MS44
Based on 1 Customer Validation
MS44 is a potent and selective AURKB PROTAC degrader with a DC50 of 103 nM. MS44 recruits the VHL E3 ligase to form a ternary complex, mediating the specific degradation of AURKB via the ubiquitin-proteasome system, and exhibits no activity against related kinases such as AURKA/C. MS44 can be used for research on AURKB-dependent tumors.
(Pink: Aurora B ligand (HY-175526); Blue: VHL ligand (HY-112078); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.89%
- Fòrmula: C57H72FN11O8S
- Peso molecular:1090.31
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas Aurora Kinase
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Aurora B 103 nM (DC50) |
VHL |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HPAF-II | DC50 |
103 nM
|
Aurora kinase B (AURKB) degradation in human HPAF-11 pancreatic cancer cells assessed via western blot after 24 h incubation.
Aurora kinase B (AURKB) degradation in human HPAF-11 pancreatic cancer cells assessed via western blot after 24 h incubation.
|
40730065 |
In Vitro
MS44 (1 nM-10 μM; 1 h-24 h) potently and selectively degrades the AURKB protein in HPAF-11 human pancreatic cancer cells in a time- and concentration-dependent manner in vitro, with a DC50 of 103 nM, and exhibits no effect on AURKA and AURKC; it also does not alter the transcriptional level of AURKB mRNA[1].
MS44 (1 μM; 24 h) does not affect the protein levels of kinases including PLK1, CDK2 and MAPK in PC-3 and HPAF-11 cells[1].
MS44 (1 μM; 24-96 h) potently degrades AURKB in human leukemia K562 and U937 cells, human pancreatic cancer CFPAC-1 cells, human astrocytoma SW1783 cells, and human colorectal adenocarcinoma HT-29 cells[1].
MS44 (1 μM; 24 h-96 h) potently inhibits the proliferation of HPAF-11 human pancreatic cancer cells, K562 and U937 human leukemia cells, and induces G2/M phase cell cycle arrest in U937 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:HPAF-11
-
Concentration:1, 3, 10, 30, 100, 300 nM, 1, 3, 10 μM
-
Incubation Time:1, 2, 4, 8, 12, 24 h
-
Result:Induced AURKB degradation in a concentration-dependent manner (DC50 = 103 nM) and exhibited a "hook effect" at higher concentrations.
Rapidly and time-dependently induced the degradation of AURKB.
-
Cell Line:HPAF-11
-
Concentration:2 h
-
Incubation Time:24 h; 1 h-24 h
-
Result:Did not alter the mRNA transcription level of AURKB.
-
Cell Line:PC-3, HPAF-11
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Did not affect the protein expression levels of PLK1, CDK2, and MAPK.
Selectively degraded AURKB without affecting AURKA and AURKC.
-
Cell Line:HPAF-11, K562, U937
-
Concentration:1 μM
-
Incubation Time:24, 48, 72, 96 h
-
Result:Effectively inhibited the proliferation of these cancer cell lines.
-
Cell Line:U937
-
Concentration:1 μM
-
Incubation Time:48 h
-
Result:Significantly decreased G1-phase cells and induced cell cycle arrest at the G2/M phase.
-
Cell Line:CFPAC-1, SW1783, HT-29
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Effectively degraded AURKB in multiple cancer cell lines overexpressing AURKB.
Chemical Information
-
Appearance Solid
-
Peso molecular 1090.31
-
Fòrmula C57H72FN11O8S
-
Color White to off-white
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
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)
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 (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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Pureza y Documentación
-
Ficha de datos (281 KB)
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
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 |
MS44 Related Classifications
HY-175525 Related Classifications
Powered by Bioz
Keywords