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Pironetin 

Cat. No. M28558
Pironetin  Structure
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Quality Control & Documentation
Biological Activity

Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.

Chemical Information
Molecular Weight 324.45
Formula C19H32O4
CAS Number 151519-02-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Gérard Vergoten, et al. Plants (Basel). Molecular Docking of Cryptoconcatones to α-Tubulin and Related Pironetin Analogues

[2] Md Abdullah Al Noman, et al. Bioorg Chem. Cytotoxicity of phenylpironetin analogs and the metabolic fate of pironetin and phenylpironetin

[3] Sara K Coulup, et al. Bioorg Med Chem Lett. Revisiting microtubule targeting agents: α-Tubulin and the pironetin binding site as unexplored targets for cancer therapeutics

[4] Andrea E Prota, et al. J Mol Biol. Pironetin Binds Covalently to αCys316 and Perturbs a Major Loop and Helix of α-Tubulin to Inhibit Microtubule Formation

[5] Jianhong Yang, et al. Nat Commun. Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule

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Keywords: Pironetin  supplier, Microtubule, inhibitors, activators


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