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盐酸米托蒽醌

盐酸米托蒽醌用途

抗肿瘤药。

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盐酸米托蒽醌名称

[ CAS 号 ]:
70476-82-3

[ 中文名 ]:
盐酸米托蒽醌

[ 英文名 ]:
Mitoxantrone 2HCl

[中文别名 ]:

[英文别名 ]:

Mitoxantrone dihydrochloride
MITOXANTHRONE HYDROCHLORIDE
Mitoxantrone 2HCl
MITOZANTRONE
MFCD00242943
MITOXANTRONE HCl
Mitoxantrone hydrochloride
Novantron
Onkotrone
UNII-U6USW86RD0

盐酸米托蒽醌生物活性

[ 描述 ]:

Mitoxantrone dihydrochloride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

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]. Venza I, et al. Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells. Pigment Cell Melanoma Res. 2013 Mar;26(2):193-204.

[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]

盐酸米托蒽醌物理化学性质

[ 沸点 ]:
805.7ºC at 760 mmHg

[ 熔点 ]:
203-205ºC

[ 分子式 ]:
C₂₂H₃₀Cl₂N₄O₆

[ 分子量 ]:
517.403

[ 闪点 ]:
441.1ºC

[ 精确质量 ]:
516.154236

[ PSA ]:
163.18000

[ LogP ]:
2.39260

[ 外观性状 ]:
固体;Dark green to Dark purple to Black powder to crystal

[ 储存条件 ]:
0-10°C;避免加热

[ 水溶解性 ]:
水溶性：实际上不溶；微溶：甲醇；不溶：氯仿,丙酮

盐酸米托蒽醌MSDS

详细MSDS(安全技术说明书)

盐酸米托蒽醌毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CB0386900

CHEMICAL NAME :: Anthracenedione, 1,4-dihydroxy-5,8-bis((2-((2-hydroxyethyl)amino)ethyl )amino)-, dihydrochloride

CAS REGISTRY NUMBER :: 70476-82-3

LAST UPDATED :: 199806

DATA ITEMS CITED :: 29

MOLECULAR FORMULA :: C22-H28-N4-O6.2Cl-H

MOLECULAR WEIGHT :: 517.46

WISWESSER LINE NOTATION :: L C666 BV IVJ DQ GQ KM2M2Q NM2M2Q &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4400 ug/kg/30W-I

TOXIC EFFECTS :: Skin and Appendages - nails

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 71 ug/kg/2W-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage)

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 682 mg/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 :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1640 mg/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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8 mg/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 - rat

DOSE/DURATION :: 5500 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 - rat

DOSE/DURATION :: 4800 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 502 mg/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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 16500 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 :: 19700 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 :: 9700 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 :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1200 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 :: Mammal - dog

DOSE/DURATION :: 375 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 :: Primate - monkey

DOSE/DURATION :: >1 mg/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 :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 125 mg/kg

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

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 310 ng/L

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 36,1375,1986

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盐酸米托蒽醌安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H340-H360

[ 警示性声明 ]:
P201-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;T+: Very toxic;

[ 风险声明 (欧洲) ]:
R46;R61

[ 安全声明 (欧洲) ]:
53-36/37/39-45-22

[ 危险品运输编码 ]:
UN 3249

[ WGK德国 ]:
3

[ RTECS号 ]:
CB5748500

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2914610000

盐酸米托蒽醌合成路线

详细合成路线

盐酸米托蒽醌上下游产品

盐酸米托蒽醌上游产品

盐酸米托蒽醌下游产品

盐酸米托蒽醌海关

[ 海关编码 ]: 2914610000

[ 中文概述 ]:
2914610000 蒽醌。监管条件:无。增值税率:17.0%。退税率:9.0%。最低关税:5.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙酮报明包装

[ Summary ]:
2914610000 anthracene-9,10-dione。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。Lowest tariff:5.5%。General tariff:30.0%

盐酸米托蒽醌文献

Molecular mechanism of T-cell protein tyrosine phosphatase (TCPTP) activation by mitoxantrone.

Biochim. Biophys. Acta 1834(10) , 1988-97, (2013)

T-cell protein tyrosine phosphatase (TCPTP) is a ubiquitously expressed non-receptor protein tyrosine phosphatase. It is involved in the negative regulation of many cellular signaling pathways. Thus, ...

Phase II trial assessing granulocyte-macrophage-colony stimulating factor, ketoconazole plus mitoxantrone in metastatic castration-resistant prostate cancer progressing after docetaxel treatments.

Cancer Invest. 31(3) , 177-82, (2013)

This study evaluated objective response and safety for the combination of granulocyte macrophage-colony stimulating factor (GM-CSF), ketoconazole, and mitoxantrone in castration-resistant prostate can...

Sequential therapy with alternating short courses of R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, prednisone) and R-FM (rituximab, fludarabine, mitoxantrone) followed by autologous stem cell transplantation results in long term remission in advanced follicular lymphoma.

Br. J. Haematol. 166(4) , 625-8, (2014)

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