Binimetinib

Binimetinib is a MEK1 and MEK2 inhibitor (IC50s = 1.8 and 0.92 nM, respectively). It is selective for MEK1/2 over a panel of RAF/MEK/ERK pathway kinases at 10 µM. Binimetinib reduces cell growth in HT-29, COLO 205, and LoVo colorectal cancer cell lines (IC50s = 0.48, 0.52, and 2.2 nM, respectively). It reduces tumor volume in a COLO 205 mouse xenograft model when administered at a dose of 0.3 mg/kg. Formulations containing binimetinib have been used in the treatment of various cancers.Formal Name: 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide. CAS Number: 606143-89-9. Synonyms: ARRY-438162, MEK162. Molecular Formula: C17H15BrF2N4O3. Formula Weight: 441.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 213, 257 nm. SMILES: BrC1=CC(F)=C(NC2=C(F)C(N=CN3C)=C3C=C2C(NOCCO)=O)C=C1. InChi Code: InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26). InChi Key: ACWZRVQXLIRSDF-UHFFFAOYSA-N.