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Mitoxantrone dihydrochloride

MCE China：Mitoxantrone dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-13502A

CAS：70476-82-3

Synonyms：Mitozantrone dihydrochloride; NSC 301739 dihydrochloride

Purity：99.55%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

In Vitro：Mitoxantrone dihydrochloride inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP[1].Mitoxantrone dihydrochloride (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone dihydrochloride induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone dihydrochloride is due to induction of apoptosis[2].Mitoxantrone dihydrochloride shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively[3].

In Vivo：Mitoxantrone dihydrochloride (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 dihydrochloride (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].

Animal Administration：Mice: Mitoxantrone is tested for antitumor activity against experimental tumors in mice and the results are compared with those of seven antitumor antibiotics. The drugs are given IP or IV, in general on days 1, 5, and 9 following tumor inoculation. Mitoxantrone is given IP at the optimal dose (1.6 mg/kg/day; as a free base)[4].

Cell Assay：The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay[3].

IC50 & Target：PKC 8.5 μM (IC50) Topoisomerase II

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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.  [Content Brief]

[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.  [Content Brief]

[3]. Venza I, et al. Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells. Pigment Cell Melanoma Res. 2013 Mar;26(2):193-204.  [Content Brief]

[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.  [Content Brief]

[5]. Sharon E Altmann, et al. Inhibition of cowpox virus and monkeypox virus infection by mitoxantrone. Antiviral Res. 2012 Feb;93(2):305-308.  [Content Brief]