GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
体外研究
GDC-0879 also inhibits pERK with an IC50 of 63 nM. 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.
体内研究
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: ka=8.20 h, ke=0.59 h, and apparent volume of distribution=6.19 L/kg.
分子式
C19H18N4O2
分子量
334.37
CAS号
905281-76-7
运输条件
Room temperature in continental US; may vary elsewhere.