AKI-603

AKI-603 is an inhibitor of Aurora A kinase (IC50 = 12 nM).1 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.2 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.WARNING This product is not for human or veterinary use.

An Aurora A kinase inhibitor

409.5

≥98%

Biochemicals/Kinase Inhibitors/Aurora/Small Molecule Inhibitors/Kinases

Formal_Name:6-(4-methyl-1-piperazinyl)-N4-(5-methyl-1H-pyrazol-3-yl)-N2-(4-nitrophenyl)-2,4-pyrimidinediamine

CN(CC1)CCN1C2=NC(NC(C=C3)=CC=C3[N+]([O-])=O)=NC(NC4=NNC(C)=C4)=C2

C19H23N9O2

1432515-73-5

≥ 4 years

DMSO: Sparingly soluble: 1-10 mg/ml Ethanol: Slightly soluble: 0.1-1 mg/ml