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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.
| Catalog Number | Size | Price | Quantity |
|---|---|---|---|
| BADC-01379 | -- | $-- |
| NCT Number | Title | Condition Or Disease | Phase | Start Date | Sponsor | Status |
|---|---|---|---|---|---|---|
| NCT00069264 | Study of E7389 in Patients With Advanced Solid Tumors | Advanced Solid Tumors | Phase 1 | September 2003 | Eisai Inc. | Completed |
| NCT00069277 | Study of E7389 Administered Once Every 3 Weeks In Patients With Advanced Solid Tumors | Cancer | Phase 1 | August 2003 | Eisai Inc. | Completed |
| NCT00097721 | A Study of E7389 in Advanced/Metastatic Breast Cancer Patients | Breast Neoplasms | Phase 2 | September 2004 | Eisai Inc. | Completed |
| NCT00246090 | A Phase II Study of E7389 in Patients With Breast Cancer, Previously Treated With Anthracycline, Taxane and Capecitabine | Breast Cancer | Phase 2 | October 2005 | Eisai Inc. | Completed |
| NCT00268905 | A Dose-Finding Study of E7389 in Combination With Carboplatin in Patients With Solid Tumors | Cancer | Phase 1 | October 2006 | Eisai Inc. | Completed |
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BOC Sciences offers comprehensive services for ADC manufacturing, including antibody modification, linker chemistry, payload conjugation, and formulation development. In particular, our payload-linker customization service offers a convenient and fast raw material channel for many ADC researchers.
BOC Sciences provides one-stop site-specific conjugation services for amino acids, glycans, unnatural amino acids, and short peptide tags. In addition, cysteine conjugation, lysine conjugation, enzymatic conjugation, thio-engineered antibody can also be obtained quickly.
BOC Sciences offers a full range of linkers, including peptide linkers, PEG linkers, click chemistry, PROTAC linkers, non-cleavable linkers, etc. We also provide custom development services for chemically labile linkers and enzymatically cleavable linkers.
