MS44
Based on 1 Customer Validation
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand.
(Pink: Aurora B ligand (HY-175526); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.89%
- Formula: C57H72FN11O8S
- Molecular Weight:1090.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Aurora B 103 nM (DC50) |
VHL |
MS44 (Compound 18) (1 nM-10 μM, 1-96 h) effectively degrades AURKB in a concentration- and time-dependent manner in HPAF-11 cells by hijacking the UPS and also in multiple cancer cell lines[1].
MS44 (1 μM, 24-96 h) inhibits the proliferation in HPAF-11, K562, U937, CFPAC-1, SW1783 and HT-29 cells[1].
MS44 (48 h) induces U937 cells G2/M arrest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HPAF-11 cells, K562 cells and U937 cells
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Concentration:1 μM
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Incubation Time:24, 48, 72 and 96 h
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Result:Effectively suppressed the proliferation of HPAF-11 cells.
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Cell Line:HPAF-11, K562, U937, CFPAC-1, SW1783 and HT-29 cells
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Concentration:1, 3, 10, 30, 100, 300 nM, 1, 3, 10 μM for HPAF-11 and 1 μM for other cells
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Incubation Time:1, 2, 4, 8, 12, and 24 h for HPAF-11 and 24 h for other cells
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Result:Induced significant degradation of AURKB in all cells.
Degraded AURKB in a concentration- and time-dependent manner in HPAF-11 cells by hijacking the UPS.
Selectively degraded AURKB over AURKA and AURKC in HPAF-11 cells.
Chemical Information
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Appearance Solid
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Molecular Weight 1090.31
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Formula C57H72FN11O8S
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCC(N(CCCOC4=CC5=NC=NC(NC6=NNC(CC(NC7=CC=CC(F)=C7)=O)=C6)=C5C=C4)CCO)=O)=O)=O)O)=O)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 : 100 mg/mL (91.72 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)
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 (2.29 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.29 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 0.9172 mL | 4.5859 mL | 9.1717 mL | 22.9293 mL |
| 5 mM | 0.1834 mL | 0.9172 mL | 1.8343 mL | 4.5859 mL | |
| 10 mM | 0.0917 mL | 0.4586 mL | 0.9172 mL | 2.2929 mL | |
| 15 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5286 mL | |
| 20 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1465 mL | |
| 25 mM | 0.0367 mL | 0.1834 mL | 0.3669 mL | 0.9172 mL | |
| 30 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 40 mM | 0.0229 mL | 0.1146 mL | 0.2293 mL | 0.5732 mL | |
| 50 mM | 0.0183 mL | 0.0917 mL | 0.1834 mL | 0.4586 mL | |
| 60 mM | 0.0153 mL | 0.0764 mL | 0.1529 mL | 0.3822 mL | |
| 80 mM | 0.0115 mL | 0.0573 mL | 0.1146 mL | 0.2866 mL |