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Diflomotecan

Cat. No. M29358
Diflomotecan Structure
Synonym:

BN 80915

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Biological Activity

Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.

Chemical Information
Molecular Weight 398.36
Formula C21H16F2N2O4
CAS Number 220997-97-7
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] Víctor Mangas-Sanjuan, et al. J Pharmacol Exp Ther. Semimechanistic cell-cycle type-based pharmacokinetic/pharmacodynamic model of chemotherapy-induced neutropenic effects of diflomotecan under different dosing schedules

[2] Judith R Kroep, et al. Expert Opin Investig Drugs. Diflomotecan, a promising homocamptothecin for cancer therapy

[3] Janet S Graham, et al. Cancer Chemother Pharmacol. A multi-centre dose-escalation and pharmacokinetic study of diflomotecan in patients with advanced malignancy

[4] Alex Sparreboom, et al. Clin Pharmacol Ther. Diflomotecan pharmacokinetics in relation to ABCG2 421C>A genotype

[5] Neil Osheroff. IDrugs. Diflomotecan. Ipsen

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  Catalog
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Keywords: Diflomotecan, BN 80915 supplier, Topoisomerase, inhibitors, activators


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