A potent inhibitor of MPS1 (IC50 = 1.8 nM); selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM; induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole; causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity; reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner

MPI-0479605 – 1 mg

Brand:
Cayman
CAS:
1246529-32-7
Storage:
-20
UN-No:
Non-Hazardous - /

MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM).{38558} It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole (Item No. 13857). It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.  

 

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Description

A potent inhibitor of MPS1 (IC50 = 1.8 nM); selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM; induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole; causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity; reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner,

Formal name: N6-cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine

Synonyms: 

Molecular weight: 407.5

CAS: 1246529-32-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling

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