米托蒽醌

中文名称:

米托蒽醌

中文同义词:

米托蒽醌;1,4-二羟基-5,8-双[[2-[(2-羟乙基)氨基]乙基]氨基]-9,10-蒽醌;米托蒽醌(米托恩醌、米拖蒽醌);盐酸米托蒽醌 (HPLC);米拖蒽醌;米托恩醌;1,4-二羟基-5,8-二[[2-[(2-羟基乙基)氨基]乙基]氨基]蒽-9,10-二酮;拓扑异构酶II(TOPOISOMERASE II)抑制剂(MITOXANTRONE)

英文名称:

Mitoxantrone

英文同义词:

MITOXANTRONE;1,4-dihydroxy-5,8-bis(2-((2-hydroxyethyl)amino)ethylamino)-9,10-anthracenedi;1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino)ethylamino]-anthracene-9,10-dione;Mitoxantrone (base and/or unspecified salts);MITOXANTRONUM;1,4-Dihydroxy-5,8-bis[2-[(2-hydroxyethyl)amino]ethylamino]-9,10-anthraquinone;MitoxantroneBase;Mitoxantrone Hcl 70476-82-3 / Base

CAS号:

65271-80-9

分子式:

C22H28N4O6

分子量:

444.48

EINECS号:

1533716-785-6

相关类别:

精细化工;有机原料;小分子抑制剂，天然产物;细胞生物学试剂;生化试剂;Inhibitors;Anti-cancerimmunity;Pharmaceutical material and intermeidates;Intermediates Fine Chemicals;Pharmaceuticals

Mol文件:

65271-80-9.mol

熔点

170-1740C

沸点

554.47°C (rough estimate)

密度

1.3049 (rough estimate)

折射率

1.6500 (estimate)

储存条件

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

pKa 5.99 (Uncertain);8.13 (Uncertain)

CAS 数据库

65271-80-9(CAS DataBase Reference)

(IARC)致癌物分类

2B (Vol. 76) 2000

生物活性

Mitoxantrone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。

靶点

PKC 8.5 μM (IC 50 ) Topoisomerase II

PKC 8.5 μM (IC 50 )

Topoisomerase II

体外研究

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 IC 50 values of 18 and 196 nM, respectively.

体内研究

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..

化学性质

蓝黑色结晶。熔点203-205℃。略溶于水，微溶于乙醇，不溶于氯仿和丙酮。无臭，易吸潮

用途

蒽环类抗癌药，抗癌活性与阿霉素相似或略高，明显高于环磷酰胺、阿糖胞苷、甲氨喋呤、氟脲嘧啶、长春新碱等常用的抗癌药。临床用于乳腺癌有突出的疗效。

危险品标志

T,T+

危险类别码

46-61-26/27/28

安全说明

53-36/37/39-45-22

WGK Germany

RTECS号