MPI-0479605

製品コードS7488 バッチS748801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H29N7O
分子量 407.51 CAS No. 1246529-32-7
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 62 mg/mL (152.14 mM)
Ethanol (warmed with 50ºC water bath) 2 mg/mL (4.9 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
5% DMSO 95% Corn oil
3.1mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
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. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 A549, Colo205, DU-4475, DU-145, HCC827, HCT116, HT29, MDA MB 231, MiaPaCa2, NCI-H69, NCI-H460, NCI-N87, OPM2, and OVCAR-3 cells.
濃度 ~10 μM
反応時間 3 or 7 days
実験の流れ

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.
動物実験 動物モデル Mice bearing subcutaneous HCT-116 or Colo-205 human tumor cell xenografts.
投薬量 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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