Eribulin mesylate

Research use only, not for human use.

Eribulin mesylate (B1939, E7389, ER-086526) is a macrocyclic ketone analogue of halichondrir B.

Eribulin mesylate (B1939, E7389, ER-086526) is a macrocyclic ketone analogue of halichondrir B, shows sub-nM growth inhibitory activities in vitro against numerous human cancer cell lines via inhibition of tubulin polymerization; induces G2-M cell cycle arrest and disruption of mitotic spindles, demonstrates marked in vivo activities at 0.1-1 mg/kg against human xenografts: MDA-MB-435 breast cancer, COLO 205 colon cancer, LOX melanoma, and NIH: OVCAR-3 ovarian cancer.Breast Cancer Approved(In Vitro):Eribulin (1-100 nM; 72 h) inhibits cells proliferation, with IC50s of 22.8 and 21.5 nM for LM8 and Dunn cells, respectively.Eribulin (10-50 nM; 12-72 h) increases early apoptosis significantly after 24 h treatment at the dose of 50 nM in LM8 cells.Eribulin (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.Eribulin (1-50 nM; 12 h) does not induce senescence in LM8 cells.Eribulin (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells.(In Vivo):Eribulin (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice.Eribulin (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase.

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.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.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.Eribulin mesylate (1-50 nM; 12 h) does not induce senescence in LM8 cells.Eribulin mesylate (1-10 nM; 16 h) induces morphological change and suppresses cell migration in a low concentration in LM8 cells. Cell Proliferation Assay Cell Line:LM8 cells and Dunn cells Concentration:0, 1, 10, 100 nM Incubation Time:72 hours Result:Inhibited cells proliferation in a dose-dependent manner.Apoptosis Analysis Cell Line:LM8 cells Concentration:0, 10, 50 nM Incubation Time:12, 24, 48, 72 hour Result:Induced early apoptosis after 12 h at the concentration of 50 nM.Not detected apoptosis at the concentration of 10 nM. Cell Cycle Analysis Cell Line:LM8 cells Concentration:0, 10, 50 nM Incubation Time:12, 24, 48, 72 hour Result:Induced G2/M arrest by 12 h treatment with 50 nM.No G2/M arrest was induced by10 nM treatment.

Eribulin mesylate (1 mg/kg; i.v. once a week for 2 weeks) reduces primary tumor growth and lung metastasis of osteosarcoma in mice.Eribulin mesylate (1 mg/kg; once i.v.) suppresses circulating tumor cells (CTC) appearance in the low-concentration phase. Animal Model:C3H/HeN mice (4-week-old) are injected LM8 cells Dosage:1 mg/kg Administration:I.v. once a week for 2 weeks Result:Suppressed primary tumor growth and induced apoptosis in tumor cells.Reduced lung metastasis.

B1939 mesylate | E7389 mesylate | ER-086526 mesylate

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Microtubule/Tubulin

Cancer

Breast Cancer

441045-17-6

826.0022

C41H63NO14S

>98% (HPLC)

10 mM in DMSO

CC1CC2CCC3C(=C)CC(O3)CCC45CC6C(O4)C7C(O6)C(O5)C8C(O7)CCC(O8)CC(=O)CC9C(CC(C1=C)O2)OC(C9OC)CC(CN)O.CS(=O)(=O)O

11,15:18,21:24,28-Triepoxy-7,9-ethano-12,15-methano-9H,15H-furo[3,2-i]furo[2',3':5,6]pyrano[4,3-b][1,4]dioxacyclopentacosin-5(4H)-one, 2-[(2S)-3-amino-2-hydroxypropyl]hexacosahydro-3-methoxy-26-methyl-20,27-bis(methylene)-, (2R,3R,3aS,7R,8aS,9S,10aR,11S,1

(-20℃)

With Ice Pack

≥ 2 years