TC Mps1 12 |
| رقم الكتالوجGC13727 |
TC Mps1 12 هو مثبط قوي وانتقائي للمغزل أحادي القطب 1 (Mps1) ، مع IC50 يبلغ 6.4 نانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1206170-62-8
Sample solution is provided at 25 µL, 10mM.
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Target: Monopolar spindle 1 (Mps1)
IC50: 6.4 nM
TC Mps1 12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor with IC50 value of 6.4 nM [1]. Monopolar spindle 1 (Mps1), also known as TTK, plays a critical role in the spindle assembly checkpoint, centrosome duplication, and the maintenance of chromosomal stability. Mps1 is highly expressed in cancer cells and activated during mitosis. Therefore, Mps1 is a promising anticancer drug target [1].
In vitro: TC Mps1 12 displayed an excellent selectivity profile in a panel of 95 kinases, except for the Flt3 and Flt3 mutants (D835Y) [1]. TC Mps1 12 showed cellular inhibition of Mps1with an IC50 value of 131 nM in cell line that stably expresses FLAG-tagged Mps1. In addition, TC Mps1 12 inhibited the growth of A549 lung carcinoma cell lines with IC50 value of 0.84 μM [1].
In vivo: TC Mps1 12 (25 mg/kg, oral administration) treatment showed good pharmacokinetic (PK) properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL in mice [1]. Moreover, TC Mps1 12 (25 to 100 mg/kg, oral administration) dose-dependently inhibited the tumor growth of A549 cells without body weight loss in the mouse A549 xenograft model [1].
Reference:
1. Kusakabe K, Ide N, Daigo Y, Itoh T, Higashino K, Okano Y, et al. Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. ACS Med Chem Lett. 2012;3(7):560-4.
| Cas No. | 1206170-62-8 | SDF | |
| Chemical Name | 4-((4-amino-6-(tert-butylamino)-5-cyanopyridin-2-yl)amino)benzamide | ||
| Canonical SMILES | CC(C)(NC1=C(C(N)=CC(NC2=CC=C(C(N)=O)C=C2)=N1)C#N)C | ||
| Formula | C17H20N6O | M.Wt | 324.38 |
| الذوبان | <32.44mg/ml in DMSO; <6.49mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0828 mL | 15.414 mL | 30.828 mL |
| 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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