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Cat. No. Name Size Price Add Cart
KI0938Topotecan25 mg$182
Topotecan50 mg$312

Chemical Characteristic

Product NameTopotecan
SynonymsHycamtin,NSC609699
CAS No.123948-87-8
Molecular Weight 421.45
FormulaC23H23N3O5
Chemical Name(S)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Smilesn1c2c(cc3c(c(ccc13)O)CN(C)C)Cn1c(=O)c3c(cc21)[C@@](C(=O)OC3)(O)CC
Chemical Structure

Biological activities

Topotecan is a topoisomerase I inhibitor.[1] The IC50 of topotecan is 13 and 2 nM against MCF-7 Luc cells and DU-145 Luc cells, respectively. [2] Topotecan significantly up-regulates the expression of TRAIL R2. Topotecan increases the sensitivity to TRAIL-dependent apoptosis. [3] Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells. Topotecan causes rapid apoptotic cell death despite high-level expression of bcl-2 protein. Topotecan dose-dependently inhibits ALL cell in vitro clonogenic growth.[4] Topotecan significantly inhibits the growth of tumors in animals inoculated s.c. with DU-145 Luc cells.[2] Topotecan exhibits potent antileukemic activity in severe combined immunodeficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improves event-free survival of SCID mice. Topotecan overcomes the resistance in A2780/CP but not in IGROV-1/Pt1 tumor xenografts.[5]

Protocols

In vivo Topotecan is dissolved in sterile water and diluted in 5% dextrose solution.[5]

References

[1] Mi Z, et al. Reduced albumin binding promotes the stability and activity of topotecan in human blood. Biochemistry. 1995, 34(42): 13722-13728. 閵嗏偓閵嗏偓
[2] Caceres G, et al. Determination of chemotherapeutic activity in vivo by luminescent imaging of luciferase-transfected human tumors. Anticancer Drugs. 2003, 14(7): 569-574. 閵嗏偓閵嗏偓
[3] Ciusani E, et al. In vitro effects of topotecan and ionizing radiation on TRAIL/Apo2L-mediated apoptosis in malignant glioma. J Neurooncol. 2005, 71(1): 19-25. 閵嗏偓閵嗏偓
[4] Uckun FM, et al. In vitro and in vivo activity of topotecan against human B-lineage acute lymphoblastic leukemia cells. Blood. 1995, 85(10): 2817-2828.
[5] Caserini C, et al. Apoptosis as a determinant of tumor sensitivity to topotecan in human ovarian tumors: preclinical in vitro/in vivo studies. Clin Cancer Res. 1997, 3(6): 955-961. 閵嗏偓閵嗏偓

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