| Identification | Back Directory | [Name]
BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]-3-pyridinyl]-3-(trifluoroMethyl)-, MonoMethanesulfonate (9CI) | [CAS]
895519-91-2 | [Synonyms]
CS-1023
HHGV678 mesylate
FluMatinib Mesylate
Flumatinib mesylate (HHGV-678)
N-(6-Methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)
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
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
BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]-3-pyridinyl]-3-(trifluoroMethyl)-, MonoMethanesulfonate (9CI)
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 | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C30H33F3N8O4S | [MDL Number]
MFCD28053502 | [MOL File]
895519-91-2.mol | [Molecular Weight]
658.694 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
H2O : 50 mg/mL (75.91 mM; Need ultrasonic)DMSO : 50 mg/mL (75.91 mM; Need ultrasonic) | [form ]
Powder | [color ]
Light brown to yellow |
| Hazard Information | Back Directory | [Uses]
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 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[1][2]. | [in vivo]
Flumatinib mesylate (HH-GV-678) (18-75 mg/kg; p.o.; Twice daily, for 14 days.) inhibits tumor growth in nude mice[1]. | Animal Model: | Nude mice (subcutaneously injecting K562 cells)[1] | | 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. |
| [IC 50]
PDGFRβ: 307.6 nM (IC50); c-Abl: 1.2 nM (IC50) | [storage]
Store at -20°C | [References]
[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. DOI:10.1038/leu.2010.169
[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. DOI:10.1111/cas.12320 |
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