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Potent 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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||4.25||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 424.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||23.56 mL||117.78 mL||235.56 mL|
|0.5 mM||4.71 mL||23.56 mL||47.11 mL|
|1 mM||2.36 mL||11.78 mL||23.56 mL|
|5 mM||0.47 mL||2.36 mL||4.71 mL|
References are publications that support the biological activity of the product.
Henry et al (2015) 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. J.Med.Chem. 58 4165 PMID: 25965804
Peng et al (2015) Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers. Cancer Cell. 28 384 PMID: 26343583
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