<生产厂家价格>

米托蒽醌

米托蒽醌用途

【用途一】
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。

米托蒽醌名称

[ CAS 号 ]:
65271-80-9

[ 中文名 ]:
米托蒽醌

[ 英文名 ]:
Mitoxantrone

[中文别名 ]:

米拖蒽醌

[英文别名 ]:

mitoxanthrone
UNII-BZ114NVM5P
MFCD00242942
PharmasubstanceEP4
DHAQ
dihydroxyanthraquinone
MITOXANTRONUM AND THE INTERMEDIATES
Mitoxantrone
[3H]-Mitoxantrone
MITOXANTRONUM

米托蒽醌生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

研究领域 >> 癌症

[ 靶点 ]

PKC:8.5 μM (IC50)

Topoisomerase II

[体外研究]

米托蒽醌以相对于组蛋白H1的竞争性方式抑制PKC,并且其Ki值为6.3μM并且以非竞争性方式相对于磷脂酰丝氨酸和ATP [1]。用米托蒽醌(0.5μg/ mL)处理B-CLL细胞48小时诱导细胞活力降低。米托蒽醌诱导DNA片段化和聚(ADP-核糖)聚合酶(PARP)的蛋白水解切割,证明米托蒽醌的细胞毒性作用是由于诱导细胞凋亡[2]。米托蒽醌显示对人乳腺癌细胞系MDA-MB-231和MCF-7的细胞毒性,IC50值分别为18和196 nM [3]。

[体内研究]

米托蒽醌以最佳剂量(1.6mg/kg /天;作为游离碱)给予IP,在IP植入L1210白血病的小鼠中产生统计学上显着数量的60天存活者(疗效)。在SC植入Lewis肺癌中,米托蒽醌和静脉注射ADM也显示出有效的抗肿瘤活性,分别产生60％和45％的ILS [4]。

[细胞实验]

将人乳腺癌细胞系MDA-MB-231和MCF-7接种在标准96孔板中。接种后一天，更换培养基，并在7天内用含有或不含DHA（30μM）的不同浓度的米托蒽醌（10-5至5μM）的培养基替换。通过四唑盐测定[3]整体测量细胞活力。

[动物实验]

小鼠：测试米托蒽醌对小鼠中实验性肿瘤的抗肿瘤活性，并将结果与七种抗肿瘤抗生素的结果进行比较。通常在肿瘤接种后第1,5和9天给予IP或IV的药物。米托蒽醌以最佳剂量（1.6mg / kg /天;作为游离碱）给予IP [4]。

[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.

[相关活性小分子]

米托蒽醌物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
805.7±65.0 °C at 760 mmHg

[ 熔点 ]:
170-174ºC

[ 分子式 ]:
C₂₂H₂₈N₄O₆

[ 分子量 ]:
444.481

[ 闪点 ]:
441.1±34.3 °C

[ 精确质量 ]:
444.200897

[ PSA ]:
163.18000

[ LogP ]:
0.45

[ 外观性状 ]:
蓝色粉末

[ 蒸汽压 ]:
0.0±3.0 mmHg at 25°C

[ 折射率 ]:
1.709

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：实际上不溶；微溶：甲醇；不溶：丙酮,氯仿

米托蒽醌毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CB5748500

CHEMICAL NAME :: Anthraquinone, 5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-di hydroxy-

CAS REGISTRY NUMBER :: 65271-80-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 22

MOLECULAR FORMULA :: C22-H28-N4-O6

MOLECULAR WEIGHT :: 444.54

WISWESSER LINE NOTATION :: L C666 BV IVJ DQ GQ KM2M2Q NM2M2Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20910 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 86500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16 mg/kg/6W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Liver - other changes Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: DNA damage

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 100 ng/L

REFERENCE :: PAACA3 Proceedings of the American Association for Cancer Research. (Waverly Press, 428 E. Preston St., Baltimore, MD 21202) V.1- 1954- Volume(issue)/page/year: 26,217,1985

米托蒽醌安全信息

[ 危害码 (欧洲) ]:
T,T+

[ 风险声明 (欧洲) ]:
R46

[ 安全声明 (欧洲) ]:
53-36/37/39-45-22

[ 危险品运输编码 ]:
3077.0

[ WGK德国 ]:
3

[ RTECS号 ]:
CB5748500

[ 危险类别 ]:
9.0

米托蒽醌

米托蒽醌用途

米托蒽醌名称

米托蒽醌生物活性

米托蒽醌物理化学性质

米托蒽醌毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

米托蒽醌安全信息

米托蒽醌上下游产品

米托蒽醌上游产品

米托蒽醌下游产品

相关化工产品/化学物质：

相关药品：

推荐生产厂家/供应商：

相关化合物