MPI-0479605

Catalog No.S7488 Batch:S748801

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Technical Data

Formula

C22H29N7O
Molecular Weight 407.51 CAS No. 1246529-32-7
Solubility (25°C)* In vitro DMSO 62 mg/mL (152.14 mM)
Ethanol 2 mg/mL (4.9 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
3.1mg/ml
Clear solution
10%DMSO 30%PEG300 5%Tween80 55%ddH2O
6.0mg/ml Taking the 1 mL working solution as an example, add 100 μL of 60 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 550 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.1mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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.
Targets
Mps1 [1]
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. 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. [1]
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. [1]

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[1]
  • Cell lines

    A549, Colo205, DU-4475, DU-145, HCC827, HCT116, HT29, MDA MB 231, MiaPaCa2, NCI-H69, NCI-H460, NCI-N87, OPM2, and OVCAR-3 cells.

  • Concentrations

    ~10 μM

  • Incubation Time

    3 or 7 days

  • Method

    Cells are treated for 3 or 7 days with various concentrations of MPI-0479605 and the GI50 is determined. Cell viability is measured with CellTiter-Glo.
Animal Study:

[1]
  • Animal Models

    Mice bearing subcutaneous HCT-116 or Colo-205 human tumor cell xenografts.

  • Dosages

    5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300

  • Administration

    i.p.

Selleck's MPI-0479605 has been cited by 7 publications

Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151] PubMed: 35355016
TTK is a potential therapeutic target for cisplatin-resistant ovarian cancer [ J Ovarian Res, 2021, 14(1):128] PubMed: 34598710
A New Quantitative Cell-Based Assay Reveals Unexpected Microtubule Stabilizing Activity of Certain Kinase Inhibitors, Clinically Approved or in the Process of Approval [ Front Pharmacol, 2020, 30;11:543] PubMed: 32425788
Centromere Dysfunction Compromises Mitotic Spindle Pole Integrity [ Curr Biol, 2019, 29(18):3072-3080.e5] PubMed: 31495582
Centromere Dysfunction Compromises Mitotic Spindle Pole Integrity. [ Curr Biol, 2019, 29(18):3072-3080] PubMed: 31495582
Differences in Mitotic Spindle Architecture in Mammalian Neural Stem Cells Influence Mitotic Accuracy during Brain Development. [ Curr Biol, 2019, 29(18):2993-3005] PubMed: 31495584
Novel Allosteric Pathway of Eg5 Regulation Identified through Multivariate Statistical Analysis of Hydrogen-Exchange Mass Spectrometry (HX-MS) Ligand Screening Data [Sheff JG Mol Cell Proteomics, 2017, 16(3):428-437] PubMed: 28062800

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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