TC-Mps1-12
Based on 1 Customer Validation
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 1206170-62-8
- Formula: C17H20N6O
- Molecular Weight:324.38
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Storage:Powder -20°C, 3 years , 4°C, 2 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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 6.4 nM (Mps1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.84 μM
Compound: 12
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Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
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[PMID: 24900510] |
| A549 | IC50 |
840 nM
Compound: 14; TC Mps1 12
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Antiproliferative activity against human A549 cells by MTT assay
Antiproliferative activity against human A549 cells by MTT assay
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[PMID: 31121430] |
| HCT-116 | GI50 |
1.6 μM
Compound: 6
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Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
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[PMID: 24256217] |
| HCT-116 | IC50 |
0.56 μM
Compound: 6
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Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
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[PMID: 24256217] |
| RERF-LC-AI | IC50 |
131 nM
Compound: 12
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Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
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[PMID: 24900510] |
| Sf9 | IC50 |
0.011 μM
Compound: 6
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Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
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[PMID: 24256217] |
TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:549 cells
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Concentration:
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Incubation Time:72 hours
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Result:Inhibited the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM.
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 mouse xenograft model[1]
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Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Oral administration; once daily; for 19 days
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Result:Inhibited the growth of A549 cells in a dose-dependent manner.
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Animal Model:A549 mouse xenograft model (pharmacokinetic )[1]
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Dosage:25 mg/kg
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Administration:Oral administration
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Result:Cmax = 3542 ng/mL, AUC = 6604 ng h/mL
Chemical Information
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CAS No. 1206170-62-8
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Appearance Solid
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Molecular Weight 324.38
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Formula C17H20N6O
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Color White to off-white
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SMILES
N#CC1=C(N=C(NC2=CC=C(C(N)=O)C=C2)C=C1N)NC(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (154.14 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)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 3.0828 mL | 15.4140 mL | 30.8280 mL | 77.0701 mL |
| 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL | 15.4140 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 mL | 7.7070 mL | |
| 15 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1380 mL | |
| 20 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8535 mL | |
| 25 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
| 30 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5690 mL | |
| 40 mM | 0.0771 mL | 0.3854 mL | 0.7707 mL | 1.9268 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 80 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9634 mL | |
| 100 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL |
TC-Mps1-12 Related Classifications
HY-110115 Related Classifications
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