Flumatinib mesylate
Flumatinib mesylate Basic information
- Product Name:
- Flumatinib mesylate
- Synonyms:
-
- 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
- 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
- N-(6-Methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)
- 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
- CS-1023
- HHGV678 mesylate
- Flumatinib mesylate (HHGV-678)
- CAS:
- 895519-91-2
- MF:
- C30H33F3N8O4S
- MW:
- 658.6944296
- EINECS:
- 200-258-5
- Mol File:
- 895519-91-2.mol
Flumatinib mesylate Chemical Properties
- 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
Flumatinib mesylate Usage And Synthesis
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].
Synthesis
Synthesis of Flumatinib Mesylate
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)
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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