BAY-3827

BAY-3827 is an inhibitor of AMP-activated protein kinase (AMPK, IC50 = 1.4 nM at 10 µM ATP). It is selective for AMPK over Aurora A kinase, FMS-related tyrosine kinase 3 (FLT3), and c-Met (IC50s = 1,324, 124, and 788 nM, respectively), p90 ribosomal S6 kinase 2 (RSK2), RSK3, RSK4, p90 ribosomal S6 kinase 1 (MSK1), and MST3 (IC50s = 52, 36, 24, 43, and 94 nM, respectively), and a panel of 331 kinases at 10 µM but does inhibit RSK1 (IC50 = 9 nM). BAY-3827 selectively inhibits the proliferation of androgen-dependent LNCaP, VCaP, and 22Rv1 prostate cancer cells (IC50s = 0.28, 1.71, and 5.55 µM, respectively) over androgen receptor-negative C4-2B, PC3, and DU145 prostate cancer cells (IC50s = >10 µM for all).Formal Name: N-[5-(3,5-dicyano-1,4-dihydro-1,2,6-trimethyl-4-pyridinyl)-6-fluoro-7-methyl-1H-indazol-3-yl]-2-ethyl-benzamide. CAS Number: 2377576-35-5. Molecular Formula: C27H25FN6O. Formula Weight: 468.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: N#CC1=C(C)N(C)C(C)=C(C1C2=CC3=C(C(C)=C2F)NN=C3NC(C4=C(C=CC=C4)CC)=O)C#N. InChi Code: InChI=1S/C27H25FN6O/c1-6-17-9-7-8-10-18(17)27(35)31-26-20-11-19(24(28)14(2)25(20)32-33-26)23-21(12-29)15(3)34(5)16(4)22(23)13-30/h7-11,23H,6H2,1-5H3,(H2,31,32,33,35). InChi Key: OZFFKOSQNBBYCA-UHFFFAOYSA-N.