An Mps1 inhibitor
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MPI-0479605

Item No. 44704

Product Insert (PDF)
Technical Information
Formal Name
N6-cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine
CAS Number
1246529-32-7
Molecular Formula
C22H29N7O
Formula Weight
407.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10mg/mlMethanol: Slightly soluble: 0.1-1mg/mlWater: Slightly soluble: 0.1-1mg/ml
SMILES
CC1=C(NC2=NC(NC3CCCCC3)=C(NC=N4)C4=N2)C=CC(N5CCOCC5)=C1
InChi Code
InChI=1S/C22H29N7O/c1-15-13-17(29-9-11-30-12-10-29)7-8-18(15)26-22-27-20-19(23-14-24-20)21(28-22)25-16-5-3-2-4-6-16/h7-8,13-14,16H,2-6,9-12H2,1H3,(H3,23,24,25,26,27,28)
InChi Key
OVJBNYKNHXJGSA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    MPI-0479605 is an inhibitor of monopolar spindle 1 (Mps1; IC50 = 1.8 nM).1 It is selective for Mps1 over a panel of 79 kinases at 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of mitotic arrest deficient 3 (Mad3), resulting in failed cytokinesis in HeLa cervical cancer cells arrested by nocodazole (Item No. 13857). It induces cell cycle arrest at the G2/M phase in HCT116 colon cancer cells, which express p53wt, and COLO 205 colon cancer cells, which express p53mut, when used at a concentration of 1 µM. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tardif, K.D., Rogers, A., Cassiano, J., et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol. Cancer Ther. 10(12), 2267-2275 (2011).