米托蒽醌

米托蒽醌

中文名称米托蒽醌
中文同义词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;米托蒽醌;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
相关类别有机原料;小分子抑制剂,天然产物;精细化工;细胞生物学试剂;生化试剂;抑制剂;Inhibitors;Pharmaceutical material and intermeidates;Intermediates & Fine Chemicals;Pharmaceuticals;Anti-cancer&immunity;APIs;API
Mol文件65271-80-9.mol
结构式米托蒽醌 结构式

米托蒽醌 性质

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
溶解度DMSO(少量)、甲醇(少量)、水(少量)
酸度系数(pKa)pKa 5.99 (Uncertain);8.13 (Uncertain)
形态固体
颜色深蓝色到黑色
CAS 数据库65271-80-9(CAS DataBase Reference)
(IARC)致癌物分类2B (Vol. 76) 2000

米托蒽醌 用途与合成方法

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。

PKC

8.5 μM (IC 50 )

Topoisomerase II

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.

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。

安全信息

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 Germany3
RTECS号CB5748500
海关编码2922.50.2500

MSDS信息

米托蒽醌 化学药品说明书

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-13502米托蒽醌
Mitoxantrone
65271-80-950mg515元
2024/01/25HY-13502米托蒽醌
Mitoxantrone
65271-80-910mM * 1mLin DMSO567元
"米托蒽醌"相关产品信息
蒽醌 羟乙基纤维素 羟基乙叉二膦酸 羟乙基淀粉 三(羟甲基)氨基甲烷 3-羟基-N,N-二乙基苯胺 羟乙基磺酸钠 酸性绿41 1,8-二氨基-4,5-二羟基-9,10-蒽二酮 酸蓝45 分散兰81 1,2-二羟基蒽醌 盐酸米托蒽醌 注射用盐酸米托蒽醌 5,8-二氯-1,4-二羟基蒽醌 分散兰56 茜素络合指示剂
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