895519-91-2

• 常用中文名：甲磺酸氟马替尼/氟马替尼
• 常用英文名：Flumatinib mesylate
• CAS号：895519-91-2
• 分子式：C₃₀H₃₃F₃N₈O₄S
• 分子量：658.694
• 相关类别： 信号通路 蛋白酪氨酸激酶 BCR-ABL
• 发布时间：2017-01-15 08:26:23
• 更新时间：2026-07-01 09:16:27
• Flumatinib (HH-GV-678)甲磺酸盐是imatinib的衍生物,为多种激酶抑制剂,对c-Abl,PDGFRβ和c-Kit的IC50为1.2 nM,307.6 nM和2662 nM。

名称

• 中文名: 甲磺酸氟马替尼/氟马替尼
• 英文名: methanesulfonic acid,4-[(4-methylpiperazin-1-yl)methyl]-N-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide
• 中文别名: 甲磺酸氟马替尼,10 MM DMSO 溶液; FLUMATINIB (HH-GV-678)甲磺酸盐; N-(6-甲基-5-((4-(吡啶-3-基)嘧啶-2-基)氨基)吡啶-3-基)-4-((4-甲基哌嗪-1-基)甲基)-3-(三氟甲基)苯甲酰胺甲磺酸盐; 甲磺酸氟马替尼; 多种激酶抑制剂(FLUMATINIB MESYLATE)
• 英文别名: N-(6-Methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl); Flumatinib (mesylate); Flumatinib mesylate, 10 mM in DMSO; FluMatinib Mesylate; HHGV-678,PDGFRβ,HHGV678,c-Abl,Bcr-Abl,Platelet-derived owth factor rector,PDGFR,HHGV 678,SCFR,Flumatinib mesylate,c-Kit,Flumatinib,CD117,Inhibitor,inhibit; 4-[(4-Methyl-1-piperazinyl)methyl]-N-(6-methyl-5-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}-3-pyridinyl)-3-(trifluoromethyl)benzamide methanesulfonate (1:1); Flumatinib mesylate (HHGV-678); BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]amino]-3-pyridinyl]-3-(trifluoroMethyl)-, MonoMethanesulfonate (9CI)/FluMatinib Mesylate; HHGV678 mesylate; N-(6-Methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzamide methanesulfonate; Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[6-methyl-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-3-pyridinyl]-3-(trifluoromethyl)-, methanesulfonate (1:1); BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]amino]-3-pyridinyl]-3-(trifluoroMethyl)-, MonoMethanesulfonate (9CI)

物化性质

• 分子式: C₃₀H₃₃F₃N₈O₄S
• 分子量: 658.694
• 精确质量: 658.229736
• PSA: 165.41000
• LogP: 5.92170
• 储存条件: 2-8℃

生物活性

• 描述: Flumatinib (HH-GV-678)甲磺酸盐是imatinib的衍生物,为多种激酶抑制剂,对c-Abl,PDGFRβ和c-Kit的IC50为1.2 nM,307.6 nM和2662 nM。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL
  信号通路 >> 蛋白酪氨酸激酶 >> c-Kit
  研究领域 >> 癌症
• 参考文献:

  [1]. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9.

  [2]. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10.

  [3]. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.