MS9715
Based on 1 Customer Validation
MS9715 is a selective NSD3 PROTAC degrader with a Kd value of 1.3 μM and a DC50 of 4.9 μM. MS9715 recruits the VHL E3 ligase to mediate the ubiquitination and degradation of NSD3. MS9715 downregulates oncogenes including CBLB, IFITM1 and MAP7. MS9715 induces Apoptosis. MS9715 is applicable to the research of hematological malignancies and lung cancer.
(Pink: NSD3 ligand (HY-114208); Blue: VHL ligand (HY-112078); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.48%
- Formel: C58H74FN9O5S
- Molecular Weight:1028.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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NSD3 4.9 μM (DC50) |
VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
2.3 μM
Compound: 40; MS-9715
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Antiproliferative activity against human EOL1 cells assessed as cell growth inhibition
Antiproliferative activity against human EOL1 cells assessed as cell growth inhibition
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[PMID: 38805937] |
MS9715 selectively degrades NSD3 (with a DC50 of 4.9 μM in MOML13 cells) and cMyc via the ubiquitin-proteasome system (UPS), downregulates NSD3-related oncogenes, and potently inhibits the growth of hematologic cancer cell lines EOL-1, RSV4;11 and MM1.S, with EC50 values of 2.3 μM, 3.5 μM and 3.3 μM, respectively[1].
MS9715 (200 μM) binds to the recombinant NSD3 PWWP1 domain, with a Kd value of 1.3 μM[2].
MS9715 (2.5-10 μM; 0-48 h) induces time- and concentration-dependent degradation of NSD3S in EOL-1, MM1.S and MOLM13 hematological cancer cells via a mechanism dependent on VHL and the ubiquitin-proteasome system, with a DC50 of 4.9 μM in MOLM13 cells[2].
MS9715 (2.5 μM; 4 weeks) potently inhibits colony formation of EOL-1 and MM1.S hematological cancer cells[2].
MS9715 effectively degrades NSD3, inhibits c-Myc expression, and suppresses the growth of acute myeloid leukemia, acute lymphoblastic leukemia, and lung cancer cells. Its activity against NSD3-dependent cancers is superior to that of BI-9321 (HY-114208)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EOL-1, MM1.S, MOLM13, 293FT WT/VHL KO hematological cancer cells
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Concentration:2.5 μM (EOL-1/MM1.S cells); 5 μM (MLN9708/MLN4924/VHL ligand pre-treatment experiments); 2.5-10 μM (293FT WT/VHL KO cells)
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Incubation Time:48 h (EOL-1/MM1.S cells); 0-48 h (EOL-1/MM1.S cells); 48 h (MLN9708/MLN4924/VHL ligand pre-treatment experiments); 48 h (293FT WT/VHL KO cells)
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Result:Induced concentration-dependent degradation of NSD3S in EOL-1, MM1.S, and MOLM13 cells, with significant degradation observed at 24 hours and more profound degradation at 48 hours.
In MOLM13 cells, had a half-maximal degradation concentration (DC50) of 4.9 μM and maximum degradation (Dmax) of greater than 80% after 48-hour treatment.
Blocked NSD3S degradation via pre-treatment with MLN9708, MLN4924, or VHL ligands in a concentration-dependent manner, and abrogated degradation in VHL-knockout 293FT cells.
Chemical Information
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Appearance Solid
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Molecular Weight 1028.33
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Formel C58H74FN9O5S
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Color White to off-white
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SMILES
O=C(NCCCCCCCCC(N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)=O)CCCNCC4=CC(C)=C(C5=C(C6=CC=NC7=C6C=CC(F)=C7)N(C)C=N5)C(C)=C4
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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 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (97.25 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: ≥ 2.5 mg/mL (2.43 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.
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 (284 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)
Verweise
[1]. Kabir M, et al. Chemically induced degradation of epigenetic targets. Chemical Society reviews. 2023 Jul 03;52(13):4313-4342. [Content Brief]
[2]. Xu C, et al. A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells. Cell chemical biology. 2022 Mar 17;29(3):386-397.e9. [Content Brief]
[3]. Liu X, et al. PROTACs in Epigenetic Cancer Therapy: Current Status and Future Opportunities. Molecules (Basel, Switzerland). 2023 Jan 26;28(3):1217. [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 | 0.9725 mL | 4.8623 mL | 9.7245 mL | 24.3113 mL |
| 5 mM | 0.1945 mL | 0.9725 mL | 1.9449 mL | 4.8623 mL | |
| 10 mM | 0.0972 mL | 0.4862 mL | 0.9725 mL | 2.4311 mL | |
| 15 mM | 0.0648 mL | 0.3242 mL | 0.6483 mL | 1.6208 mL | |
| 20 mM | 0.0486 mL | 0.2431 mL | 0.4862 mL | 1.2156 mL | |
| 25 mM | 0.0389 mL | 0.1945 mL | 0.3890 mL | 0.9725 mL | |
| 30 mM | 0.0324 mL | 0.1621 mL | 0.3242 mL | 0.8104 mL | |
| 40 mM | 0.0243 mL | 0.1216 mL | 0.2431 mL | 0.6078 mL | |
| 50 mM | 0.0194 mL | 0.0972 mL | 0.1945 mL | 0.4862 mL | |
| 60 mM | 0.0162 mL | 0.0810 mL | 0.1621 mL | 0.4052 mL | |
| 80 mM | 0.0122 mL | 0.0608 mL | 0.1216 mL | 0.3039 mL |
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