| Identification | Back Directory | [Name]
NSC 299195 | [CAS]
70711-41-0 | [Synonyms]
NSC 299195
Mitoxantrone (diacetate)
2-[[5,8-dihydroxy-4-[2-(2-hydroxyethylazaniumyl)ethylamino]-9,10-dioxoanthracen-1-yl]amino]ethyl-(2-hydroxyethyl)azanium:diacetate | [Molecular Formula]
C24H32N4O8 | [MOL File]
70711-41-0.mol | [Molecular Weight]
504.54 |
| Hazard Information | Back Directory | [Description]
Mitoxantrone diacetate is an anthraquinone that intercalates in DNA and inhibits topoisomerase II. | [Uses]
Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity[1][2][3][4]. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively[5]. | [in vivo]
Mitoxantrone diacetate (IP, 0-3.2 mg/kg/day) produces a statistically significant number of 60-day survivors at 1.6 mg/kg in mice with IP implanted L1210 leukemia[4].
Mitoxantrone diacetate (IV, 0-3.2 mg/kg/day) shows effective antitumor activities and produces a 60% ILS (increase in lifespan) at 3.2 mg/kg in SC implanted Lewis lung carcinoma[4]. | [IC 50]
Topoisomerase II; PKC: 8.5 μM (IC50) | [References]
[1] Takeuchi N, et al. Inhibitory effect of mitoxantrone on activity of protein kinase C and growth of HL60 cells. J Biochem. 1992 Dec;112(6):762-7. DOI:10.1093/oxfordjournals.jbchem.a123972
[2] Bellosillo B, et al. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6. DOI:10.1046/j.1365-2141.1998.00520.x
[3] Vibet S, et al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines. Drug Metab Dispos. 2007 May;35(5):822-8. DOI:10.1124/dmd.106.013474
[4] Fujimoto S, et al. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-62. DOI:10.1007/BF00255476
[5] Sharon E Altmann, et al. Inhibition of cowpox virus and monkeypox virus infection by mitoxantrone. Antiviral Res. 2012 Feb;93(2):305-308. DOI:10.1016/j.antiviral.2011.12.001 |
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