Mitoxantrone diacetate 是一种有效的拓扑异构酶II (Topoisomerase II) 抑制剂。Mitoxantrone diacetate 也可抑制蛋白激酶 C (PKC)，其IC50值为 8.5 μM。Mitoxantrone diacetate 诱导 B- 慢性淋巴细胞白血病 (B-CLL) 细胞凋亡 (Apoptosis)。Mitoxantrone diacetate 具有抗肿瘤活性。Mitoxantrone diacetate 还具有抗正痘病毒 (orthopoxvirus) 活性，对牛痘和猴痘的EC50分别为 0.25 μM 和 0.8 μM。

Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C ( PKC ) activity with an IC 50 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 EC 50 s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively [5].

Mitoxantrone diacetate inhibits PKC in a competitive manner with respect to histone H1, and its K i value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP [1]. 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 [2]. Mitoxantrone diacetate shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC 50 values of 18 and 196 nM, respectively [3].

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].

70711-41-0

C26H36N4O10

564.58

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years