WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406382
Description: MPI-0479605 is a potent and selective ATP competitive inhibitor of Mps1. Cells treated with MPI-0479605 undergo aberrant mitosis, resulting in aneuploidy and formation of micronuclei. In cells with wild-type p53, this promotes the induction of a postmitotic checkpoint characterized by the ATM- and RAD3-related-dependent activation of the p53-p21 pathway. In both wild-type and p53 mutant cells lines, there is a growth arrest and inhibition of DNA synthesis. Subsequently, cells undergo mitotic catastrophe and/or an apoptotic response. In xenograft models, MPI-0479605 inhibits tumor growth, suggesting that drugs targeting Mps1 may have utility as novel cancer therapeutics.
MedKoo Cat#: 406382
Chemical Formula: C22H29N7O
Exact Mass: 407.24336
Molecular Weight: 407.51
Elemental Analysis: C, 64.84; H, 7.17; N, 24.06; O, 3.93
Synonym: MPI0479605; MPI 0479605; MPI-0479605.
IUPAC/Chemical Name: N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine
SMILES Code: CC1=CC(N2CCOCC2)=CC=C1NC3=NC(NC4CCCCC4)=C5N=CNC5=N3
1: Vijay Kumar D, Hoarau C, Bursavich M, Slattum P, Gerrish D, Yager K, Saunders M, Shenderovich M, Roth BL, McKinnon R, Chan A, Cimbora DM, Bradford C, Reeves L, Patton S, Papac DI, Williams BL, Carlson RO. Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4377-85. doi: 10.1016/j.bmcl.2012.04.131. Epub 2012 May 5. PubMed PMID: 22632936.
2: Tardif KD, Rogers A, Cassiano J, Roth BL, Cimbora DM, McKinnon R, Peterson A, Douce TB, Robinson R, Dorweiler I, Davis T, Hess MA, Ostanin K, Papac DI, Baichwal V, McAlexander I, Willardsen JA, Saunders M, Christophe H, Kumar DV, Wettstein DA, Carlson RO, Williams BL. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-75. doi: 10.1158/1535-7163.MCT-11-0453. Epub 2011 Oct 6. PubMed PMID: 21980130.