Eribulin mesylate

SKU: orb2655705

Description

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.

Images & Validation

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Key Properties

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CAS Number	441045-17-6
MW	826.0022
Purity	>98% (HPLC)
Formula	C₄₁H₆₃NO₁₄S
SMILES	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
Target	Microtubule/Tubulin
Solubility	10 mM in DMSO

Bioactivity

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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. 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.
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. 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.

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. 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.

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. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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B1939 mesylate | E7389 mesylate | ER-086526 mesylate

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Quick Database Links

Gene Symbol

Microtubule/Tubulin

Protocol Information

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Purity:	>99.99% (May vary between batches)
CAS Number:	441045-17-6
MW:	826
Formula:	C₄₁H₆₃NO₁₄S