LY3009120

LY3009120 is an inhibitor of Raf kinases, including A-Raf, B-Raf, and c-Raf (IC50s = 44, 31-47, and 42 nM, respectively, in whole cell lysates). It also inhibits B-Raf mutants V600E and V600E+G468A (IC50s = 5.8 and 17 nM, respectively, in biochemical assays). LY3009120 induces Raf dimerization and, unlike vemurafenib (PLX4032, Cay-10618) and dabrafenib (Cay-16989), inhibits kinase activity of induced dimers. It inhibits cell cycling in B-Raf or Ras mutant cancer cells and has significant antitumor activity in B-Raf and K-Ras mutant preclinical models of colorectal cancer. LY3009120 is also active against B-Raf in-frame deletions in vitro and in mouse models.Formal Name: N-(3,3-dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-urea. CAS Number: 1454682-72-4. Synonyms: DP-4978. Molecular Formula: C23H29FN6O. Formula Weight: 424.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO:. lambdamax: 240, 276, 366 nm. SMILES: CC1=CC(F)=C(NC(NCCC(C)(C)C)=O)C=C1C2=C(C)N=C(N=C(NC)N=C3)C3=C2. InChi Code: InChI=1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30). InChi Key: HHCBMISMPSAZBF-UHFFFAOYSA-N.