Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl . Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC 50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model In Vitro Flumatinib mesylate (HH-GV-678) (0-1000 μM; 4, 7 and 10 days) blocks cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation in K562 leukemia cells. Flumatinib mesylate (HH-GV-678) (0-10 μM; 72 hours) remarkably decreases the number of cells in chronic myelogenous leukemia cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Chronic myelogenous leukemia cell line Concentration: 0-10 μM Incubation Time: 72 hours Result: The proliferation inhibitory activity was 32-to 58-fold more potent than that of imatinib and 2-to 5-fold more potent than that of nilotinib. Western Blot AnalysisCell Line: K562 cells Concentration: 0, 1, 3, 10, 30, 100, 300 and 1000 μM Incubation Time: 4, 7 and 10 days Result: Suppressed cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. In Vivo Flumatinib mesylate (HH-GV-678) (18-75 mg/kg; p.o.; Twice daily, for 14 days.) inhibits tumor growth in nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (subcutaneously injecting K562 cells) Dosage: 18.75, 37.5, 75 mg/kg Administration: Oral administration; Twice daily, for 14 days. Result: Inhibited the growth of K562 xenografts in a dose-dependent manner and induced regression in all tumors at a daily dose of 75 mg/kg for nine days. Form:Solid IC50& Target:PDGFRβ 307.6 nM (IC 50 ) c-Abl 1.2 nM (IC 50 )
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Flumatinib mesylate
CAS number：895519-91-2 molecular formula：C30H33F3N8O4S
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| Chinese alias | 甲磺酸氟马替尼 | ||
| English alias | MFCD28053502 | DTXSID9026184 | SCHEMBL4889246 | EX-A2059 | N-(6-methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzamide mesylate | N-methyl-N-nitrosouree | Q27271825 | 95Y8L63NBC | DTXS | ||
| CAS number | 895519-91-2 | molecular formula | C30H33F3N8O4S |
| molecular weight | 658.7 g/mol | Exact mass | ≥99% |
| PSA | 162.000 Ų | logp | - |
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