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Mitoxantrone-diacetate

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Category Orthopoxvirus
CAS 70711-41-0
Description 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.
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Product Information

Synonyms Dhaq diacetate|Mitoxantrone diacetate|D08FPM|1,4-Dihydroxy-5,8-bis(2-((2-hydroxyethyl)amino)ethylamino)-9,10-anthracenedione diacetate|70711-41-0|5,8-Bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-dihydroxy-9,10-anthracenedione diacetate|5,8-Bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-dihydroxyanthraquinone 1,4-diaceate|Anthraquinone, 5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-dihydroxy-, 1,4-diacetate (salt)|2-[[5,8-dihydroxy-4-[2-(2-hydroxyethylazaniumyl)ethylamino]-9,10-dioxoanthracen-1-yl]amino]ethyl-(2-hydroxyethyl)azanium diacetate
Molecular Weight 564.58
Molecular Formula C26H36N4O10
Purity ≥98% (HPLC)
Solubility In vitro:
10 mM in DMSO
Appearance Solid powder
Storage Store at -20°C
In Vitro Mitoxantrone diacetate 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.
Mitoxantrone diacetate (0.5 μg/mL, 48 h) induces a decrease in B-CLL cells. Mitoxantrone diacetate induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of Mitoxantrone diacetate is due to induction of Apoptosis.
Mitoxantrone diacetate shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively.
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.
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.
PSA 144.91000
Target Topoisomerase; PKC; Orthopoxvirus; Apoptosis; Endogenous Metabolite

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