Mitoxantrone diacetate(Synonyms: NSC 299195; Mitozantrone diacetate)

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Mitoxantrone diacetate (Synonyms: NSC 299195; Mitozantrone diacetate)

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(Synonyms: NSC 299195; Mitozantrone diacetate)

Mitoxantrone diacetate Chemical Structure

CAS No. : 70711-41-0

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Mitoxantrone diacetate 的其他形式现货产品:

Mitoxantrone Mitoxantrone dihydrochloride

生物活性

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. Mitoxantrone diacetate shows antitumor activity[1][2][3][4].

IC50 & Target

Topoisomerase II

 

PKC

8.5 μM (IC50)

体外研究
(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[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 IC50 values of 18 and 196 nM, respectively[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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[4].
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[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

564.58

Formula

C26H36N4O10
CAS 号

70711-41-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

    [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.

    [3]. Vibet S, et al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines. Drug Metab Dispos. 2007 May;35(5):822-8.

    [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.

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