Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(B1939 mesylate; E7389 mesylate; ER-086526 mesylate)
Eribulin mesylate Chemical Structure
|Product name: Eribulin mesylate|
|Cat. No.: HY-13442A|
Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.
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 .
|M.Wt||826.0||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||1.2107 mL||6.0533 mL||12.1065 mL|
|5 mM||0.2421 mL||1.2107 mL||2.4213 mL|
|10 mM||0.1211 mL||0.6053 mL||1.2107 mL|
. Towle, M.J., et al., Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res, 2011. 71(2): p. 496-505.
CAS No.: 253128-41-5 Get quote
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.
10-Oxo Docetaxel(Docetaxel Impurity) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 (plusmn) 0.11 (mu)M for the inhibition of BPAEC migration.
4(acute)-Demethylepipodophyllotoxin(4(acute)-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.
7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C; 7-Epitaxotere) is a impurity of docetaxel.
7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) derivative; Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.
ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 (mu)M in neuroblastoma and non-neuroblastoma cell lines, respectively.
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.
Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates.