GDC-0879

GDC-0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme). It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 µM. GDC-0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that express B-RafV600E (IC50s = 29 and 59 nM, respectively). In vivo, GDC-0879 (15-200 mg/kg) inhibits tumor growth in a dose-dependent manner in an A375 mouse xenograft model.Formal Name: 2,3-dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one, oxime. CAS Number: 905281-76-7. Molecular Formula: C19H18N4O2. Formula Weight: 334.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: slightly, DMSO: slightly, Ethanol: slightly. lambdamax: 267, 298 nm. SMILES: OCCN1N=C(C2=CC=NC=C2)C(C3=CC=C(/C(CC4)=N/O)C4=C3)=C1. InChi Code: InChI=1S/C19H18N4O2/c24-10-9-23-12-17(19(21-23)13-5-7-20-8-6-13)15-1-3-16-14(11-15)2-4-18(16)22-25/h1,3,5-8,11-12,24-25H,2,4,9-10H2/b22-18+. InChi Key: DEZZLWQELQORIU-RELWKKBWSA-N.