Mps1-IN-3
Based on 1 publication(s) in Google Scholar
Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 1609584-72-6
- Formula: C26H31N7O4S
- Molecular Weight:537.63
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) Mps1-IN-3
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Biological Activity
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Mps1 50 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
2415 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human DLD-1 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human DLD-1 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| DLD-1 | IC50 |
7931 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human DLD-1 cells harboring Mps1 S611R mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human DLD-1 cells harboring Mps1 S611R mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HCT-116 | IC50 |
1624 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HCT-116 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HCT-116 cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HCT-116 | IC50 |
3234 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HCT-116 cells harboring Mps1 I531M mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HCT-116 cells harboring Mps1 I531M mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HCT-116 | IC50 |
5403 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HCT-116 cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HCT-116 cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HeLa | IC50 |
3417 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HeLa cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HeLa cells assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HeLa | IC50 |
4793 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HeLa cells harboring Mps1 I598F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HeLa cells harboring Mps1 I598F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HeLa | IC50 |
6793 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HeLa cells harboring Mps1 C604F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HeLa cells harboring Mps1 C604F mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
| HeLa | IC50 |
8974 nM
Compound: Chemical probe: Mps1-IN-3
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Inhibition of colony formation in human HeLa cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
Inhibition of colony formation in human HeLa cells harboring Mps1 C604Y mutant assessed as cell survival incubated for 5 days by crystal violet staining based colony formation assay
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[PMID: 26364596] |
Mps1-IN-3 is a potent MPS1 kinase inhibitor, with an IC50 of 50 nM. Mps1-IN-3 inhibits the proliferation of U251 glioblastoma cells with an IC50 of appr 5 µM. Mps1-IN-3 (2 μM) can completely abrogates checkpoint[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1609584-72-6
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Appearance Solid
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Molecular Weight 537.63
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Formula C26H31N7O4S
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Color White to light brown
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SMILES
OC1CCN(C2=CC=C(NC3=NC(NC4=CC=CC=C4S(=O)(C(C)C)=O)=C5N=CNC5=N3)C(OC)=C2)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Metab
2021 Jun 1;33(6):1111-1123.e4. PMID: 33811821
Solvent & Solubility
DMSO : 100 mg/mL (186.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (4.65 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 (4.65 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol
Mice[1]
Six-week old athymic female nude mice weighing about 25 g are stereotactically injected with 1 × 106 U251-FM-shCTRL or shMPS1 cells, or U251-FM, or 3 × 105 GBM8-FM cells (in 10 and 4 μL PBS, respectively) using a stereotactic instrument after drilling a small hole in the cranium of the mice. For the U251-FM-shRNA experiment, a minimum of 3 mice per group is used, and for the U251-FM and GBM8-FM cells, at least 5 mice per group are used. Tumor growth is monitored by Fluc bioluminescence imaging after injection of 150 μL D-luciferin (50 mg/mL) and imaging 10 min later for luciferase-mediated photon activity using the IVIS Lumina imaging system for the U251-FM model and the IVIS Spectrum for the GBM8-FM model. When tumors reach a size around 107 radiance for the U251 model and 5 × 105 radiance for the GBM8 model, mice are intravenously injected with vehicle, and/or 2 mg/kg MPS1-IN-3 in 20% hydroxypropyl-beta-cyclodextrin (HPbetaCD), twice/week over three weeks. Tumor volume is monitored weekly by Fluc imaging[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 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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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8600 mL | 9.3001 mL | 18.6002 mL | 46.5004 mL |
| 5 mM | 0.3720 mL | 1.8600 mL | 3.7200 mL | 9.3001 mL | |
| 10 mM | 0.1860 mL | 0.9300 mL | 1.8600 mL | 4.6500 mL | |
| 15 mM | 0.1240 mL | 0.6200 mL | 1.2400 mL | 3.1000 mL | |
| 20 mM | 0.0930 mL | 0.4650 mL | 0.9300 mL | 2.3250 mL | |
| 25 mM | 0.0744 mL | 0.3720 mL | 0.7440 mL | 1.8600 mL | |
| 30 mM | 0.0620 mL | 0.3100 mL | 0.6200 mL | 1.5500 mL | |
| 40 mM | 0.0465 mL | 0.2325 mL | 0.4650 mL | 1.1625 mL | |
| 50 mM | 0.0372 mL | 0.1860 mL | 0.3720 mL | 0.9300 mL | |
| 60 mM | 0.0310 mL | 0.1550 mL | 0.3100 mL | 0.7750 mL | |
| 80 mM | 0.0233 mL | 0.1163 mL | 0.2325 mL | 0.5813 mL | |
| 100 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4650 mL |
Mps1-IN-3 Related Classifications
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