Eribulin mesylateCAS# 441045-17-6 |
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Quality Control & MSDS
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| Cas No. | 441045-17-6 | SDF | Download SDF |
| PubChem ID | 17755248 | Appearance | Powder |
| Formula | C41H63NO14S | M.Wt | 826.0 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | B1939 mesylate; E7389 mesylate; ER-086526 mesylate | ||
| Solubility | DMSO : ≥ 100 mg/mL (121.07 mM) Ethanol : ≥ 100 mg/mL (121.07 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-one;methanesulfonic acid | ||
| SMILES | CC1CC2CCC3C(=C)CC(O3)CCC45CC6C(O4)C7C(O6)C(O5)C8C(O7)CCC(O8)CC(=O)CC9C(CC(C1=C)O2)OC(C9OC)CC(CN)O.CS(=O)(=O)O | ||
| Standard InChIKey | QAMYWGZHLCQOOJ-WRNBYXCMSA-N | ||
| Standard InChI | InChI=1S/C40H59NO11.CH4O3S/c1-19-11-24-5-7-28-20(2)12-26(45-28)9-10-40-17-33-36(51-40)37-38(50-33)39(52-40)35-29(49-37)8-6-25(47-35)13-22(42)14-27-31(16-30(46-24)21(19)3)48-32(34(27)44-4)15-23(43)18-41;1-5(2,3)4/h19,23-39,43H,2-3,5-18,41H2,1,4H3;1H3,(H,2,3,4)/t19-,23+,24+,25-,26+,27+,28+,29+,30-,31+,32-,33-,34-,35+,36+,37+,38-,39+,40+;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Eribulin (E7389;ER-086526) mesylate is a soft sponge B analogue that inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. References: | |||||
Eribulin mesylate Dilution Calculator
Eribulin mesylate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.2107 mL | 6.0533 mL | 12.1065 mL | 24.2131 mL | 30.2663 mL |
| 5 mM | 0.2421 mL | 1.2107 mL | 2.4213 mL | 4.8426 mL | 6.0533 mL |
| 10 mM | 0.1211 mL | 0.6053 mL | 1.2107 mL | 2.4213 mL | 3.0266 mL |
| 50 mM | 0.0242 mL | 0.1211 mL | 0.2421 mL | 0.4843 mL | 0.6053 mL |
| 100 mM | 0.0121 mL | 0.0605 mL | 0.1211 mL | 0.2421 mL | 0.3027 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.
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Clinical effects of prior trastuzumab on combination eribulin mesylate plus trastuzumab as first-line treatment for human epidermal growth factor receptor 2 positive locally recurrent or metastatic breast cancer: results from a Phase II, single-arm, multicenter study.[Pubmed:27994483]
Breast Cancer (Dove Med Press). 2016 Dec 7;8:231-239.
Eribulin mesylate, a novel nontaxane microtubule dynamics inhibitor in the halichondrin class of antineoplastic drugs, is indicated for the treatment of patients with metastatic breast cancer who previously received >/=2 chemotherapy regimens in the metastatic setting. Primary data from a Phase II trial for the first-line combination of eribulin plus trastuzumab in human epidermal growth factor receptor 2 positive patients showed a 71% objective response rate and tolerability consistent with the known profile of these agents. Here, we present prespecified analyses of efficacy of this combination based on prior trastuzumab use. Patients received Eribulin mesylate 1.4 mg/m(2) (equivalent to 1.23 mg/m(2) eribulin [expressed as free base]) intravenously on days 1 and 8 plus trastuzumab (8 mg/kg intravenously/cycle 1, then 6 mg/kg) on day 1 of each 21-day cycle. Objective response rates, progression-free survival, and tolerability were assessed in patients who had and had not received prior adjuvant or neoadjuvant (neo/adjuvant) trastuzumab treatment. Fifty-two patients (median age: 59.5 years) received eribulin/trastuzumab for a median treatment duration of ~31 weeks; 40.4% (n=21) had been previously treated with neo/adjuvant trastuzumab prior to treatment with eribulin plus trastuzumab for metastatic disease (median time between neo/adjuvant and study treatment: 23 months). In trastuzumab-naive patients (n=31) compared with those who had received prior trastuzumab, objective response rate was 77.4% versus 61.9%, respectively; duration of response was 11.8 versus 9.5 months, respectively; clinical benefit rate was 87.1% versus 81.0%, respectively; and median progression-free survival was 12.2 versus 11.5 months, respectively. The most common grade 3/4 treatment-emergent adverse events (occuring in >/=5% of patients) in patients who received prior trastuzumab versus trastuzumab naive patients, respectively, were neutropenia (47.6% vs 32.3%), peripheral neuropathy (14.3% vs 25.8%), febrile neutropenia (14.3% vs 3.2%), fatigue (9.5% vs 6.5%), nausea (9.5% vs 0%), vomiting (9.5% vs 3.2%), and leukopenia (9.5% vs 3.2%). In patients with human epidermal growth factor receptor 2 positive metastatic breast cancer, first-line eribulin/trastuzumab treatment demonstrated substantial antitumor activity and was well tolerated, regardless of prior neo/adjuvant trastuzumab treatment.
Antitumor Effects of Eribulin Mesylate in Gemcitabine-resistant Pancreatic Cancer Cell Lines.[Pubmed:27793935]
Anticancer Res. 2016 Nov;36(11):6077-6082.
BACKGROUND/AIM: One reason of poor survival rate of patients with pancreatic cancer is the development of chemoresistance. The aim of the present study was to investigate the effects of Eribulin mesylate in gemcitabine-refractory advanced pancreatic cancer cell lines. MATERIALS AND METHODS: Three human pancreatic cancer cell lines (AsPC-1, Panc-1, and SUIT-2) and human pancreatic endoderm (hPE) cells were used to evaluate the antitumor effects of gemcitabine and Eribulin mesylate. Cell viability after treatment of cells with different concentrations of gemcitabine and Eribulin mesylate was evaluated using water-soluble tetrazolium salts (WST) assays; cytotoxic effects were evaluated on the basis of morphological changes to cells. RESULTS: Gemcitabine had no effect on cell viability of AsPC-1 nor Panc-1 cells, whereas gemcitabine reduced cell viability of SUIT-2 cells in a dose-dependent manner. Eribulin mesylate significantly reduced cell viability of both AsPC-1 and Panc-1 cells (p<0.001 and p=0.002, respectively), but had no effect on hPE cells. Microscopic examination of AsPC-1 and Panc-1 cells after treatment with Eribulin mesylate revealed morphological changes that included cell shrinkage, membrane blebbing, and fragmentation of the cells after drug exposure, and these were concentration-dependent effects. CONCLUSION: The findings of the present study suggest that Eribulin mesylate may be a promising potential anticancer drug for gemcitabine-refractory advanced pancreatic cancer.
Efficacy and safety of eribulin mesylate in advanced soft tissue sarcomas.[Pubmed:27688604]
Indian J Med Paediatr Oncol. 2016 Jul-Sep;37(3):125-30.
Despite recent advances in the field, treatment options for metastatic soft tissue sarcoma patients are limited. Eribulin, an antimitotic derived from the natural marine sponge product halichondrin B, is currently approved for the treatment of metastatic breast cancer. Following the promising activity of eribulin in sarcoma in a Phase II trial, the drug was recently compared to dacarbazine in pretreated advanced leiomyosarcoma (LMS) and liposarcoma (LPS) patients in a Phase III trial. Eribulin was associated with a significant 2-month improvement in median overall survival compared to dacarbazine (13.5 vs. 11.5 months, heart rate: 0.768) despite no documented significant difference in progression-free survival. In a subgroup analysis, the survival advantage associated with eribulin was evident in the LPS subgroup but not in the LMS subgroup. Following these encouraging results, the Food and Drug Administration has approved eribulin for the treatment of advanced LPS for patients who received prior anthracycline chemotherapy. In this short review, we will evaluate the evidence for eribulin in soft tissue sarcoma, highlight its mechanisms of action, and summarize the results of the major preclinical and clinical studies with a particular focus on the results of the Phase III trial.
