Description
Topotecan (Hycamtin, NSC 609699) can inhibit topoisomerase I with IC50 of around 2 nM- 13 nM.
Alias
Hycamtin, NSC 609699
Storage
2 years at -20 centigrade
Synonyms
Hycamtin, NSC 609699
Molecular Formula
C23H23N3O5.HCl
Solubility
DSMO 92 mg/mL Water 92 mg/mL Ethanol
In vitro
Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break.
In vivo
Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells.
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