RO4987655

RO4987655 is a MEK inhibitor (IC50 = 5 nM). It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Cay-11597) to reduce tumor volume in an HCT116 mouse xenograft model.Formal Name: 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(tetrahydro-3-oxo-2H-1,2-oxazin-2-yl)methyl]-benzamide. CAS Number: 874101-00-5. Synonyms: CH4987655. Molecular Formula: C20H19F3IN3O5. Formula Weight: 565.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml, DMSO: 10 mg/ml. lambdamax: 280 nm. SMILES: O=C1CCCON1CC2=C(F)C(F)=C(NC3=CC=C(I)C=C3F)C(C(NOCCO)=O)=C2. InChi Code: InChI=1S/C20H19F3IN3O5/c21-14-9-12(24)3-4-15(14)25-19-13(20(30)26-31-7-5-28)8-11(17(22)18(19)23)10-27-16(29)2-1-6-32-27/h3-4,8-9,25,28H,1-2,5-7,10H2,(H,26,30). InChi Key: FIMYFEGKMOCQKT-UHFFFAOYSA-N.