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Eribulin mesylate

Cat. No. M10393
Eribulin mesylate Structure
Synonym:

B1939 mesylate; E7389 mesylate; ER-086526 mesylate

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1mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

Eribulin mesylate inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. Eribulin (1-10 nM) 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.

Chemical Information
Molecular Weight 826.00
Formula C41H63NO14S
CAS Number 441045-17-6
Solubility (25°C) DMSO 90 mg/mL
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kenta Watanabe, et al. Oncotarget. Low-dose eribulin reduces lung metastasis of osteosarcoma in vitro and in vivo

[2] Murray J Towle, et al. Cancer Res. Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions

[3] Jennifer A Smith, et al. Biochemistry. Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability

[4] Tatiana Okouneva, et al. Mol Cancer Ther. Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase

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Keywords: Eribulin mesylate, B1939 mesylate; E7389 mesylate; ER-086526 mesylate supplier, Microtubule, inhibitors, activators


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