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MPI-0479605

Chemical Structure : MPI-0479605

CAS No.: 1246529-32-7

MPI-0479605 (MPI0479605)

Catalog No.: PC-43142Not For Human Use, Lab Use Only.

MPI-0479605 is a potent, selective, ATP competitive inhibitor of Mps1 with IC50 of 1.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MPI-0479605 is a potent, selective, ATP competitive inhibitor of Mps1 with IC50 of 1.8 nM.
MPI-0479605 triggers the time-dependent degradation of both cyclin B and securin, decreases BubR1 phosphorylation in nocodazole-arrested cells, blocks apparent autophosphorylation of Mps1 at threonine 676 in HEK293T cells.
MPI-0479605 impairs spindle assembly checkpoint (SAC), resulting in chromosome segregation defects and aneuploidy, induces p53-p21 pathway in an ATM- and ATR-dependent manner.
MPI-0479605 exhibits cytotoxicity across a broad range of tumor cell lines and antitumor activity in human tumor xenografts.

Physicochemical Properties

M.Wt 407.512
Formula C22H29N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 11 mg/mL

Chemical Name/SMILES

9H-Purine-2,6-diamine, N6-cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-

References

1. Tardif KD, et al. Mol Cancer Ther. 2011 Dec;10(12):2267-75.

2. Vijay Kumar D, et al. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4377-85.

3. Uitdehaag JCM, et al. J Mol Biol. 2017 Jul 7;429(14):2211-2230.

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