MS934
Based on 1 Customer Validation
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma.
(Pink: MEK1 and MEK2 ligand (HY-168288); Blue: VHL ligand (HY-112078); Black: linker (HY-168289)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.48%
- CAS 番号: 2756323-15-4
- 分子式: C52H69F3IN7O6S
- 分子量:1104.11
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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CRAF |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | GI50 |
23 μM
Compound: 27; MS934
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Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
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[PMID: 33284613] |
| SK-MEL-28 | GI50 |
40 nM
Compound: 27; MS934
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Antiproliferative activity against human SK-MEL-28 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SK-MEL-28 cells incubated for 3 days by WST8 assay
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[PMID: 33284613] |
| SU-DHL-1 | GI50 |
330 nM
Compound: 27; MS934
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Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
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[PMID: 33284613] |
MS934 (0.1 nM-10 μM, 3 days) shows antiproliferative activity against human HT-29 cells, SK-MEL-28 cells and SU-DHL-1 cells, with GI50s of 23 μM, 40 nM and 330 nM[1].
MS934 (10 nM-3.3 μM, 24 h) causes collateral degradation of CRAF in KRAS mutant cells via a PROTAC-mechanism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 cells
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Concentration:0.01, 0.04, 0.12, 0.37, 1.1 and 3.3 μM
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Incubation Time:24 h
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Result:Showed a reduction in MEK1 and MEK2 protein levels, as well as active phosphorylated MEK1/2(S218/S222).
Showed a dose-dependent reduction in phosphorylated CRAF(S338) and total CRAF protein levels.
化学情報
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CAS 番号 2756323-15-4
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性状 Solid
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分子量 1104.11
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分子式 C52H69F3IN7O6S
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Color White to off-white
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SMILES
O=C(C1=C(C(F)=C(C=C1)F)NC2=C(C=C(C=C2)I)F)NOCCCCNCCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(N=CS5)C)C=C4)C)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (45.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 1.25 mg/mL (1.13 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
純度とドキュメンテーション
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データシート (272 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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取扱説明書 (2659 KB)
参考文献
[1]. Hu J, et al. Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders. J Med Chem. 2020 Dec 24;63(24):15883-15905. [Content Brief]
[3]. Kurimchak AM, et al. The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells. Sci Signal. 2022 Aug 30;15(749):eabn2707. [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 (protect from light, stored under nitrogen). 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 | 0.9057 mL | 4.5285 mL | 9.0571 mL | 22.6427 mL |
| 5 mM | 0.1811 mL | 0.9057 mL | 1.8114 mL | 4.5285 mL | |
| 10 mM | 0.0906 mL | 0.4529 mL | 0.9057 mL | 2.2643 mL | |
| 15 mM | 0.0604 mL | 0.3019 mL | 0.6038 mL | 1.5095 mL | |
| 20 mM | 0.0453 mL | 0.2264 mL | 0.4529 mL | 1.1321 mL | |
| 25 mM | 0.0362 mL | 0.1811 mL | 0.3623 mL | 0.9057 mL | |
| 30 mM | 0.0302 mL | 0.1510 mL | 0.3019 mL | 0.7548 mL | |
| 40 mM | 0.0226 mL | 0.1132 mL | 0.2264 mL | 0.5661 mL |
MS934 関連分類
HY-153863 関連分類
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