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Eribulin

  CAS No.: 253128-41-5   Cat No.: BADC-01379   Purity: >98% 4.5  

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. [(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. 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.

Eribulin

Structure of 253128-41-5

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Category
ADC Cytotoxin
Molecular Formula
C40H59NO11
Molecular Weight
729.9
Shipping
Store at 0-4°C for short term (days to weeks) or -20°C for long term (months to years), protect from light, stored under nitrogen

* For research and manufacturing use only. We do not sell to patients.

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Popular Publications Citing BOC Sciences Products
Synonyms
Halaven; B1939; E7389; ER-086526
IUPAC 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
Canonical 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
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
InChIKey
UFNVPOGXISZXJD-JBQZKEIOSA-N
Appearance
Solid powder
Quantity
Milligrams-Grams
Storage
Store at 0-4°C for short term (days to weeks) or -20°C for long term (months to years), protect from light, stored under nitrogen
NCT NumberTitleCondition Or DiseasePhaseStart DateSponsorStatus
NCT00069264Study of E7389 in Patients With Advanced Solid TumorsAdvanced Solid TumorsPhase 1September 2003Eisai Inc.Completed
NCT00069277Study of E7389 Administered Once Every 3 Weeks In Patients With Advanced Solid TumorsCancerPhase 1August 2003Eisai Inc.Completed
NCT00097721A Study of E7389 in Advanced/Metastatic Breast Cancer PatientsBreast NeoplasmsPhase 2September 2004Eisai Inc.Completed
NCT00246090A Phase II Study of E7389 in Patients With Breast Cancer, Previously Treated With Anthracycline, Taxane and CapecitabineBreast CancerPhase 2October 2005Eisai Inc.Completed
NCT00268905A Dose-Finding Study of E7389 in Combination With Carboplatin in Patients With Solid TumorsCancerPhase 1October 2006Eisai Inc.Completed
1.Results of the Belgian expanded access program of eribulin in the treatment of metastatic breast cancer closely mirror those of the pivotal phase III trial.
Aftimos P1, Polastro L2, Ameye L3, Jungels C2, Vakili J2, Paesmans M3, van den Eerenbeemt J2, Buttice A2, Gombos A2, de Valeriola D2, Gil T2, Piccart-Gebhart M2, Awada A2. Eur J Cancer. 2016 Apr 20;60:117-124. doi: 10.1016/j.ejca.2016.03.010. [Epub ahead of print]
BACKGROUND: Eribulin is a non-taxane microtubule dynamics inhibitor that showed a survival benefit versus treatment of physician's choice in a phase III trial enrolling patients with metastatic breast cancer (MBC).
2.In vivo imaging of eribulin-induced reoxygenation in advanced breast cancer patients: a comparison to bevacizumab.
Ueda S1, Saeki T1, Takeuchi H1, Shigekawa T1, Yamane T2, Kuji I2, Osaki A1. Br J Cancer. 2016 May 3. doi: 10.1038/bjc.2016.122. [Epub ahead of print]
BACKGROUND: Eribulin mesylate (eribulin) is a first-in-class halichondrin B-based microtubule dynamics inhibitor. To compare the anti-angiogenic activity of eribulin to that of bevacizumab, we compared tumour vessel remodelling and reoxygenation between the two agents.
3.Patient Management with Eribulin in Metastatic Breast Cancer: A Clinical Practice Guide.
Ro J1, Cheng FT2, Sriuranpong V3, Villalon A4, Smruti BK5, Tsang J6, Yap YS7; Asian Working Group for Eribulin Clinical Guide. J Breast Cancer. 2016 Mar;19(1):8-17. doi: 10.4048/jbc.2016.19.1.8. Epub 2016 Mar 25.
Eribulin, an antimicrotubule chemotherapeutic agent, is approved for the treatment of pretreated metastatic breast cancer (mBC) based on the positive outcomes of phase II and phase III clinical trials, which enrolled mainly Western patients. Eribulin has recently been approved in an increasing number of Asian countries; however, there is limited clinical experience in using the drug in certain countries. Therefore, we established an Asian working group to provide practical guidance for eribulin use based on our clinical experience. This paper summarizes the key clinical trials, and the management recommendations for the reported adverse events (AEs) of eribulin in mBC treatment, with an emphasis on those that are relevant to Asian patients, followed by further elaboration of our eribulin clinical experience. It is anticipated that this clinical practice guide will improve the management of AEs resulting from eribulin treatment, which will ensure that patients receive the maximum treatment benefit.
4.Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue Sarcoma.
Kawano S1, Asano M1, Adachi Y1, Matsui J2. Anticancer Res. 2016 Apr;36(4):1553-61.
BACKGROUND: Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models.

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