An Aurora A kinase inhibitor
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AKI-603

Item No. 40840

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $116

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    5 mg

    $521

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    10 mg

    $924

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    25 mg

    $2,022

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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Luo, Y., Deng, Y.-Q., Wang, J., et al. Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors. Eur. J. Med. Chem. 78, 65-71 (2014).

    2. Zheng, F.-M., Long, Z.-J., Hou, Z.-J.L., Y., et al. A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance. Mol. Cancer Ther. 13(8), 1991-2003 (2014).