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盐酸硫蒽酮

盐酸硫蒽酮用途

Lucanthone hydrochloride 是 Apurinic 内切核酸酶-1 (APE-1) 的内切核酸酶抑制剂。

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盐酸硫蒽酮名称

[ CAS 号 ]:
548-57-2

[ 中文名 ]:
盐酸硫蒽酮

[ 英文名 ]:
Lucanthone hydrochloride

[英文别名 ]:

Lycanthone
thioxanthone

盐酸硫蒽酮生物活性

[ 描述 ]:

Lucanthone hydrochloride 是 Apurinic 内切核酸酶-1 (APE-1) 的内切核酸酶抑制剂。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 自噬 >> 自噬

[ 靶点 ]

APE-1[1]

[体外研究]

盐酸Lucantone是一种新型的自噬抑制剂,可诱导组织蛋白酶D介导的细胞凋亡。为了研究盐酸Lucantone的抗癌活性,用MTT法测定细胞活力。在一个由七个癌症细胞系组成的小组中,盐酸Lucanthone将细胞活力降低到类似的程度。此外,直接比较显示,在降低乳腺癌症细胞活力方面,盐酸Lucanthone的效力显著高于氯喹(CQ),平均IC50为7.2μM,而CQ为66μM。通过ATPlite测定和台盼蓝排除法测量两种具有代表性的细胞系(MDA-MB-231和BT-20)的细胞活力可得出类似的结果[2]。

[参考文献]

[1]. Chowdhury SM, et al. Graphene nanoribbons as a drug delivery agent for lucanthone mediated therapy of glioblastoma multiforme. Nanomedicine. 2015 Jan;11(1):109-18.

[2]. Carew JS, et al. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. J Biol Chem. 2011 Feb 25;286(8):6602-13.

盐酸硫蒽酮物理化学性质

[ 沸点 ]:
512.4ºC at 760 mmHg

[ 熔点 ]:
195-196ºC

[ 分子式 ]:
C₂₀H₂₅ClN₂OS

[ 分子量 ]:
376.94

[ 闪点 ]:
263.7ºC

[ 精确质量 ]:
376.13800

[ PSA ]:
60.58000

[ LogP ]:
5.35180

盐酸硫蒽酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XO1605800

CHEMICAL NAME :: Thioxanthen-9-one, 1-(2-(diethylaminoethyl)amino)-4-methyl-, monohydrochloride

CAS REGISTRY NUMBER :: 548-57-2

LAST UPDATED :: 199707

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C20-H24-N2-O-S.Cl-H

MOLECULAR WEIGHT :: 376.98

WISWESSER LINE NOTATION :: T C666 BS IVJ D1 GM2N2&2 &GH

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 :: 181 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >500 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

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

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Sex chromosome loss and nondisjunction

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - mouse Lymphocyte

DOSE/DURATION :: 1 mg/L/2H

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 59,61,1979

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盐酸硫蒽酮安全信息

[ 海关编码 ]:
2932999099

盐酸硫蒽酮海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%