Description
Topotecan-d
6 is intended for use as an internal standard for the quantification of topotecan by GC- or LC-MS. Topotecan is an inhibitor of DNA topoisomerase I and a derivative of the DNA topoisomerase I inhibitor camptothecin . Topotecan inhibits DNA topoisomerase I in human MCF-7 breast and DU145 prostate cancer cells with IC
50 values of 13 and 2 nM, respectively, in a cell-based luciferase reporter assay. Topotecan induces cytotoxicity and DNA damage in HT-29 human colon adenocarcinoma cells (IC
50s = 33 and 280 nM, respectively). Formulations containing topotecan have been used in the treatment of small-cell lung cancer.
Chemical Properties
Light Yellow to Greenish Powder
Uses
Labelled Topotecan (T542500). A DNA topoisomerase I inhibitor; semisynthetic analog of Camptothecin. Antineoplastic.
Uses
Labelled Topotecan. A DNA topoisomerase I inhibitor; semisynthetic analog of Camptothecin. Antineoplastic
References
[1] ROTHENBERG M L. Topoisomerase I inhibitors: Review and update[J]. Annals of Oncology, 1997, 8 9: Pages 837-855. DOI:
10.1023/a:1008270717294[2] J DANCEY EA E. Current perspectives on camptothecins in cancer treatment[J]. British Journal of Cancer, 1996, 74 3: 327-338. DOI:
10.1038/bjc.1996.362[3] JHM SCHELLENS. Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor[J]. British Journal of Cancer, 1996, 73 10: 1268-1271. DOI:
10.1038/bjc.1996.243[4] GISELA CACERES. Determination of chemotherapeutic activity in vivo by luminescent imaging of luciferase-transfected human tumors.[J]. Anti-Cancer Drugs, 2003, 14 7: 569-574. DOI:
10.1097/00001813-200308000-00010
