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
Molecular Weight | 457.91 |
Formula | C23H23N3O5.HCl |
CAS Number | 119413-54-6 |
Solubility (25°C) | DMSO 35 mg/mL Water 33 mg/mL |
Storage | 2-8°C, protect from light, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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