Topotecan hydrochloride (trade name Hycamtin) is a potent antineoplastic agent. It is a water soluble analog of the alkaloid camptothecin that potently inhibits DNA topoisomerase I. Topotecan hydrochloride induces rapid apoptotic death in human B-lineage acute lymphoblastic leukemia (ALL) cells with IC50 values of 33 nM and 0.28 μM, respectively. Topotecan improves survival in three mouse models of poor prognosis ALL and downregulates B-Myb and MycN expression in neuroblastoma cells. Topotecan demonstrates a broad spectrum of antitumor activity against a variety of other tumors including ovarian cancer, cervical cancer, neuroblastoma, brainstem glioma, and Ewing’s sarcoma.
J Korean Med Sci. 2016 Jun;31(6): 836–842.
Silencing of ABCG2 by MicroRNA-3163 Inhibits Multidrug Resistance in Retinoblastoma Cancer Stem Cells
Topotecan hydrochloride purchased from AbMole
|Source||J Korean Med Sci (2016). Figure 5. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).|
|Method||CCK8 Assay and ABCG2 ATPase assay|
|Cell Lines||RCSC cells|
|Incubation Time||72 h|
|Results||MiR-3163 plays important roles in multidrug resistance (Table 1, Fig. 5A). Results showed that when miR-3163 was overexpressed in RCSCs, the ATPase activity of ABCG2 was significantly downregulated compared to RCSCs with Scramble (Fig. 5B).|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 82 mg/mL
Water 70 mg/mL
A chemical screen identifies the chemotherapeutic drug topotecan as a specific inhibitor of the B-MYB/MYCN axis in neuroblastoma.
Sottile F, et al. Oncotarget. 2012 May;3(5):535-45. PMID: 22619121.
Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor.
Schellens JH, et al. Br J Cancer. 1996 May;73(10):1268-71. PMID: 8630291.
In vitro and in vivo activity of topotecan against human B-lineage acute lymphoblastic leukemia cells.
Uckun FM, et al. Blood. 1995 May 15;85(10):2817-28. PMID: 7742543.
|Related Topoisomerase Products|
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
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