| Identification | Back Directory | [Name]
BenzaMide, 3-(1-aMino-1-Methylethyl)-N-[(2R)-1,2,3,4-tetrahydro-7-[(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-4-yl)oxy]-2-naphthalenyl]-5-(trifluoroMethyl)- | [CAS]
1237586-97-8 | [Synonyms]
3-(2-aminopropan-2-yl)-N-[(2R)-7-[(7-oxo-6,8-dihydro-5H-1,8-naphthyridin-4-yl)oxy]-1,2,3,4-tetrahydronaphthalen-2-yl]-5-(trifluoromethyl)benzamide
BenzaMide, 3-(1-aMino-1-Methylethyl)-N-[(2R)-1,2,3,4-tetrahydro-7-[(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-4-yl)oxy]-2-naphthalenyl]-5-(trifluoroMethyl)- | [Molecular Formula]
C29H29F3N4O3 | [MDL Number]
MFCD19443164 | [MOL File]
1237586-97-8.mol | [Molecular Weight]
538.56 |
| Hazard Information | Back Directory | [Description]
BGB659 is a potent BRAF inhibitor. | [Uses]
ML786 is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers[1]. | [in vivo]
ML786 (75 mg/kg; p.o. once daily for 21 d) inhibits the subcutaneous A375 M xenografts in immunocompromised mice[1].
ML786 (75 mg/kg; a single p.o.) strongly inhibits the Raf pathway in mice[1].
ML786 (10 mg/kg; p.o.) exhibits oral bioavailability of 85% and AUC1-24h of 35.9 μM·h in rats[1].
ML786 (1 mg/kg; i.v.) exhibits plasma clearance of 0.44 L/h/kg and Vss of 3.93 L/kg in rats[1]. | [References]
[1] Gould AE, et, al. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem. 2011 Mar 24;54(6):1836-46. DOI:10.1021/jm101479y |
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