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Fumagillin

Cat. No. M5224
Fumagillin Structure
Synonym:

Amebacilin; NSC9168

Size Price Availability Quantity
1mg USD 66  USD66 In stock
5mg USD 230  USD230 In stock
10mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

In vitro: Fumagillin selectively inhibits the growth of a Δmap1 strain but not a wild-type or a Δmap2 S. cerevisiae strain missing MetAP-2. In budding yeast cells, as a potent inhibitor of angiogenesis, Fumagillin not only reverses the growth inhibitory activity of Vpr, but also inhibits Vpr-dependent viral gene expression upon the infection of human macrophages. Though the toxicity of fumagillin has limited its use for human applications, the analogues using structure-activity relationships relating to its angiogenesis properties may be further explored in the treatment of angiogenesis-dependent diseases. In vivo: In DEN-treated rats, fumagillin (30 mg/kg, i.p.) inhibits both progression of HCC in the liver itself and systemic metastasis.

Protocol (for reference only)
Cell Experiment
Cell lines lymphoma cell lines
Preparation method The transcript and protein product of replication transcriptional activator (RTA) were induced by 1-10 μM fumagillin at 24 and 48 h, respectively. Western blot analysis demonstrated that 10 μM fumagillin induced not only RTA expression but also other KSHV-encoded lytic proteins. A real-time PCR array detecting KSHV gene expression demonstrated that the expression profiles of KSHV induced by fumagillin were similar to those induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), but the amounts of each transcript were lower than those induced by TPA. Finally, real-time PCR demonstrated an increase in that viral DNA copy number per cell in fumagillin-stimulated primary effusion lymphoma cell lines, indicating replication of KSHV.
Concentrations 1-10 μM
Incubation time 48h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 458.54
Formula C26H34O7
CAS Number 23110-15-8
Solubility (25°C) 72 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Mendoza Y, et al. J Econ Entomol. Nosema ceranae Winter Control: Study of the Effectiveness of Different Fumagillin Treatments and Consequences on the Strength of Honey Bee (Hymenoptera: Apidae) Colonies.

[2] Kanno T, et al. Biochem Biophys Res Commun. Fumagillin, a potent angiogenesis inhibitor, induces Kaposi sarcoma-associated herpesvirus replication in primary effusion lymphoma cells.

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Keywords: Fumagillin, Amebacilin; NSC9168 supplier, Antibiotic, inhibitors, activators


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