AKI-603

AKI-603 is an inhibitor of Aurora A kinase (IC50 = 12 nM). It reduces the proliferation of HL-60 promyeoloblast leukemia cells, K562 chronic myeloid leukemia (CML) cells, U937 lymphoma monocytes, MOLT-4 T cell lymphoblasts, and MCF-7 and MDA-MD-231 breast cancer cells (IC50s = 69, 137, 43, 18, 424, and 84 nM, respectively). AKI-603 (600 nM) induces cell cycle arrest at the G2/M phase in SUM149 triple negative breast cancer cells. It decreases the endogenous elevated levels of beta-catenin, c-Myc, SOX2, Nanog, and octamer-binding transcription factor 4 (Oct4) in epirubicin-resistant MCF-7 breast cancer cells (MCF-7/Epi) when used at a concentration of 5 µM. AKI-603 (78 nM) reduces the number of mammospheres formed by SUM149 cells. In vivo, AKI-603 (50 mg/kg per day) decreases tumor volume and weight without reducing body weight in an MCF-7/Epi mouse xenograft model.Formal Name: 6-(4-methyl-1-piperazinyl)-N4-(5-methyl-1H-pyrazol-3-yl)-N2-(4-nitrophenyl)-2,4-pyrimidinediamine. CAS Number: 1432515-73-5. Molecular Formula: C19H23N9O2. Formula Weight: 409.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: CN(CC1)CCN1C2=NC(NC(C=C3)=CC=C3[N+]([O-])=O)=NC(NC4=NNC(C)=C4)=C2. InChi Code: InChI=1S/C19H23N9O2/c1-13-11-17(25-24-13)21-16-12-18(27-9-7-26(2)8-10-27)23-19(22-16)20-14-3-5-15(6-4-14)28(29)30/h3-6,11-12H,7-10H2,1-2H3,(H3,20,21,22,23,24,25). InChi Key: UNKOUVAYOLLXER-UHFFFAOYSA-N.