM Incubation Duration: 12, 24, 48, 72 hrs (hours) Experimental Results: Treatment with 50 nM for 12 hrs (hours) induces G2/M arrest. 10 nM treatment did not induce G2/M arrest. |
| Animal Protocol |
Animal/Disease Models: C3H/HeN mice (4 weeks old) were injected with LM8 cells [1]
Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection once a week for 2 weeks Experimental Results: Inhibited primary tumor growth and induced tumor cell apoptosis Death. Reduce lung metastasis. Lost weight. |
| References |
[1]. Watanabe K, et, al. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo. Oncotarget. 2019 Jan 4; 10(2): 161-174.
[2]. Okouneva, T., et al., Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase. Mol Cancer Ther, 2008. 7(7): p. 2003-11. [3]. Smith, J.A., et al., Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability. Biochemistry, 2010. 49(6): p. 1331-7. [4]. Towle, M.J., et al., Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res, 2011. 71(2): p. 496-505. |
| Molecular Formula |
C₄₀H₅₉NO₁₁
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|---|---|
| Molecular Weight |
729.90
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| CAS # |
253128-41-5
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| Related CAS # |
Eribulin mesylate;441045-17-6
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| SMILES |
C=C1C[C@@](CC[C@@]2(C[C@@]3([H])O4)O[C@]([C@](O[C@](C5)([H])CC6)([H])[C@@]6([H])O7)([H])[C@@]4([H])[C@]7([H])[C@@]3([H])O2)([H])O[C@@]1([H])CC[C@](C[C@@H](C)C8=C)([H])O[C@]8([H])C[C@@](O[C@H](C[C@H](O)CN)[C@@H]9OC)([H])[C@]9([H])CC5=O
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| Synonyms |
B1939 E7389 ER086526B 1939 E 7389 ER 086526B-1939 E-7389 ER-086526
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~274.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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