| 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)- | [CAS]
895519-90-1 | [Synonyms]
HHGV678
FLUMATINIB (HHGV678)
4-[(4-Methyl-1-piperazinyl)methyl]-N-[6-methyl-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-3-pyridinyl]-3-(trifluoromethyl)benzamide
BenzaMide, 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[6-Methyl-5-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]-3-pyridinyl]-3-(trifluoroMethyl)- | [Molecular Formula]
C29H29F3N8O | [MDL Number]
MFCD18633213 | [MOL File]
895519-90-1.mol | [Molecular Weight]
562.59 |
| Chemical Properties | Back Directory | [density ]
1.340±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);177.75(Max Conc. mM) | [form ]
A solid | [pka]
11.84±0.70(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1]. | [storage]
Store at -20°C | [References]
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[2] 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
[3] 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
[4] 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. DOI:10.1124/dmd.110.032326 |
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