Formulation: A solid
Formal Name: 6-(4-methyl-1-piperazinyl)-N4-(5-methyl-1H-pyrazol-3-yl)-N2-(4-nitrophenyl)-2,4-pyrimidinediamine
Purity: ≥98%
Formula Markup: C19H23N9O2
Formula Weight: 409,5
Shelf life (days): 1460
CAS Number: 1432515-73-5
Notes: AKI-603 is an inhibitor of Aurora A kinase (IC50 = 12 nM).{69762} 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.{69763} It decreases the endogenous elevated levels of β-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.
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