N-[4-[(3-溴苯基)氨基]-6-喹唑啉基]-2-丁炔酰胺

• 常用名: N-[4-[(3-溴苯基)氨基]-6-喹唑啉基]-2-丁炔酰胺
• 英文名: CL-387,785
• CAS号: 194423-06-8
• 分子量: 381.226
• 密度: 1.6±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₈H₁₃BrN₄O
• 熔点: 276 °C
• 闪点: N/A

名称

• 中文名: N-[4-[(3-溴苯基)氨基]-6-喹唑啉基]-2-丁炔酰胺
• 英文名: N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide

生物活性

• 相关类别:
  研究领域 >> 癌症
• 靶点:

  EGFR:370 pM (IC50)

• 参考文献:

  [1]. Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25.

  [2]. Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57(1):33-40.

  [3]. Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2(11):e313.

  [4]. Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65(16):7096-101.

物理化学性质

• 密度: 1.6±0.1 g/cm3
• 熔点: 276 °C
• 分子式: C₁₈H₁₃BrN₄O
• 分子量: 381.226
• 精确质量: 380.027252
• PSA: 70.40000
• LogP: 4.68
• 外观性状: 固体;White to Orange to Green powder to crystal
• 折射率: 1.755
• 储存条件: <0°C;避免加热

英文别名

• N-{4-[(3-Bromophenyl)amino]-6-quinazolinyl}-2-butynamide
• N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}but-2-ynamide
• CL-387,785
• N-[4-[(3-Bromophenyl)amino]quinazolin-6-yl]but-2-ynamide
• N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide
• 2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-
• EKI-785
• UNII-B4W27J1Z8B
• 4-anilinoquinazoline deriv. 1
• CL-387785