MPI-0479605

Name: MPI-0479605
Brand: Selleck Chemicals
SKU: S7488
Rating: 5 (4 reviews)

For research use only.

Catalog No.S7488

4 publications

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.

Selleck's MPI-0479605 has been cited by 4 publications

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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

Kinase Assay: ^[1]	- Collapse 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 Research: ^[1]	- Collapse 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. (Only for Reference)
Animal Research: ^[1]	- Collapse 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. (Only for Reference)

References

[1] Tardif KD, et al. Mol Cancer Ther. 2011, 10(12), 2267-2275.

Solubility (25°C)

In vitro	DMSO	62 mg/mL warmed (152.14 mM)
	Ethanol	2 mg/mL warmed (4.9 mM)
	Water	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.

Chemical Information Download MPI-0479605 SDF

Molecular Weight	407.51
Formula	C₂₂H₂₉N₇O
CAS No.	1246529-32-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CC1=CC(=CC=C1NC2=NC3=C(N=C[NH]3)C(=N2)NC4CCCCC4)N5CCOCC5

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Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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MPI-0479605