SB-590885

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi. SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM). It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases. SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations. Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion. SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.Formal Name: 5-[2-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime. CAS Number: 405554-55-4. Molecular Formula: C27H27N5O2. Formula Weight: 453.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 3 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 307 nm. SMILES: CN(C)CCOC1=CC=C(C2=NC(C3=CC=NC=C3)=C(C4=CC=C(/C(CC5)=N/O)C5=C4)N2)C=C1. InChi Code: InChI=1S/C27H27N5O2/c1-32(2)15-16-34-22-7-3-19(4-8-22)27-29-25(18-11-13-28-14-12-18)26(30-27)21-5-9-23-20(17-21)6-10-24(23)31-33/h3-5,7-9,11-14,17,33H,6,10,15-16H2,1-2H3,(H,29,30)/b31-24+. InChi Key: MLSAQOINCGAULQ-QFMPWRQOSA-N.