LY 3009120

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Cat.No. 6854 - LY 3009120 | C23H29FN6O | CAS No. 1454682-72-4
Description: Potent pan-Raf kinase inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 424.52
Formula C23H29FN6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1454682-72-4
PubChem ID 71721540
InChI Key HHCBMISMPSAZBF-UHFFFAOYSA-N
Smiles CNC1=NC2=C(C=N1)C=C(C(C)=N2)C1=CC(NC(=O)NCCC(C)(C)C)=C(F)C=C1C

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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

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References

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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