MS4077
Based on 1 Customer Validation
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37 nM for binding affinity to ALK.
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- Pureza: 99.66%
- No. CAS: 2230077-10-6
- Fòrmula: C55H72ClN9O13S
- Peso molecular:1134.73
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Almacenamiento:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ALK |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H2228 | IC50 |
46 nM
Compound: 5; MS4077
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Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay
Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay
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[PMID: 29627725] |
| SU-DHL-1 | IC50 |
46 nM
Compound: 5; MS4077
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Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay
Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay
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[PMID: 29627725] |
MS4077 effectively inhibits cancer cell proliferation. MS4077 (10-3-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 46 ± 4 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4077(10-2-100.5 μM; 3 days)[1].
MS4077 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4077 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 3±1 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4077 reduces the EML4-ALK protein levels with similar DC50 value of 34±9 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-1 and NCI-H2228 cells
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Concentration:10-3, 10-2.5, 10-2,10-1.5, 10-1, 10-0.5, and 1 μM for SU-DHL-1 cells; 10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM for NCI-H2228 cells
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Incubation Time:3 days
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Result:Inhibited proliferation of SU-DHL-1 cells (IC50=46 ± 4 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells.
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Cell Line:SU-DHL-1 and NCI-H2228 cells
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Concentration:1, 3, 10, 30, and 100 μM for SU-DHL-1 cells; 3, 10, 30, 60, and 100 μM for NCI-H2228 cells
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Incubation Time:16 hours
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Result:Reduced the NPM-ALK protein levels with impressive DC50 of 3 ± 1 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC50 of 34 ± 9 nM in NCI-H2228 cells.
Chemical Information
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No. CAS 2230077-10-6
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Appearance Solid
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Peso molecular 1134.73
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Fòrmula C55H72ClN9O13S
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Color Yellow to green
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SMILES
CC(C)S(C1=C(NC2=NC(NC3=C(OC(C)C)C=C(C4CCN(CC(NCCOCCOCCOCCOCCOCCNC5=C(C(N(C6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)CC4)C(C)=C3)=NC=C2Cl)C=CC=C1)(=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 110 mg/mL (96.94 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: 6 mg/mL (5.29 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 6 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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: ≥ 6 mg/mL (5.29 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
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Ficha de datos (270 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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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 (sealed storage, away from moisture and light). 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 | 0.8813 mL | 4.4063 mL | 8.8127 mL | 22.0317 mL |
| 5 mM | 0.1763 mL | 0.8813 mL | 1.7625 mL | 4.4063 mL | |
| 10 mM | 0.0881 mL | 0.4406 mL | 0.8813 mL | 2.2032 mL | |
| 15 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 20 mM | 0.0441 mL | 0.2203 mL | 0.4406 mL | 1.1016 mL | |
| 25 mM | 0.0353 mL | 0.1763 mL | 0.3525 mL | 0.8813 mL | |
| 30 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL | |
| 40 mM | 0.0220 mL | 0.1102 mL | 0.2203 mL | 0.5508 mL | |
| 50 mM | 0.0176 mL | 0.0881 mL | 0.1763 mL | 0.4406 mL | |
| 60 mM | 0.0147 mL | 0.0734 mL | 0.1469 mL | 0.3672 mL | |
| 80 mM | 0.0110 mL | 0.0551 mL | 0.1102 mL | 0.2754 mL |
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