EribulinCAS# 253128-41-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 253128-41-5 | SDF | Download SDF |
| PubChem ID | 11354606 | Appearance | Powder |
| Formula | C40H59NO11 | M.Wt | 729.9 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | B1939; E7389; ER-086526 | ||
| Solubility | Soluble in DMSO | ||
| 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 | ||
| Standard InChIKey | UFNVPOGXISZXJD-JBQZKEIOSA-N | ||
| Standard InChI | InChI=1S/C40H59NO11/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/h19,23-39,43H,2-3,5-18,41H2,1,4H3/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), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.
Target: Microtubule/Tubulin
Eribulin suppressed centromere dynamics at concentrations that arrest mitosis. At 60 nmol/L eribulin (2 x mitotic IC(50)), the relaxation rate was suppressed 21%, the time spent paused increased 67%, and dynamicity decreased 35% (but without reduction in mean centromere separation), indicating that eribulin decreased normal microtubule-dependent spindle tension at the kinetochores, preventing the signal for mitotic checkpoint passage [1]. [(3)H]eribulin binds soluble tubulin at a single site; however, this binding is complex with an overall K(d) of 46 microM, but also showing a real or apparent very high affinity (K(d) = 0.4 microM) for a subset of 25% of the tubulin. Eribulin also binds microtubules with a maximum stoichiometry of 14.7 +/- 1.3 molecules per microtubule (K(d) = 3.5 microM), strongly suggesting the presence of a relatively high-affinity binding site at microtubule ends. At 100 nM, the concentration that inhibits microtubule plus end growth by 50%, we found that one molecule of eribulin is bound per two microtubules, indicating that the binding of a single eribulin molecule at a microtubule end can potently inhibit its growth. Eribulin does not suppress dynamic instability at microtubule minus ends [2]. Eribulin's in vivo superiority derives from its ability to induce irreversible mitotic blockade, which appears related to persistent drug retention and sustained Bcl-2 phosphorylation [3]. References: | |||||
Eribulin Dilution Calculator
Eribulin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.3701 mL | 6.8503 mL | 13.7005 mL | 27.401 mL | 34.2513 mL |
| 5 mM | 0.274 mL | 1.3701 mL | 2.7401 mL | 5.4802 mL | 6.8503 mL |
| 10 mM | 0.137 mL | 0.685 mL | 1.3701 mL | 2.7401 mL | 3.4251 mL |
| 50 mM | 0.0274 mL | 0.137 mL | 0.274 mL | 0.548 mL | 0.685 mL |
| 100 mM | 0.0137 mL | 0.0685 mL | 0.137 mL | 0.274 mL | 0.3425 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 (E7389; ER-086526), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.
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A systematic review and pooled analysis of retrospective series of eribulin in metastatic breast cancer.[Pubmed:28263201]
Anticancer Drugs. 2017 Jun;28(5):557-564.
Eribulin is one of the newer chemotherapeutic agents approved for use in later line treatment of patients with metastatic breast cancer. Phase III studies have shown a useful clinical response rate for Eribulin as well as equivalence to another commonly used drug in metastatic breast cancer, capecitabine. Nevertheless, whether this clinical value observed in trial patients is maintained in patients seen in clinical oncology practice, outside trials remains a question. Several series published over the last few years sought to answer this question. The current paper carries out a pooled analysis of these retrospective series to obtain efficacy and toxicity data for Eribulin in metastatic breast cancer patients treated off trials. Thirteen series with a total of 1095 patients were identified. Pooled estimates of response rate and clinical benefit rate were 20.1% (95% confidence interval: 16.3-23.9%) and 46.3% (95% confidence interval: 39.4-53.2%) respectively. These were somewhat higher than the response rate and clinical benefit rate observed in a pooled analysis of two randomized phase III trials (14.9 and 30.9%, respectively, conducted in an intension-to-treat manner). In contrast overall survival was longer in the phase III trials (median 15.2 months) than in the retrospective studies (pooled estimate 9.8 months). All grades toxicities were similar in practice compared with trials with slightly higher grade 3 toxicities (46.1 vs. 38.7%) but lower grade 4 toxicities (17.2 vs. 27.7%) in patients off trials.
Patient-derived solitary fibrous tumour xenografts predict high sensitivity to doxorubicin/dacarbazine combination confirmed in the clinic and highlight the potential effectiveness of trabectedin or eribulin against this tumour.[Pubmed:28284173]
Eur J Cancer. 2017 May;76:84-92.
BACKGROUND: Preclinical models that mimic pathological and molecular features of solitary fibrous tumour (SFT) represent an important tool to select effective regimes and novel compounds to be tested in the clinic. This study was aimed at developing two preclinical models of SFT, assessing their predictive value in the clinic and selecting potential novel effective treatments. MATERIAL AND METHODS: Two dedifferentiated-SFT (D-SFT) models obtained from patients' biopsies were grown in immunodeficient mice. The antitumour activity on these models of doxorubicin, dacarbazine (DTIC), ifosfamide (monotherapy or combination), trabectedin and Eribulin was tested. Twelve SFT patients were treated with doxorubicin and DTIC. Response by RECIST, progression-free survival and overall survival were retrospectively evaluated, distinguishing malignant-SFT (M-SFT) and D-SFT. RESULTS: Two D-SFT patient-derived xenografts (PDXs) that represent the first available preclinical in vivo models of SFT were developed and characterised. Doxorubicin/DTIC, DTIC/ifosfamide, doxorubicin/ifosfamide combinations consistently induced better antitumour activity than the single-agents. Particularly, doxorubicin/DTIC combination caused a max tumour volume inhibition >80% in both models. Doxorubicin/DTIC combo showed activity also in the case-series. Best RECIST responses were: 6 responses (M-SFT = 2 of 7, D-SFT = 4 of 5), 1 stable disease, 5 progressions, with a 6-month median progression-free survival (M-SFT = 6, D-SFT = 10 months). The PDXs were very sensitive to trabectedin and Eribulin. CONCLUSION: Doxorubicin plus DTIC combination was effective in our two D-SFT mice models and appeared to be active also in the clinic, especially in high-grade D-SFT patients. Among additional drugs tested in the PDXs, trabectedin and Eribulin were highly effective, providing a rational to test these drugs in D-SFT patients.
Eribulin in heavily pretreated metastatic breast cancer: A tertiary care center experience from India.[Pubmed:28244486]
Indian J Cancer. 2016 Jul-Sep;53(3):460-463.
INTRODUCTION: Heavily pretreated metastatic breast cancer (MBC) remains a major therapeutic challenge with limited treatment options this. Eribulin, an anti-microtubule agent, has been recently approved for this indication. There are sparse data from the Asian region for Eribulin and merits exploration. MATERIALS AND METHODS: This was a single institution retrospective analysis of MBC patients treated with Eribulin from 2013 to 2014. These patients had received at least 2 lines of prior therapy for metastatic disease. Patients received standard doses of Eribulin and were monitored for toxicity and responses. RESULTS: Eighteen patients were included in this analysis. They had received a median of 6 lines of therapy previously (including adjuvant treatment) and had significant visceral involvement (median 3 organs). A median of 4 cycles of Eribulin was delivered. There were no complete responses; partial responses were seen in 33% (6/18), stable disease status in 28% (5/18) patients, and progressive disease on Eribulin in 39% (7/18) patients. The median progression-free survival was 15 weeks (3.5 months), and median overall survival was 27 weeks (6.2 months). Significant Grade 3/4 toxicities seen included peripheral neuropathy in 28% (5/18) and neutropenia in 28% (5/18) of patients while dose reductions were required in 22% (4/18) of patients. CONCLUSION: Eribulin offers a viable, well-tolerated regimen that provides meaningful clinical benefit in Indian patients with MBC.
Efficacy and safety of eribulin in taxane-refractory patients in the 'real world'.[Pubmed:28326833]
Future Oncol. 2017 May;13(11):971-978.
AIM: Recent clinical, randomized and observational studies showed that Eribulin, an analogous of Halichondrin B, was beneficial and well-tolerated in heavily pretreated metastatic breast cancer patients. Here, we aim to evaluate the effectiveness and safety of Eribulin in taxane-refractory metastatic breast cancer patients. PATIENTS & METHODS: In this subanalysis of the ESEMPIO study database, we selected 91 subjects with well-defined taxane refractoriness and complete data available. RESULTS: 41 patients (45.2%) showed clinical benefit; one complete response (2.2%) and 16 partial responses (17.6%) were observed. Median progression-free survival and median overall survival were 3.1 and 11.6 months, respectively. The most experienced adverse event was asthenia/fatigue (58%), followed by neutropenia (30%). The treatment-related toxicity led to Eribulin-dose reduction in 19 patients and suspension in nine. CONCLUSION: This study shows that Eribulin is effective and well tolerated also in taxane-refractory patients in clinical practice.
