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Mitoxantrone dihydrochloride

CAS No. : 70476-82-3

MCE 站：Mitoxantrone dihydrochloride

产品活性：Mitoxantrone dihydrochloride是拓扑异构酶II (topoisomerase II)的抑制剂；也可抑制蛋白激酶C (PKC)， IC₅₀值为8.5 μM。

研究领域：Cell Cycle/DNA Damage  |  TGF-beta/Smad  |  Epigenetics

作用靶点：Topoisomerase  |  PKC

In Vitro: Mitoxantrone 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. Treatment of B-CLL cells for 48 h with mitoxantrone (0.5 μg/mL) induces a decrease in cell viability. Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone 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 given IP at the optimal dose (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 and ADM administered IV also shows effective antitumor activities and produces a 60% and a 45% ILS, respectively..

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