Tunlametinib

A MEK1 inhibitor, selective for MEK1 over a panel of kinases panel at 10 µM, selectively reduces proliferation in a panel of cancer cell lines expressing mutant K-Ras or B-RAF (IC50s = 0.67-59.89 nM) over H1975 cells expressing wild-type K-Ras and B-Raf (IC50 = >1,000 nM), inhibits ERK phosphorylation in A375 cells (IC50 = 1.16 nM), inhibits intratumoral ERK phosphorylation in an A375 mouse xenograft model at 1, 3, and 9 mg/kg, reduces tumor growth in an A375 mouse xenograft model at 3 and 9 mg/kg. SMILES: O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO. InChi Code: InChI=1S/C16H12F2IN3O3S/c17-10-5-8(19)1-2-11(10)21-14-9(16(24)22-25-4-3-23)6-12-15(13(14)18)20-7-26-12/h1-2,5-7,21,23H,3-4H2,(H,22,24). InChi Key: UFZJUVFSSINETF-UHFFFAOYSA-N