57998-68-2

• 常用中文名：亚丝醌
• 常用英文名：Carbamic acid,N,N'-[2,5-bis(1-aziridinyl)-3,6-dioxo-1,4-cyclohexadiene-1,4-diyl]bis-,C,C'-diethyl ester
• CAS号：57998-68-2
• 分子式：C₁₆H₂₀N₄O₆
• 分子量：364.35300
• 相关类别： 研究领域 癌症
• 发布时间：2018-08-31 23:03:30
• 更新时间：2024-01-13 17:33:48
• 二氮醌(Diaziquone)是一种水溶性合成叠氮啶基苯醌,具有潜在的抗肿瘤活性[1]。

名称

• 中文名: 亚丝醌
• 英文名: ethyl N-[2,5-bis(aziridin-1-yl)-4-(ethoxycarbonylamino)-3,6-dioxocyclohexa-1,4-dien-1-yl]carbamate
• 中文别名: 地吖醌
• 英文别名: AZQ; 2,5-di(aziridin-1-yl)-3,6-bis(carboethoxyamino)-1,4-benzoquinone; 3,6-bis<(ethylcarboxy)amino>-2,5-diaziridinyl-1,4-benzoquinone; 2,5-diaziridinyl-3,6-bis(carboethoxy-amino)-1,4-benzoquinone; diaziquone; CI-904; Diaziquonum [INN-Latin]; Aziridinylquinone; Aziridinylbenzoquinone

物化性质

• 密度: 1.45g/cm3
• 沸点: 469ºC at 760mmHg
• 分子式: C₁₆H₂₀N₄O₆
• 分子量: 364.35300
• 闪点: 237.4ºC
• 精确质量: 364.13800
• PSA: 116.82000
• LogP: 0.34240
• 折射率: 1.62
• 储存条件: 通风低温干燥,与库房食品原料分开存放

生物活性

• 描述: 二氮醌(Diaziquone)是一种水溶性合成叠氮啶基苯醌,具有潜在的抗肿瘤活性[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 其他 >> 其他
• 体内研究: 二氮醌(6.75mg/m2,连续5天或单剂量26mg/m2)对原发性神经系统肿瘤具有广泛的二氮醌活性,并与1,3-双(2-氯乙基)-1-亚硝基脲或丙卡巴嗪联合使用对无胸腺小鼠具有增强作用[1]。动物模型：纯合nu/nu BALB/c无胸腺小鼠[1]剂量：6.75mg/sq m或26 mg/sq m给药：6.75mg/m2,连续5天每天给药,或单次给药26 mg/sqm结果：显示无胸腺鼠血浆中的快速清除,半衰期约为11.5 min。产生显著的生长延迟。导致中位生长延迟显著增加,肿瘤退变数量显著增加。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : EY8794000 CHEMICAL NAME : Carbamic acid, (2,5-bis(1-aziridinyl)-3,6-dioxo-1,4-cyclohexadien-1, 4-diyl)bis-, diethyl ester CAS REGISTRY NUMBER : 57998-68-2 BEILSTEIN REFERENCE NO. : 1333277 LAST UPDATED : 199612 DATA ITEMS CITED : 18 MOLECULAR FORMULA : C16-H20-N4-O6 MOLECULAR WEIGHT : 364.40 WISWESSER LINE NOTATION : L6V DV AU DUTJ BMVO2 C- AT3NTJ& EMVO2 F- AT3NTJ 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 : 11290 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 : 10300 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 1250 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 : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 1550 ug/kg/5D-I TOXIC EFFECTS : Behavioral - food intake (animal) Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 2400 ug/kg/33D-I TOXIC EFFECTS : Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 6250 ug/kg/5D-I TOXIC EFFECTS : Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified) Blood - changes in spleen TYPE OF TEST : Micronucleus test TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : Sister chromatid exchange MUTATION DATA TYPE OF TEST : Unscheduled DNA synthesis TEST SYSTEM : Rodent - hamster Ovary DOSE/DURATION : 300 nmol/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: 24,322,1983

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 40

合成路线

17619-22-6 33251-22-8 ~85% 57998-68-2

文献：United States of America Patent: US4337196 A1, 1982 ;

151-56-4 33251-22-8 ~78% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

3908-48-3 ~% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

24118-25-0 ~% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

125659-82-7 ~% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

24118-24-9 ~% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

81720-96-9 ~% 57998-68-2

文献：Dzielendziak, Adam; Butler, John Synthesis, 1989 , # 8 p. 643 - 645

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17619-22-6 33251-22-8 151-56-4 3908-48-3
24118-25-0 81720-96-9
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