GDC-0879

DESCRIPTION

An inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme); selective for B-RafV600E over a panel of 140 kinases at 1 μM; 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); inhibits tumor growth in an A375 mouse xenograft model from 15-200 mg/kg

DETAILS

Inchi: 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+
Purity: ≥95%
Raptas: Product Type|Biochemicals|Kinase Inhibitors|RAF||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling
Smiles: OCCN1N=C(C2=CC=NC=C2)C(C3=CC=C(/C(CC4)=N/O)C4=C3)=C1
Inchikey: DEZZLWQELQORIU-RELWKKBWSA-N
Cas Number: 905281-76-7
Formulation: A crystalline solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C19H18N4O2
Formula Weight: 334.4
Shelf Life Days: 1460