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Signaling Pathway

Eribulin

HY-13442

(B1939; E7389; ER-086526)

Eribulin

Eribulin Chemical Structure

Eribulin (E7389; ER-086526), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

Eribulin

CAS No.: 253128-41-5 Backordered

Size Price Stock Quantity
1 mg $3500 Backordered

Eribulin mesylate

CAS No.: 441045-17-6 In-stock

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Inquiry Information
Product name: Eribulin
Cat. No.: HY-13442

Eribulin Data Sheet

  • Network Version

    DataSheet

Related Compound Libraries

Biological Activity of Eribulin

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].
 

Chemical Information

M.Wt 729.9 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₄₀H₅₉NO₁₁
CAS No 253128-41-5
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.3701 mL 6.8503 mL 13.7005 mL
5 mM 0.2740 mL 1.3701 mL 2.7401 mL
10 mM 0.1370 mL 0.6850 mL 1.3701 mL

References on Eribulin

Inhibitor Kit

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