tcsc0158 GDC-0879

GDC-0879 is a potent and selective B-Raf inhibitor with an IC₅₀ of 0.13 nM.

IC50 & Target: IC50: 0.13 nM (B-Raf)^[1]

In Vitro: GDC-0879 also inhibits pERK with an IC₅₀ of 63 nM^[1]. GDC-0879 represents a novel potent and selective B-Raf inhibitor that is being evaluated as a potential antitumor agent. GDC-0879 exhibits potent inhibition of Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines with low cellular pMEK1 inhibition IC₅₀ estimates of 59 and 29 nM in A375 melanoma and Colo205 colorectal carcinoma cells, respectively^[2].

In Vivo: The pharmacokinetic parameters of GDC-0879 after oral administration of 15, 25, 50, 100, and 200 mg/kg in MCT in mice are estimated as follows: k_a=8.20 h^-1, k_e=0.59 h^-1, and apparent volume of distribution=6.19 L/kg^[2].