DS12881479
Based on 1 publication(s) in Google Scholar
DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.63%
- CAS. Nr.: 2373065-59-7
- Formel: C16H19N3OS
- Molecular Weight:301.41
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) DS12881479
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Biologische Aktivität
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MNK1 387 nM (IC50) |
eIF4E |
DYRK1A |
DS12881479 potently inhibits recombinant MNK1 kinase activity with an IC50 of 387 ± 94 nM[1].
DS12881479 (72-120 h) inhibits proliferation of MV4-11, MOLM-13, and MM.1S cancer cells with IC50 values of 3.32 ± 0.66 μM, 12.08 ± 0.92 μM, and 5.32 ± 1.38 μM, respectively, and lacks activity against MDA-MB-231 cells (IC50 >20 μM)[1].
DS12881479 (300-1000 nM; 24 h) inhibits eIF4E phosphorylation in MV4-11 cells without degrading MNK1 or MNK2 protein[1].
DS12881479 (300 nM; 24 h) weakly induces apoptosis in MV4-11 cells, with a total apoptotic rate of 13.9%[1].
DS12881479 potently inhibits inactive human Mnk1 with an IC50 of 21 nM, and shows weaker inhibition of active human Mnk1 with an IC50 of 416 nM[2].
DS12881479 (5 μM) inhibits only FLT3 and DYRK1a by over 50%, demonstrating good selectivity for human Mnk1 over most other tested active kinases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:300 nM, 1000 nM
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Incubation Time:24 h
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Result:Reduced p-eIF4E levels in a concentration-dependent manner.
Did not reduce MNK1 or MNK2 protein levels.
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Cell Line:MV4-11 cells
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Concentration:300 nM
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Incubation Time:24 h
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Result:Induced 13.9% total apoptosis in MV4-11 cells, with a low level of late apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-PrkdcscidIl2rgem1/Smoc mice (female, 5 weeks old, acute myeloid leukemia xenograft model with MV4-11 cells)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 16 days
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Result:Achieved a tumor growth inhibition rate of 28%.
Reduced p-eIF4E levels.
Showed no significant difference in body weight and ALT, TBIL, ALP, TBA, UA, CR compared with the vehicle control group.
Chemical Information
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CAS. Nr. 2373065-59-7
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Appearance Solid
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Molecular Weight 301.41
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Formel C16H19N3OS
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Color White to off-white
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SMILES
O=C(C1CCN(C)CC1)NC2=NC=C(C3=CC=CC=C3)S2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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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J Med Chem
Discovery of P11-2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. [Abstract]2025 May 22;68(10):10092-10110. PMID: 40334145
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (829.43 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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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)
Verweise
[1]. Yang Z, et al. Discovery of P11-2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. J Med Chem. 2025;68(10):10092-10110. [Content Brief]
[2]. Matsui Y, et al. A novel inhibitor stabilizes the inactive conformation of MAPK-interacting kinase 1. Acta Crystallogr F Struct Biol Commun. 2018;74(Pt 3):156-160. [Content Brief]
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 | 3.3177 mL | 16.5887 mL | 33.1774 mL | 82.9435 mL |
| 5 mM | 0.6635 mL | 3.3177 mL | 6.6355 mL | 16.5887 mL | |
| 10 mM | 0.3318 mL | 1.6589 mL | 3.3177 mL | 8.2943 mL | |
| 15 mM | 0.2212 mL | 1.1059 mL | 2.2118 mL | 5.5296 mL | |
| 20 mM | 0.1659 mL | 0.8294 mL | 1.6589 mL | 4.1472 mL | |
| 25 mM | 0.1327 mL | 0.6635 mL | 1.3271 mL | 3.3177 mL | |
| 30 mM | 0.1106 mL | 0.5530 mL | 1.1059 mL | 2.7648 mL | |
| 40 mM | 0.0829 mL | 0.4147 mL | 0.8294 mL | 2.0736 mL | |
| 50 mM | 0.0664 mL | 0.3318 mL | 0.6635 mL | 1.6589 mL | |
| 60 mM | 0.0553 mL | 0.2765 mL | 0.5530 mL | 1.3824 mL | |
| 80 mM | 0.0415 mL | 0.2074 mL | 0.4147 mL | 1.0368 mL | |
| 100 mM | 0.0332 mL | 0.1659 mL | 0.3318 mL | 0.8294 mL |
DS12881479 Related Classifications
HY-148105 Related Classifications
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