Eribulin mesylate
Based on 8 publication(s) in Google Scholar
Eribulin mesylate is an inhibitor for microtubule. Eribulin mesylate inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate exhibits antitumor efficacy in mouse model.
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- 純度: 98.97%
- CAS 番号: 441045-17-6
- 分子式: C41H63NO14S
- 分子量:826.00
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Eribulin mesylate
More- J Control Release. 2025 Oct 14;388(Pt 1):114325. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Dev Cell. 2025 Mar 25:S1534-5807(25)00151-0. [Abstract]
- NPJ Breast Cancer. 2025 Feb 17;11(1):17. [Abstract]
- mBio. 2025 Aug 15:e0048425. [Abstract]
- Molecules. 2025 Feb 14;30(4):895. [Abstract]
- iScience. 2022 Sep 6;25(10):105081. [Abstract]
- Res Sq. 2024 Sep 17.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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Apoptosis Analysis
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In Vivo Efficacy Study
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Cell Imaging/Staining
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MES-SA | IC50 |
1.66 nM
Compound: Halaven
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Antiproliferative activity against human MES-SA cells
Antiproliferative activity against human MES-SA cells
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[PMID: 21324687] |
| MES-SA | IC50 |
1.7 nM
Compound: 1
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Cytotoxicity against human MES-SA cells
Cytotoxicity against human MES-SA cells
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[PMID: 23141916] |
| SF-295 | IC50 |
27.85 nM
Compound: Halaven
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Antiproliferative activity against human SF295 cells
Antiproliferative activity against human SF295 cells
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[PMID: 21324687] |
| U-251 | IC50 |
5.87 nM
Compound: Halaven
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Antiproliferative activity against human U251 cells
Antiproliferative activity against human U251 cells
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[PMID: 21324687] |
Eribulin mesylate (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 mesylate (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 mesylate (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 mesylate (1-50 nM; 12 h) does not induce senescence in LM8 cells[1].
Eribulin mesylate (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LM8 cells and Dunn cells
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Concentration:0, 1, 10, 100 nM
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Incubation Time:72 hours
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Result:Inhibited cells proliferation in a dose-dependent manner.
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Cell Line:LM8 cells
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Concentration:0, 10, 50 nM
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Incubation Time:12, 24, 48, 72 hour
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Result:Induced early apoptosis after 12 h at the concentration of 50 nM.
Not detected apoptosis at the concentration of 10 nM.
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Cell Line:LM8 cells
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Concentration:0, 10, 50 nM
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Incubation Time:12, 24, 48, 72 hour
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Result:Induced G2/M arrest by 12 h treatment with 50 nM.
No G2/M arrest was induced by10 nM treatment.
Eribulin mesylate (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeN mice (4-week-old) are injected LM8 cells[1]
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Dosage:1 mg/kg
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Administration:I.v. once a week for 2 weeks
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Result:Suppressed primary tumor growth and induced apoptosis in tumor cells.
Reduced lung metastasis.
化学情報
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CAS 番号 441045-17-6
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性状 Solid
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分子量 826.00
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分子式 C41H63NO14S
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Color White to off-white
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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.CS(=O)(O)=O
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別名
B1939 mesylate; E7389 mesylate; ER-086526 mesylate
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輸送条件
Shipping with dry ice.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (8)
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Journal Impact Factor
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Most Recent
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J Control Release
Improved biodistribution and antitumor effects of a Nectin4 and Trop2 bispecific fatty acid-modified nanobody conjugate. [Abstract]2025 Oct 14;388(Pt 1):114325. PMID: 41101697 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Dev Cell
2025 Mar 25:S1534-5807(25)00151-0. PMID: 40157365
Eribulin mesylate purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Mar 25:S1534-5807(25)00151-0. [Abstract]
Eribulin (0-210 nM; 72 h). Cell viability of 4T1 S1, R4, and R8 cells following treatments of Eribulin for 72 h.
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NPJ Breast Cancer
Development and validation of a functional ex vivo paclitaxel and eribulin sensitivity assay for breast cancer, the REMIT assay. [Abstract]2025 Feb 17;11(1):17. PMID: 39962055
Eribulin mesylate purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2025 Feb 17;11(1):17. [Abstract]
Eribulin (1 nM; 72 h). Microscopic images of EdU (pink) and DAPI (blue) channels for two selected models: HBCx-4B and HBCx-39.
Eribulin mesylate purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2025 Feb 17;11(1):17. [Abstract]
Eribulin (1 nM; 72 h). Quantification of HBCx-4B and HBCx-39 TUNEL staining. Each data point represents quantification of the percentage of cells in apoptosis within one microscopic field of view; ten fields of view were analyzed per condition in triplicate.
Eribulin mesylate purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2025 Feb 17;11(1):17. [Abstract]
Eribulin (0.4 mg/kg; IV). Results of the in vivo eribulin treatment of the HBCx-137 PDX model, representing the measurements of the tumor size in mm3 over the time in culture.
Eribulin mesylate purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2025 Feb 17;11(1):17. [Abstract]
Eribulin (1 nM; 72 h). Representative images of the pH3- (green) and EdU-positive (pink) cells with and without Eribulin treatment for the HBCx-137 PDX model (Eribulin-sensitive in vivo).
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mBio
2025 Aug 15:e0048425. PMID: 40815147 -
Molecules
Small Molecules Identified by an In Silico Docking Screen Targeting Anaphase-Promoting Complex/Cyclosome Subunit 1 (APC1) Potentiate Paclitaxel-Induced Breast Cancer Cell Death. [Abstract]2025 Feb 14;30(4):895. PMID: 40005207 -
iScience
Multiomic characterization and drug testing establish circulating tumor cells as an ex vivo tool for personalized medicine. [Abstract]2022 Sep 6;25(10):105081. PMID: 36204272 -
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (121.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (285 KB)
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SDS (394 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. 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. [Content Brief]
[3]. Okouneva, T., et al., Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase. Mol Cancer Ther, 2008. 7(7): p. 2003-11. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2107 mL | 6.0533 mL | 12.1065 mL | 30.2663 mL |
| 5 mM | 0.2421 mL | 1.2107 mL | 2.4213 mL | 6.0533 mL | |
| 10 mM | 0.1211 mL | 0.6053 mL | 1.2107 mL | 3.0266 mL | |
| 15 mM | 0.0807 mL | 0.4036 mL | 0.8071 mL | 2.0178 mL | |
| 20 mM | 0.0605 mL | 0.3027 mL | 0.6053 mL | 1.5133 mL | |
| 25 mM | 0.0484 mL | 0.2421 mL | 0.4843 mL | 1.2107 mL | |
| 30 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.0089 mL | |
| 40 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL | |
| 50 mM | 0.0242 mL | 0.1211 mL | 0.2421 mL | 0.6053 mL | |
| 60 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL | |
| 80 mM | 0.0151 mL | 0.0757 mL | 0.1513 mL | 0.3783 mL | |
| 100 mM | 0.0121 mL | 0.0605 mL | 0.1211 mL | 0.3027 mL |
Eribulin mesylate 関連分類
HY-13442A 関連分類
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