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Mitoxantrone diacetate

CAS No. : 70711-41-0

MCE 站：Mitoxantrone diacetate

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  TGF-beta/Smad  |  Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：Topoisomerase  |  PKC  |  Apoptosis  |  Endogenous Metabolite

In Vitro: 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.
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, 1.6 mg/kg/day; as a free base) produces a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia.
In SC implanted Lewis lung carcinoma, Mitoxantrone diacetate ａnd ADM administered IV also shows effective antitumor activities ａnd produces a 60% ａnd a 45% ILS, respectively.

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