BI-847325

BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively. It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim. At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.Formal Name: 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide. CAS Number: 1207293-36-4. Molecular Formula: C29H28N4O2. Formula Weight: 464.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml, DMSO: 5 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 298, 398 nm. SMILES: O=C(NCC)C#CC1=CC2=C(/C(C(N2)=O)=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4)C=C1. InChi Code: InChI=1S/C29H28N4O2/c1-4-30-26(34)17-13-20-12-16-24-25(18-20)32-29(35)27(24)28(22-8-6-5-7-9-22)31-23-14-10-21(11-15-23)19-33(2)3/h5-12,14-16,18,31H,4,19H2,1-3H3,(H,30,34)(H,32,35)/b28-27+. InChi Key: FLBNLJLONKAPLR-BYYHNAKLSA-N.