548-57-2

• 常用中文名：盐酸硫蒽酮
• 常用英文名：Lucanthone hydrochloride
• CAS号：548-57-2
• 分子式：C₂₀H₂₅ClN₂OS
• 分子量：376.94
• 相关类别： 信号通路 自噬 自噬
• 发布时间：2018-04-20 08:00:00
• 更新时间：2024-01-09 10:54:37
• Lucanthone hydrochloride 是 Apurinic 内切核酸酶-1 (APE-1) 的内切核酸酶抑制剂。

名称

• 中文名: 盐酸硫蒽酮
• 英文名: lucanthone hydrochloride
• 英文别名: 1-(2-Diaethylamino-aethylamino)-4-methyl-thioxanthen-9-on,Hydrochlorid; 1-(2-Diethylamino-ethylamino)-4-methylthiaxanthon,Lucanthon; Lycanthone; 1-(2-diethylamino-ethylamino)-4-methyl-thioxanthen-9-one,hydrochloride; thioxanthone; 1-(2-diethylamino-ethylamino)-4-methyl-thioxanthen-9-one; 1-<2-Diaethylamino-aethylamino>-4-methyl-thioxanthenon-(9); 1-[[2-(Diethylamino)ethyl]amino]-4-methyl-9H-thioxanthen-9-one; 1-(2-Diaethylamino-aethylamino)-4-methyl-thioxanthen-9-on

物化性质

• 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

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.

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

安全

• 海关编码: 2932999099

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%