Eribulin (mesylate)

Eribulin mesylate is an inhibitor for microtubule. Eribulin mesylate inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate exhibits antitumor efficacy in mouse model^[1]. In Vitro:Eribulin mesylate (1-100 nM; 72 h) inhibits cells proliferation, with IC₅₀s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively^[1].
Eribulin mesylate (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells^[1].
Eribulin mesylate (10-50 nM; 12-72 h) induces G2/M arrest by 12 h treatment with at the dose of 50 nM, but not by long-term treatment (72 h) with 10 nM in LM8 cells^[1].
Eribulin mesylate (1-50 nM; 12 h) does not induce senescence in LM8 cells^[1].
Eribulin mesylate (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells^[1]. In Vivo:Eribulin mesylate (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice^[1].
Eribulin mesylate (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase^[1].