Catalog No.S1231 Synonyms: NSC609699, Nogitecan HCl, SKFS 104864A
Molecular Weight(MW): 457.91
Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.
Cited by 6 Publications
2 Customer Reviews
Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.
BMC Cancer, 2015, 10.1186/s12885-015-1231-z. Topotecan HCl purchased from Selleck.
Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.
PLoS Genet 2014 10(1), e1004107. Topotecan HCl purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.|
|Features||Topotecan is a water-soluble derivative of camptothecin.|
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. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. 
|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.  Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels.  Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. |
-  Caceres G, et al. Anticancer Drugs. 2003, 14(7), 569-574.
-  Uckun FM, et al. Blood. 1995. 85(10), 2817-2828.
-  Ciusani E, et al. J Neurooncol. 2005, 71(1), 19-25.
|In vitro||DMSO||92 mg/mL (200.91 mM)|
|Water||92 mg/mL (200.91 mM)|
|In vivo||Saline||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||NSC609699, Nogitecan HCl, SKFS 104864A|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02348398||Not yet recruiting||Cervical Cancer||M.D. Anderson Cancer Center|GlaxoSmithKline||August 2016||Phase 2|
|NCT02822157||Not yet recruiting||Ovarian Epithelial Cancer||Universitaire Ziekenhuizen Leuven|AstraZeneca||August 2016||Phase 2|
|NCT02566993||Not yet recruiting||Small-cell Lung Cancer||PharmaMar||July 2016||Phase 3|
|NCT02813135||Recruiting||Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies||Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France||June 2016||Phase 1|Phase 2|
|NCT02786719||Recruiting||Neuroblastoma||Baylor College of Medicine|Texas Childrens Hospital||June 2016||--|
|NCT02649673||Recruiting||Small Cell Lung Cancer|Ovarian Cancer||SCRI Development Innovations, LLC|Novartis Pharmaceuticals||March 2016||Phase 1|Phase 2|
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Frequently Asked Questions
I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?
Topotecan HCl is generally prepared by Saline for I.P. administration.