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MPI-0479605 MPS1 inhibitor

Cat.No.S7488

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 MPS1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 407.51

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Quality Control

Batch: S748801 DMSO]62 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.62%
99.62

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (152.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 407.51 Formula

C22H29N7O

 Storage (From the date of receipt)
CAS No. 1246529-32-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=CC(=C1)N2CCOCC2)NC3=NC4=C(C(=N3)NC5CCCCC5)NC=N4

Mechanism of Action

Targets/IC50/Ki
Mps1
1.8 nM
In vitro
MPI-0479605 impairs the SAC and the bipolar attachment of chromosomes to the mitotic spindle, which results in chromosome segregation defects and aneuploidy. This compound 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, it also causes cell growth arrest and ultimately promotes cell death by apoptosis or mitotic catastrophe.
Kinase Assay
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. This compound (500 nM) is also screened against a larger kinase panel.
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.
References

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