Mps1-IN-1
Based on 5 publication(s) in Google Scholar
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.77%
- CAS No.: 1125593-20-5
- 화학식: C28H33N5O4S
- 분자량:535.66
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Mps1-IN-1
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Biological Activity
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Mps1 367 nM (IC50) |
Mps1 27 nM (Kd) |
ALK 21 nM (Kd) |
LTK 29 nM (Kd) |
PYK2 280 nM (Kd) |
FAK 440 nM (Kd) |
IGF1R 750 nM (Kd) |
INSR 470 nM (Kd) |
CLK1 1900 nM (Kd) |
ERK2 2900 nM (Kd) |
INSRR 1200 nM (Kd) |
TNK1 2600 nM (Kd) |
TNK2 3100 nM (Kd) |
GAK 1100 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AU565 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| BT-20 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| BT-474 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| BT-549 | IC50 |
1.73 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| CAL-51 | IC50 |
2.92 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| CAMA-1 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| HCC1937 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| Hs-578T | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| MCF7 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| MDA-MB-436 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| MDA-MB-453 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| MDA-MB-468 | IC50 |
1.85 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| SK-BR-3 | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
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[PMID: 28259529] |
| T47D | IC50 |
>10 μM
Compound: Mps1-IN-1
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Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay
|
[PMID: 28259529] |
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with Kds of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 μM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 μM) suppresses the proliferative capacity of HCT116[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1125593-20-5
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Appearance Solid
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분자량 535.66
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화학식 C28H33N5O4S
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Color Light yellow to yellow
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SMILES
O=S(C(C=CC=C1)=C1NC2=CC(NC3=C(OC)C=C(N4CCC(O)CC4)C=C3)=NC5=C2C=CN5)(C(C)C)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Cancer
Proline-rich acidic protein 1 upregulates mitotic arrest deficient 1 to promote cisplatin-resistance of colorectal carcinoma by restraining mitotic checkpoint complex assembly. [Abstract]2023 May 21;14(9):1515-1530. PMID: 37325046 -
Mol Reprod Dev
Phospholipase D2 Regulates Microtubule Acetylation by Modulating Gsk3β-Tau Signaling in Mouse Oocytes During Meiotic Maturation. [Abstract]2025 Aug;92(8):e70051. PMID: 40838360 -
J Cell Biochem
Mps1 controls spindle assembly, SAC, and DNA repair in the first cleavage of mouse early embryos. [Abstract]2021 Feb;122(2):290-300. PMID: 33025669 -
용액&용해도
DMSO : ≥ 39 mg/mL (72.81 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 (4.67 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.
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
The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-1), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block is performed using the following treatment regimen: thymidine for 18-20 hrs., release for 10 hrs. with doxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hours after the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cell populations is monitored with Cell Titer GLO assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (280 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, 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 | 1.8669 mL | 9.3343 mL | 18.6686 mL | 46.6714 mL |
| 5 mM | 0.3734 mL | 1.8669 mL | 3.7337 mL | 9.3343 mL | |
| 10 mM | 0.1867 mL | 0.9334 mL | 1.8669 mL | 4.6671 mL | |
| 15 mM | 0.1245 mL | 0.6223 mL | 1.2446 mL | 3.1114 mL | |
| 20 mM | 0.0933 mL | 0.4667 mL | 0.9334 mL | 2.3336 mL | |
| 25 mM | 0.0747 mL | 0.3734 mL | 0.7467 mL | 1.8669 mL | |
| 30 mM | 0.0622 mL | 0.3111 mL | 0.6223 mL | 1.5557 mL | |
| 40 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1668 mL | |
| 50 mM | 0.0373 mL | 0.1867 mL | 0.3734 mL | 0.9334 mL | |
| 60 mM | 0.0311 mL | 0.1556 mL | 0.3111 mL | 0.7779 mL |
Mps1-IN-1 Related Classifications
HY-13298 Related Classifications
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