1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

Eribulin mesylate (Synonyms: B1939 mesylate; E7389 mesylate; ER-086526 mesylate)

Cat. No.: HY-13442A Purity: 98.83%
Data Sheet SDS Handling Instructions

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

For research use only. We do not sell to patients.
Eribulin mesylate Chemical Structure

Eribulin mesylate Chemical Structure

CAS No. : 441045-17-6

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Other Forms of Eribulin mesylate:

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Description

Eribulin Mesylate (E7389 Mesylate), 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].

Clinical Trial
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References
Molecular Weight

826.0

Formula

C₄₁H₆₃NO₁₄S

CAS No.

441045-17-6

Storage

-20°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Eribulin mesylate
Cat. No.:
HY-13442A
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