FCN-159 (Luvometinib) is an orally available and highly potent selective MEK1/2 inhibitor.
FCN-159 (Luvometinib) is 10 times more selective than trametinib, and blocks downstream MAPK signalling.
FCN-159 (Luvometinib) exhibits remarkable potency against the cell proliferation of a panel of human cancer cell lines with RAS/RAF mutations while sparing normal or cancer cell lines expressing wild type RAS/RAF, indicating highly selective inhibition against RAS/RAF/MEK signaling pathway.
FCN-159 (Luvometinib) dose-dependently inhibits the phosphorylation of MEK downstream effector ERK and induced cell cycle arrest as well as cell apoptosis in human colon cancer cells.
FCN-159 (Luvometinib) shows significant and dose-dependent anti-tumor activities in a variety of human tumor xenograft models, derived from colon cancer (HT-29 and Colo205), melanoma (A375), NSCLC (Calu-6) and AML (HL-60).
FCN-159 (Luvometinib) potently inhibits tumor growth in two patient-derived xenograft (PDX) models bearing NRAS mutation.