LY 3009120 New
Chemical Name: N-(3,3-Dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea
Biological ActivityPotent pan-Raf kinase inhibitor (IC50 values are 31 - 47, 42 and 44 nM for b-RAF, c-RAF and a-RAF in A375 cells, respectively). Also inhibits kinase activity of Raf hetero- and homodimers. Displays antiproliferative effects against b-RAF and Ras mutant melanoma cells. Inhibits MEK and ERK phosphorylation, and b-RAF and Ras mutant tumor growth in mouse xenograft models.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry et al.
Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers.
Peng et al.
Cancer Cell., 2015;28:384
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