MK-8745
Based on 4 publication(s) in Google Scholar
MK-8745 is an aurora A kinase inhibitor with an IC50 of 0.6 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.08%
- No. CAS: 885325-71-3
- Fòrmula: C20H19ClFN5OS
- Peso molecular:431.91
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) MK-8745
MoreVer todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 0.6 nM (IC50) |
MK-8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK-8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression[1]. 1 μM of MK-8745 exposure for 24 h induces cell cycle arrest in all NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly sensitive to MK-8745 (1 μ M) treatment and induces an approximate 5.5-fold increase in the G2/M phase cell population by 96 h. MK-8745 treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has no effect. MK-8745 specifically inhibits Aurora-A specific function. MK-8745 treatment leads to apoptotic cell death[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 885325-71-3
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Appearance Solid
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Peso molecular 431.91
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Fòrmula C20H19ClFN5OS
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Color White to yellow
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SMILES
O=C(C1=CC=CC(Cl)=C1F)N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Cell Sci
Repair-independent functions of DNA-PKcs protect irradiated cells from mitotic slippage and accelerated senescence. [Abstract]2019 Jul 1;132(13):jcs229385. PMID: 31189537 -
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Elife
2020 Dec 7:9:e61405. PMID: 33284104
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (231.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
A total of 10000 cells are plated per well in a 96-well plate and treated with MK-8745 for varying time points starting 24 h after plating. Cell viability is measured by the MTT assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. [Content Brief]
[2]. Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012 Mar, 53(3):462-71. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3153 mL | 11.5765 mL | 23.1530 mL | 57.8824 mL |
| 5 mM | 0.4631 mL | 2.3153 mL | 4.6306 mL | 11.5765 mL | |
| 10 mM | 0.2315 mL | 1.1576 mL | 2.3153 mL | 5.7882 mL | |
| 15 mM | 0.1544 mL | 0.7718 mL | 1.5435 mL | 3.8588 mL | |
| 20 mM | 0.1158 mL | 0.5788 mL | 1.1576 mL | 2.8941 mL | |
| 25 mM | 0.0926 mL | 0.4631 mL | 0.9261 mL | 2.3153 mL | |
| 30 mM | 0.0772 mL | 0.3859 mL | 0.7718 mL | 1.9294 mL | |
| 40 mM | 0.0579 mL | 0.2894 mL | 0.5788 mL | 1.4471 mL | |
| 50 mM | 0.0463 mL | 0.2315 mL | 0.4631 mL | 1.1576 mL | |
| 60 mM | 0.0386 mL | 0.1929 mL | 0.3859 mL | 0.9647 mL | |
| 80 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7235 mL | |
| 100 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL |
MK-8745 Related Classifications
HY-13819 Related Classifications
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