受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
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) |
|
||||||||||||||
* <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. |
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] |
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. |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。