847949-49-9

• 常用中文名：4-[(3-氯-4-氟苯基)氨基]-6-[3-(4-吗啉基)丙氧基]-7-羟基喹唑啉
• 常用英文名：O-Desmethyl gefitinib
• CAS号：847949-49-9
• 分子式：C₂₁H₂₂ClFN₄O₃
• 分子量：432.87600
• 相关类别： 信号通路 JAK/STAT信号通路 EGFR
• 发布时间：2018-12-17 16:37:11
• 更新时间：2026-07-15 16:43:21
• O-Desmethyl gefitinib 是 Gefitinib 在人血浆中的活性代谢产物。O-Desmethyl gefitinib 的形成依赖于 CYP2D6 活性。在亚细胞试验中,O-Desmethyl gefitinib 抑制 EGFR,IC50 为 36 nM。

名称

• 中文名: 4-[(3-氯-4-氟苯基)氨基]-6-[3-(4-吗啉基)丙氧基]-7-羟基喹唑啉
• 英文名: 4-(3-chloro-4-fluoroanilino)-6-(3-morpholin-4-ylpropoxy)-1H-quinazolin-7-one
• 中文别名: 7-羟基喹唑啉,4-[(3-氯-4-氟苯基)氨基]-6-[3-(4-吗啉基)丙氧基]; O-去甲吉非替尼; O-去甲基吉非替尼,10 MM DMSO 溶液; 7-羟基喹唑啉, 4-[(3-氯-4-氟苯基)氨基]-6-[3-(4-吗啉基)丙氧基]; 吉非替尼杂质; 氧位O-脱甲基吉非替尼; 吉非替尼O-地甲基杂质; 4-((3-氯-4-氟苯基)氨基)-6-(3-吗啉丙氧基)喹唑啉-7-醇; 吉非替尼杂质03; 吉非替尼杂质H; O-Desmethyl gefitinib (O-去甲基吉非替尼); O-去甲基吉非替尼; 氘8-O-去甲基吉非替尼; O-Demethyl-Gefitinib 试剂; 吉非替尼杂质11盐酸盐; 去甲基吉非替尼; 吉非替尼杂质-11; 氧去甲基吉非替尼杂质; O-去甲基吉非替尼 D8
• 英文别名: Gefitinib impurity 11 HCl; M523595; O-Desmethyl gefitinib, 10 mM in DMSO; 7-Quinazolinol,4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]; 4-[(3-Chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol; Gefitinib Impurity (O-Desmethyl Gefitinib): 4-[(3-Chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol; human,Gefitinib,O-Desmethyl gefitinib,ODesmethyl gefitinib,plasma,inhibit,HER1,EGFR,CYP2D6,idermal owth factor rector,O Desmethyl gefitinib,ErbB-1,Inhibitor; Gefitinib Impurity 13; Gefitinib impurity 6/O-Desmethyl Gefitinib/4-((3-chloro-4-fluorophenyl)amino)-6-(3-morpholinopropoxy)quinazolin-7-ol; 4-(3-chloro-4-fluoro-anilino)-6-(3-morpholinopropoxy)quinazolin-7-ol; 7-Quinazolinol, 4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-Morpholinyl)propoxy]; 4-[(3-Chloro-4-fluorophenyl)amino]-6-[3-(morpholin-4-yl)propoxy]quinazolin-7-ol (O-Demethylgefitinib); 4-((3-chloro-4-fluorophenyl)amino)-6-(3-morpholinopropoxy)quinazolin-7-ol; 4-(3'-chloro-4'-fluoroanilino)-7-hydroxy-6-(3-morpholinopropoxy)quinazoline; D8-O-Desmethyl Gefitinib; N-(3-chloro-4-fluorophenyl)-6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-amine; Gefitinib O-Desmethyl Impurity; Gefitinib impurity H; O-Demethyl-Gefitinib; O-DesmethylGefitinibmetabolite; Gefitinib impurities133; Gefitinib Impurity 1; O-Desmethyl Gefitinib; Gefitinib-7

物化性质

• 密度: 1.386g/cm3
• 沸点: 606.4ºC at 760 mmHg
• 熔点: 117-120ºC
• 分子式: C₂₁H₂₂ClFN₄O₃
• 分子量: 432.87600
• 闪点: 320.5ºC
• 精确质量: 432.13600
• PSA: 79.74000
• LogP: 3.98350
• 折射率: 1.65
• 储存条件: -20°C，密闭，干燥

生物活性

• 描述: O-Desmethyl gefitinib 是 Gefitinib 在人血浆中的活性代谢产物。O-Desmethyl gefitinib 的形成依赖于 CYP2D6 活性。在亚细胞试验中,O-Desmethyl gefitinib 抑制 EGFR,IC50 为 36 nM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> JAK/STAT信号通路 >> EGFR
  信号通路 >> 蛋白酪氨酸激酶 >> EGFR
• 靶点:

  IC50: 36 nM (EGFR)[2]

• 参考文献:

  [1]. Kobayashi H, et al. Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinib. Med Oncol. 2016 Jun;33(6):57.

  [2]. McKillop D, et al. Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica. 2006 Jan;36(1):29-39.

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• 海关编码: 2934999090

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海关编码	2934999090
中文概述	2934999090. 其他杂环化合物. 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%
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Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%