89459-25-6

• 常用中文名：N-[2-(二甲基氨基)乙基]-4-吖啶甲酰胺
• 常用英文名：XR-5000
• CAS号：89459-25-6
• 分子式：C₁₈H₁₉N₃O
• 分子量：293.36300
• 相关类别： 信号通路 细胞周期/DNA损伤 拓扑异构酶
• 发布时间：2016-09-01 03:13:39
• 更新时间：2024-01-14 11:41:29
• DACA 在体外抑制两种必需的核酶,DNA 拓扑异构酶 I (topo I) 和 DNA拓扑异构酶 II (topo II) 。DACA 稳定人白血病 CCRF-CEM 细胞中的 topo I, topo II α 和 topo II β 可切割复合物。

名称

• 中文名: N-[2-(二甲基氨基)乙基]-4-吖啶甲酰胺
• 英文名: N-[2-(dimethylamino)ethyl]acridine-4-carboxamide
• 英文别名: Acridine carboxamide; N-(2-(Dimethylamino)ethyl)-4-acridinecarboxamide; N-(2-(Dimehtylamino)ehtyl)acridine-4-carboxamide; Daca; 4-Acridinecarboxamide,N-(2-(dimethylamino)ethyl); N-[2-(Dimethyl-amino)ethyl]acridine-4-carboxamide

物化性质

• 密度: 1.182g/cm3
• 沸点: 544.1ºC at 760 mmHg
• 分子式: C₁₈H₁₉N₃O
• 分子量: 293.36300
• 闪点: 282.9ºC
• 精确质量: 293.15300
• PSA: 48.72000
• LogP: 3.25420
• 折射率: 1.657
• 储存条件: 2-8°C

生物活性

• 描述: DACA 在体外抑制两种必需的核酶,DNA 拓扑异构酶 I (topo I) 和 DNA拓扑异构酶 II (topo II) 。DACA 稳定人白血病 CCRF-CEM 细胞中的 topo I, topo II α 和 topo II β 可切割复合物。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶
• 参考文献:

  [1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000;60(6):817-821.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AR7622610 CHEMICAL NAME : 4-Acridinecarboxamide, N-(2-(dimethylamino)ethyl)- CAS REGISTRY NUMBER : 89459-25-6 LAST UPDATED : 199612 DATA ITEMS CITED : 2 MOLECULAR FORMULA : C18-H19-N3-O MOLECULAR WEIGHT : 293.40 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 44597 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold MUTATION DATA TYPE OF TEST : Mutation in microorganisms TEST SYSTEM : Bacteria - Salmonella typhimurium DOSE/DURATION : 150 nmol/plate REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 268,35,1992

合成路线

188054-38-8 ~% 89459-25-6

文献：Spicer, Julie A.; Gamage, Swarna A.; Atwell, Graham J.; Finlay, Graeme J.; Baguley, Bruce C.; Denny, William A. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1919 - 1929

108-00-9 188054-45-7 ~62% 89459-25-6

文献：Gamage, Swarna A.; Spicer, Julie A.; Rewcastle, Gordon W.; Denny, William A. Tetrahedron Letters, 1997 , vol. 38, # 4 p. 699 - 702 Title/Abstract Full Text View citing articles Show Details Spicer, Julie A.; Gamage, Swarna A.; Atwell, Graham J.; Finlay, Graeme J.; Baguley, Bruce C.; Denny, William A. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1919 - 1929

100038-81-1 ~% 89459-25-6

文献：Gamage, Swarna A.; Spicer, Julie A.; Rewcastle, Gordon W.; Denny, William A. Tetrahedron Letters, 1997 , vol. 38, # 4 p. 699 - 702

24782-64-7 ~% 89459-25-6

文献：Atwell, Graham J.; Rewcastle, Gordon W.; Baguley, Bruce C.; Denny, William A. Journal of Medicinal Chemistry, 1987 , vol. 30, # 4 p. 664 - 669