甲磺酸氟马替尼/氟马替尼

• 常用名: 甲磺酸氟马替尼/氟马替尼
• 英文名: Flumatinib mesylate
• CAS号: 895519-91-2
• 分子量: 658.694
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₀H₃₃F₃N₈O₄S
• 熔点: N/A
• 闪点: N/A

甲磺酸氟马替尼/氟马替尼用途

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。

甲磺酸氟马替尼/氟马替尼名称

• 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

甲磺酸氟马替尼/氟马替尼生物活性

• 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.

甲磺酸氟马替尼/氟马替尼物理化学性质

• 分子式: C₃₀H₃₃F₃N₈O₄S
• 分子量: 658.694
• 精确质量: 658.229736
• PSA: 165.41000
• LogP: 5.92170
• InChIKey: ZSASDYCFROUKTJ-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)O.Cc1ncc(NC(=O)c2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1Nc1nccc(-c2cccnc2)n1
• 储存条件: 2-8℃

甲磺酸氟马替尼/氟马替尼靶点实验

查看更多实验

实验名称：Antitumor activity against human K562 cells xenografted in BALB/cA nude mouse assesse... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881248

实验名称：Antitumor activity against human K562 cells xenografted in po dosed BALB/cA nude mous... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881249

实验名称：Antitumor activity against human K562 cells xenografted in BALB/cA nude mouse assesse... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881251

实验名称：Potency index, ratio of imatinib IC50 to compound IC50 for Bcr-Abl in human K562 cell... 来源：ChEMBL 靶标：Breakpoint cluster region protein External Id：CHEMBL3881246

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Antitumor activity against human K562 cells xenografted in BALB/cA nude mouse assesse... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881247

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

实验名称：Antitumor activity against human K562 cells xenografted in BALB/cA nude mouse assesse... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881252

实验名称：Toxicity in BALB/cA nude mouse xenografted with human K562 cells assessed as body wei... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL3881253

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

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甲磺酸氟马替尼/氟马替尼英文别名

• 4-[(4-Methyl-1-piperazinyl)methyl]-N-(6-methyl-5-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}-3-pyridinyl)-3-(trifluoromethyl)benzamide methanesulfonate (1:1)
• Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[6-methyl-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-3-pyridinyl]-3-(trifluoromethyl)-, methanesulfonate (1:1)
• Flumatinib mesylate
• Flumatinib (mesylate)