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).|
|Solubility (25°C)||DMSO 35 mg/mL
Water 33 mg/mL
|Storage||2-8°C, protect from light, sealed|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Related Topoisomerase Products|
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria.
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
Bimolane (AT-1727), a human topoisomerase II inhibitor, can be used as an anti-neoplastic agent and for the research of psoriasis. Bimolane shows leukemogenic activity and induces multiple types of chromosomal aberrations in human lymphocytes.
MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
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