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65271-80-9生产厂家

65271-80-9价格

65271-80-9

65271-80-9结构式
65271-80-9结构式
  • 常用中文名:米托蒽醌
  • 常用英文名:Mitoxantrone
  • CAS号:65271-80-9
  • 分子式:C22H28N4O6
  • 分子量:444.481
  • 相关类别: 原料药 抗肿瘤药 抗肿瘤辅助用药
  • 发布时间:2018-06-23 20:03:41
  • 更新时间:2024-01-02 21:17:23
  • 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。

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中文名 米托蒽醌
英文名 mitoxantrone
中文别名 1,4-二羟基-5,8-双[[2-[(2-羟乙基)氨基]乙基]氨基]-9,10-蒽醌
米拖蒽醌
英文别名 1,4-Dihydroxy-5,8-bis({2-[(2-hydroxyethyl)amino]ethyl}amino)-9,10-anthraquinone
mitoxanthrone
1,4-Dihydroxy-5,8-bis({2-[(2-hydroxyethyl)amino]ethyl}amino)anthracen-9,10-dion
UNII-BZ114NVM5P
MFCD00242942
PharmasubstanceEP4
1,4-dihydroxy-5,8-bis({2-[(2-hydroxyéthyl)amino]éthyl}amino)anthracène-9,10-dione
DHAQ
1,4-dihydroxy-5,8-bis[[2-(2-hydroxy-ethylamino)ethyl]amino]anthraquinone
9,10-Anthracenedione, 1,4-dihydroxy-5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-
dihydroxyanthraquinone
1,4-dehydroxy-5,8-bis[[[2-(2-hydroxyethyl)amino]ethyl]amino]-9,19-antracenedion
9,10-Anthracenedione, 1,4-dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-
MITOXANTRONUM AND THE INTERMEDIATES
1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione
1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthraquinone
1,4-bis-[2-(2-hydroxyethylamino)ethylamino]-5,8-dihydroxy-9,10-anthracenedione
1,4-bis[2-(2-hydroxyethylamino)ethylamino]-5,8-dihydroxyanthraquinone
Mitoxantrone
[3H]-Mitoxantrone
MITOXANTRONUM
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
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.

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

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

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
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