Molecular Weight(MW): 407.51
MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.
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|Description||MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.|
MPI-0479605 impairs the SAC and the bipolar attachment of chromosomes to the mitotic spindle, which results in chromosome segregation defects and aneuploidy. MPI-0479605 results in a significant decrease in cell viability with GI50 ranging from 30 to 100 nM in a panel of tumor cell lines. In addition, MPI-0479605 also causes cell growth arrest and ultimately promotes cell death by apoptosis or mitotic catastrophe. 
|In vivo||MPI-0479605 (30 mg/kg daily or 150 mg/kg every 4 days, i.p.) shows antitumor activity in colon cancer xenograft models. |
In Vitro Kinase Assays and Selectivity Screening :To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel.
|In vitro||DMSO||62 mg/mL warmed (152.14 mM)|
|Ethanol||2 mg/mL warmed (4.9 mM)|
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