产品描述:
Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}