Selective inhibitor of protein kinase, targeting B-Raf (V600E).GDC-0879 is a highly selective, novel potent, orally bioavailable B-Raf inhibitor in various in vitro and cell-based assays with an IC50 estimate of 0.13 nM against purified B-Raf V600E enzyme and a cellular pERK IC50 of 63 nM in the MALME-3M cell line.For this compound, subnanomolar enzyme potency translated into very effective reduction of cellular viability of BRAF-mutant Malme3M cells (EC50 values were 0.75 umol/L for GDC-0879).In GDC-0879-treated mice, both cell line- and patient-derived BRAFV600E tumors exhibited stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors

2.Hoeflich KP, et al. Cancer Res. 2009, 69(7), 3042-3051.