MKI-2
MKI-2 is a selective MASTL inhibitor with an IC50 of 37.44 nM. MKI-2 induces mitotic catastrophe resulting from the modulation of the MASTL-PP2A axis in breast cancer cells. MKI-2 reduces phospho-ENSA, total, phospho-c-Myc levels. MKI-2 inhibts cancer cells proliferation, migration and induces DNA damage. MKI-2 inhibits germinal vesicle breakdown in mouse oocytes. MKI-2 can be used for the research of cancer, such as breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 438204-56-9
- Formula: C22H19N7
- Molecular Weight:381.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
MKI-2 potently inhibits recombinant MASTL kinase activity with an IC50 of 37.44 nM[1].
MKI-2 (14 h) inhibits cellular MASTL activity in MCF7 breast cancer cells with an IC50 of 142.7 nM, as measured by reduced phospho-ENSA levels[1].
MKI-2 (100 nM) is selective for MASTL, as it does not inhibit recombinant ROCK1, PKACα, or p70S6K kinases and only slightly inhibits AKT1 at a concentration of 100 nM[1].
MKI-2 (250 nM; 12-24 h) modulates the MASTL-PP2A-c-Myc axis in MCF7, BT549, and MDA-MB-468 breast cancer cells by increasing PP2A activity, reducing phospho-ENSA and total, phospho-c-Myc levels[1].
MKI-2 (250 nM; 24 h) induces mitotic catastrophe in MCF7 breast cancer cells at 250 nM for 24 h, as evidenced by mitotic arrest, altered apoptotic and increased DNA damage marker (γ-H2AX) levels, and increased aberrant nuclear cells[1].
MKI-2 (15.63-1000 nM; 72 h) inhibits the proliferation of MCF7, BT549, MDA-MB-468, and 4T1 breast cancer cells with IC50 values ranging from 56.53 nM to 124.6 nM after 72 h of treatment[1].
MKI-2 (6.25-25 nM) inhibits colony, 3D spheroid, and mammosphere formation of MCF7 breast cancer cells[1].
MKI-2 (250 nM; 24 h) inhibits the migration and invasion of BT549 breast cancer cells at 250 nM for 24 h[1].
MKI-2 (250 nM-2 μM; 12-48 h) reduces the percentage of GVBD and has no significant effects on mouse oocytes viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7, BT549, and MDA-MB-468 breast cancer cells
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Concentration:250 nM
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Incubation Time:12 h
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Result:Reduced levels of phospho-ENSA and phospho-c-Myc (Ser62), and decreased total c-Myc protein levels in treated breast cancer cells.
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Cell Line:MCF7, BT549, MDA-MB-468, and 4T1 breast cancer cells
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Concentration:15.63-1000 nM
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Incubation Time:72 h
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Result:Inhibited proliferation of all tested breast cancer cell lines with IC50 values of 124.6 nM (MCF7), 58.65 nM (BT549), 56.53 nM (4T1), and 94.22 nM (MDA-MB-468).
Chemical Information
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CAS No. 438204-56-9
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Molecular Weight 381.43
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Formula C22H19N7
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SMILES
N#CCC1=CC=C(NC2=NC(NC3=NNC(C4CC4)=C3)=C5C=CC=CC5=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (262.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (6.55 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.
In Vivo Dissolution Calculator
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.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6217 mL | 13.1086 mL | 26.2171 mL | 65.5428 mL |
| 5 mM | 0.5243 mL | 2.6217 mL | 5.2434 mL | 13.1086 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6217 mL | 6.5543 mL | |
| 15 mM | 0.1748 mL | 0.8739 mL | 1.7478 mL | 4.3695 mL | |
| 20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2771 mL | |
| 25 mM | 0.1049 mL | 0.5243 mL | 1.0487 mL | 2.6217 mL | |
| 30 mM | 0.0874 mL | 0.4370 mL | 0.8739 mL | 2.1848 mL | |
| 40 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5243 mL | 1.3109 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0924 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3277 mL | 0.8193 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 mL |
MKI-2 Related Classifications
HY-185310 Related Classifications
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