Refametinib

Refametinib is an allosteric, selective inhibitor of MEK1 and MEK2 (IC50s = 19 and 47 nM, respectively). It blocks phosphorylation of ERK1/2 across several human cancer cell lines differing in tissue origin and BRAF mutational status (EC50s = 2.5-16 nM), inhibiting cell cycling in cancer cells but not in primary cells. Refametinib is orally available and active in human tumor xenograft models. It has potential utility, particularly in combination therapy, in certain forms of cancer.Formal Name: N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-cyclopropanesulfonamide. CAS Number: 923032-37-5. Synonyms: BAY 86-9766, RDEA119. Molecular Formula: C19H20F3IN2O5S. Formula Weight: 572.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 1 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS(pH 7.2) (1:5): 0.1 mg/ml. lambdamax: 275, 299 nm. SMILES: FC1=CC(OC)=C(NS(C2(CC2)C[C@H](O)CO)(=O)=O)C(NC3=CC=C(I)C=C3F)=C1F. InChi Code: InChI=1S/C19H20F3IN2O5S/c1-30-15-7-13(21)16(22)18(24-14-3-2-10(23)6-12(14)20)17(15)25-31(28,29)19(4-5-19)8-11(27)9-26/h2-3,6-7,11,24-27H,4-5,8-9H2,1H3/t11-/m0/s1. InChi Key: RDSACQWTXKSHJT-NSHDSACASA-N.