MPI-0479605

MPI-0479605 is an inhibitor of monopolar spindle 1 (Mps1. IC50 = 1. nM). 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 (Cay-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. 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: DMSO: Sparingly soluble: 1-10mg/ml Methanol: Slightly soluble: 0.1-1mg/ml Water: 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. Storage: -20°C. Stability: > 4 years.