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

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

Cat. No.: HY-13442
Handling Instructions

Eribulin (E7389; ER-086526), 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 Chemical Structure

Eribulin Chemical Structure

CAS No. : 253128-41-5

Size Inquiry
1 mg Get quote for price and lead time

* Please select Quantity before adding items.

Other In-stock Forms of Eribulin:

Other Forms of Eribulin:

  • Biological Activity

  • Protocol

  • Technical Information

  • References

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].

Clinical Trial
View MoreCollapse
References
Molecular Weight

729.9

Formula

C₄₀H₅₉NO₁₁

CAS No.

253128-41-5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Eribulin
Cat. No.:
HY-13442
Quantity: