Identification | Back Directory | [Name]
Benzamide, N-[3-(7-amino-1,4-dihydro-1-methyl-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl)-4-methylphenyl]-3-(trifluoromethyl)- | [CAS]
839708-29-1 | [Synonyms]
GNF-6 Benzamide, N-[3-(7-amino-1,4-dihydro-1-methyl-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl)-4-methylphenyl]-3-(trifluoromethyl)- | [Molecular Formula]
C22H19F3N6O2 | [MOL File]
839708-29-1.mol | [Molecular Weight]
456.42 |
Hazard Information | Back Directory | [Uses]
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation[1]. | [References]
[1] David F. Woodward, et al. Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents. WO1994006433A1. DOI:10.1038/nsmb.1486 |
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