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Eribulin mesylate

Cat. No. M10393
Eribulin mesylate Structure
Synonym:

B1939 mesylate; E7389 mesylate; ER-086526 mesylate

Size Price Availability Quantity
1mg USD 1200  USD1200 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 826.00
Formula C41H63NO14S
CAS Number 441045-17-6
Purity >99%
Solubility DMSO 90 mg/mL
Storage -20°C, protect from light, sealed
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

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