TAK-901

TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively). It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 µM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 µM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 µM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models.Formal Name: 5-[3-(ethylsulfonyl)phenyl]-3,8-dimethyl-N-(1-methyl-4-piperidinyl)-9H-pyrido[2,3-b]indole-7-carboxamide. CAS Number: 934541-31-8. Molecular Formula: C28H32N4O3S. Formula Weight: 504.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml. lambdamax: 215, 309, 354 nm. SMILES: CC1=C(C(NC2CCN(C)CC2)=O)C=C(C3=CC(S(CC)(=O)=O)=CC=C3)C4=C1NC5=C4C=C(C)C=N5. InChi Code: InChI=1S/C28H32N4O3S/c1-5-36(34,35)21-8-6-7-19(14-21)23-15-22(28(33)30-20-9-11-32(4)12-10-20)18(3)26-25(23)24-13-17(2)16-29-27(24)31-26/h6-8,13-16,20H,5,9-12H2,1-4H3,(H,29,31)(H,30,33). InChi Key: WKDACQVEJIVHMZ-UHFFFAOYSA-N.