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Mitoxantrone diacetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Mitoxantrone diacetate图片
CAS NO:70711-41-0

Mitozantrone diacetate
NSC 301739 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 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。
生物活性

Mitoxantrone diacetate is a potenttopoisomeraseIIinhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with anIC50of 8.5 μM. Mitoxantrone diacetate inducesapoptosisof B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity[1][2][3][4]. Mitoxantrone diacetate also has anti-orthopoxvirusactivity withEC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively[5].

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 Kivalue 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 IC50values of 18 and 196 nM, respectively[3].

体内研究
(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[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].

Clinical Trial
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.

 
 
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