MS4078
Based on 4 publication(s) in Google Scholar
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.72%
- CAS. Nr.: 2229036-62-6
- Formel: C45H52ClN9O8S
- Molecular Weight:914.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) MS4078
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Biologische Aktivität
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ALK |
Cereblon |
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Cell Line
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Type | Value | Description | References |
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| NCI-H2228 | IC50 |
33 nM
Compound: 6; MS4078
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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 |
16 nM
Compound: 41; MS4048
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Antiproliferative activity against human SU-DHL-1 cells
Antiproliferative activity against human SU-DHL-1 cells
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[PMID: 35763424] |
| SU-DHL-1 | IC50 |
33 nM
Compound: 6; MS4078
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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] |
MS4078 effectively inhibits cancer cell proliferation. MS4078 (10-3, 10-2.5, 10-2, 10-1.5, 10-1, 10-0.5, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 33±1 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4078(10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM; 3 days)[1].
MS4078 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, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 11±2 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, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of 59 ± 16 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=33 ± 1 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 11 ± 2 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC50 of 59 ± 16 nM in NCI-H2228 cells
Chemical Information
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CAS. Nr. 2229036-62-6
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Appearance Solid
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Molecular Weight 914.47
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Formel C45H52ClN9O8S
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Color Light yellow to yellow
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SMILES
CC(C)S(C1=C(NC2=NC(NC3=C(OC(C)C)C=C(C4CCN(CC(NCCNC5=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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Int J Pharm
2024 Jan 25:650:123725. PMID: 38113976 -
Colloids Surf B Biointerfaces
Precision targeting of ALK-positive lung cancer: Engineering HFN@MS4078 nanocages for optimized PROTAC delivery. [Abstract]2025 Jul 22:255:114974. PMID: 40712494 -
Mol Pharm
PROTAC Enabling Formulation In Vivo: Implications of the Polymeric Carrier Eudragit E PO. [Abstract]2025 Aug 24. PMID: 40849796 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (54.68 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (2.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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.
Reinheit & Dokumentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0935 mL | 5.4676 mL | 10.9353 mL | 27.3382 mL |
| 5 mM | 0.2187 mL | 1.0935 mL | 2.1871 mL | 5.4676 mL | |
| 10 mM | 0.1094 mL | 0.5468 mL | 1.0935 mL | 2.7338 mL | |
| 15 mM | 0.0729 mL | 0.3645 mL | 0.7290 mL | 1.8225 mL | |
| 20 mM | 0.0547 mL | 0.2734 mL | 0.5468 mL | 1.3669 mL | |
| 25 mM | 0.0437 mL | 0.2187 mL | 0.4374 mL | 1.0935 mL | |
| 30 mM | 0.0365 mL | 0.1823 mL | 0.3645 mL | 0.9113 mL | |
| 40 mM | 0.0273 mL | 0.1367 mL | 0.2734 mL | 0.6835 mL | |
| 50 mM | 0.0219 mL | 0.1094 mL | 0.2187 mL | 0.5468 mL |
MS4078 Related Classifications
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