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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.
Structure of 253128-41-5
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Eribulin is a synthetic microtubule dynamics inhibitor and a potent ADC cytotoxin used as an ADC payload in antibody-drug conjugates. Its cytotoxic mechanism involves binding to the plus ends of microtubules, inhibiting their elongation while sparing depolymerization, leading to suppression of mitotic spindle formation, G2/M cell cycle arrest, and apoptosis in proliferating tumor cells. The chemical structure of Eribulin allows stable conjugation to monoclonal antibodies via cleavable or non-cleavable linkers, enabling precise intracellular delivery in ADC applications.
Within antibody-drug conjugates, Eribulin is covalently attached to antibodies through linker chemistries designed for systemic stability and controlled intracellular release. The ADC remains inactive in circulation, preventing off-target cytotoxicity. Following receptor-mediated internalization into antigen-expressing tumor cells, enzymatic or chemical cleavage liberates Eribulin, which binds microtubule plus ends, disrupts mitotic spindle assembly, and triggers apoptosis. This targeted mechanism ensures cytotoxic effects are restricted to tumor cells, enhancing the specificity and reproducibility of tumor-targeted therapy.
Applications of Eribulin include integration into ADCs targeting both solid tumors and hematologic malignancies with defined antigen expression. Its chemical compatibility with diverse linker chemistries allows optimization of conjugation efficiency, intracellular release kinetics, and pharmacokinetics. Eribulin demonstrates reproducible cytotoxicity in target-expressing tumor cells, supporting the development of ADCs with precise antimitotic activity. Its well-characterized mechanism of microtubule inhibition enables controlled apoptosis induction, providing a mechanistically robust payload for ADC design and development in targeted cancer therapy.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-00660 | VCP-Eribulin | 2130869-17-7 | |
| BADC-00860 | Mal-PEG2-VCP-Eribulin | 2130869-18-8 | |
| BADC-01611 | Farletuzumab ecteribulin | 2407465-18-1 | |
| BADC-01399 | Eribulin Mesylate | 441045-17-6 |
What is Eribulin?
Eribulin is a synthetic microtubule inhibitor used as a cytotoxic payload in antibody-drug conjugates. It binds to microtubule plus ends, preventing polymerization and leading to mitotic blockade, providing targeted cytotoxicity when delivered via antibodies.
10/10/2021
Dear BOC Sciences, how does Eribulin function in ADCs?
Eribulin exerts cytotoxic effects in ADCs by disrupting microtubule dynamics upon internalization into target cells. This leads to mitotic arrest and selective apoptosis of antigen-expressing tumor cells, enhancing therapeutic specificity.
12/1/2023
Dear BOC Sciences, which linker types are suitable for Eribulin conjugation?
Eribulin can be conjugated using cleavable linkers that respond to intracellular triggers or non-cleavable linkers that retain cytotoxicity post-antibody degradation. Linker selection depends on desired release kinetics and therapeutic design.
5/11/2022
May I ask what safety measures are recommended for handling Eribulin?
Handling Eribulin requires cytotoxic safety protocols, including personal protective equipment, containment, and proper waste disposal. These measures reduce exposure risks during laboratory handling, conjugation, and analytical evaluation.
19/9/2021
Dear team, can Eribulin be used in preclinical ADC development?
Yes, Eribulin is commonly applied in preclinical ADC studies to evaluate microtubule-targeted cytotoxicity, optimize linker chemistry, and investigate antibody-mediated selective delivery in tumor models.
12/6/2021
— Dr. David Miller, Senior ADC Researcher (USA)
Eribulin delivered by BOC Sciences showed high purity and stability, supporting our ADC development studies.
5/11/2022
— Dr. Christopher Reed, Senior Scientist (USA)
Eribulin supplied by BOC Sciences demonstrated excellent purity and reproducibility, critical for our ADC conjugation work.
12/6/2021
— Ms. Lena Fischer, Research Scientist (Germany)
We received comprehensive analytical documentation with Eribulin, streamlining internal quality checks.
19/9/2021
— Dr. William Hughes, Biotech Researcher (UK)
Eribulin batches were stable and consistent, enabling smooth ADC payload optimization.
10/10/2021
— Mr. Antoine Dubois, Medicinal Chemist (France)
Professional support from BOC Sciences made Eribulin procurement straightforward and efficient.
— Dr. Ingrid Svensson, Laboratory Director (Sweden)
High-quality Eribulin has become a reliable component in our ADC development projects.
12/1/2023
Eribulin
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Eribulin
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