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TAS-103

Cat. No. M28840
TAS-103 Structure
Synonym:

BMS-247615

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Biological Activity

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.

Chemical Information
Molecular Weight 333.38
Formula C20H19N3O2
CAS Number 174634-08-3
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] Makoto Yoshida, et al. Mol Pharmacol. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads

[2] Keisuke Ishida, et al. Biochim Biophys Acta. Self-association and unique DNA binding properties of the anti-cancer agent TAS-103, a dual inhibitor of topoisomerases I and II

[3] R B Ewesuedo, et al. J Clin Oncol. Phase I clinical and pharmacogenetic study of weekly TAS-103 in patients with advanced cancer

[4] T Ohyama, et al. Jpn J Cancer Res. A dual topoisomerase inhibitor, TAS-103, induces apoptosis in human cancer cells

[5] Y Aoyagi, et al. Jpn J Cancer Res. In vitro antitumor activity of TAS-103, a novel quinoline derivative that targets topoisomerases I and II

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  Catalog
Abmole Inhibitor Catalog




Keywords: TAS-103, BMS-247615 supplier, Topoisomerase, inhibitors, activators


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