Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 µM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively. It is an anthracenedione (not an anthracycline) antineoplastic agent. It disrupts DNA synthesis and DNA repair in both healthy cells and cancer cells. It is used in the treatment of certain types of cancer, mostly metastatic breast cancer, acute myeloid leukemia, and non-Hodgkin’s lymphoma. It was also shown to improve the survival of children suffering from first relapse of acute lymphoblastic leukaemia. It also engages in intercalation.
J Korean Med Sci. 2016 Jun;31(6): 836–842.
Silencing of ABCG2 by MicroRNA-3163 Inhibits Multidrug Resistance in Retinoblastoma Cancer Stem Cells
Mitoxantrone purchased from AbMole
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Source | J Korean Med Sci (2016). Figure 5. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience Inc. (Houston, USA). |
| Method | CCK8 Assay and ABCG2 ATPase assay | |
| Cell Lines | RCSC cells | |
| Concentrations | 0~10 μM | |
| 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). |
-1.jpg) |
Source | J Korean Med Sci (2016). Figure 4. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience Inc. (Houston, USA). |
| Method | CCK8 Assay and flow cytometry analysis | |
| Cell Lines | RCSC cells | |
| Concentrations | 0~10 μM | |
| Incubation Time | 72 h | |
| Results | A lower proliferation rate was observed in RCSCs transfected with miR-3163 Mimics using the CCK-8 assay (Fig. 4A).RCSCs treated with miR-3163 Mimics were more susceptible to cisplatin-induced apoptosis compared to those treated with Scramble (Fig.4B). |
| Molecular Weight | 444.48 |
| Formula | C22H28N4O6 |
| CAS Number | 65271-80-9 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | -20°C, protect from light |
| 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.
[1] Abraham Chang. A case of mitoxantrone extravasation
[2] Mirela Enache, et al. Mitoxantrone-Surfactant Interactions: A Physicochemical Overview
[3] Benny J Evison, et al. Mitoxantrone, More than Just Another Topoisomerase II Poison
[4] F Martinelli Boneschi, et al. Mitoxantrone for multiple sclerosis
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