MDEG-541
Based on 1 Customer Validation
MDEG-541 is a PROTAC degrader targeting MYC, GSPT1/2 and PLK1. MDEG-541 induces degradation via proteasome- and ubiquitin-dependent pathways. MDEG-541 exhibits anti-tumor activity in gastrointestinal cancer cells and patient-derived organoids. MDEG-541 can be used for the research of gastrointestinal cancer.
(Pink: MYC-MAX ligand (HY-175964); Blue: Cereblon ligand (HY-14658); Black: linker).
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 : 98.68%
- 分子式: C35H38N4O6S2
- 分子量:674.83
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保管条件:Powder -20°C, 3 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]
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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
製品説明
IC50 & Target
[1]|
PLK1 |
eRF3a/GSPT1 |
eRF3b/GSPT2 |
体外実験
MDEG-541 (5-20 μM; 24 h) reduces MYC protein expression in MYC-amplified HCT116 colon cancer cells and PSN1 pancreatic cancer cells in a dose-dependent manner, and almost completely depletes this protein at a concentration of 20 μM[1].
MDEG-541 (0.049-50 μM; 72 h) reduces the viability of HCT116 colon cancer cells and PSN1 pancreatic cancer cells, with GI50 values of 14.3 μM and 10.7 μM for the two cell lines, respectively[1].
MDEG-541 (0.048-50 μM; 72 h) reduces the viability of 17 human colon and pancreatic cancer cell lines, with GI50 values ranging from 3 μM to 50 μM, and cell sensitivity is positively correlated with CRBN mRNA expression[1].
MDEG-541 (0.19-50 μM; 72 h) reduces the viability of patient-derived primary gastrointestinal cancer organoids, with a GI50 value ranging from 0.97 μM to 20.5 μM[1].
MDEG-541 (10 μM; 3-24 h) first degrades GSPT1/2 (3 h) and then MYC (12 h) in KP4 cells via the CRBN-ubiquitin-proteasome axis[1].
MDEG-541 (5-20 μM; 3-24 h) induces CRBN-, ubiquitin- and proteasome-dependent degradation of PLK1 in a dose- and time-dependent manner, leading to nearly complete depletion of PLK1 at 24 h in HCT116 colon cancer cells and PSN1 pancreatic cancer cells[1].
MDEG-541 (10 μM; 3-24 h) induces time-dependent downregulation of GSPT1, GSPT2 and MYC proteins in PSN1 pancreatic cancer cells, and depletion of GSPT1 and GSPT2 occurs earlier than that of MYC after treatment with 10 μM MDEG-541[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:human colon cancer HCT116 cells, human pancreatic cancer PSN1 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent decrease in MYC protein expression in both cell lines.
Reduced relative MYC expression to ~60% at 5 μM, ~40% at 10 μM, and ~10% at 20 μM in HCT116 cells.
Reduced relative MYC expression to ~80% at 5 μM, ~60% at 10 μM, and ~5% at 20 μM in PSN1 cells.
Induced statistically significant reduction compared to vehicle controls.
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Cell Line:human colon cancer HCT116 cells, human pancreatic cancer PSN1 cells
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Concentration:0.049 μM, 0.098 μM, 0.19 μM, 0.39 μM, 0.78 μM, 1.56 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM
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Incubation Time:72 h
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Result:Caused a dose-dependent reduction in cell viability in both cell lines.
Exhibited a half-maximal growth inhibitory concentration (GI50) of 14.3 μM in HCT116 cells.
Exhibited a half-maximal growth inhibitory concentration (GI50) of 10.7 μM in PSN1 cells.
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Cell Line:human pancreatic cancer KP4 cells
human colon cancer HCT116 cells, human pancreatic cancer PSN1 cells -
Concentration:5 μM, 10 μM, 20 μM (24 h treatment); 10 μM (time-course intervals)
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Incubation Time:3 h, 12 h, 24 h
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Result:Induced degradation of multiple oncoproteins in gastrointestinal cancer cells via the CRBN-ubiquitin-proteasome axis.
In KP4 cells, treatment with 10 μM of the compound induced degradation of GSPT1/2 as early as 3 h, followed by MYC degradation starting at 12 h, with near-complete depletion of MYC by 24 h.
In HCT116 and PSN1 cells, 5-20 μM of the compound for 24 h dose-dependently reduced PLK1 expression; time-course analysis (10 μM) showed that PLK1 levels decreased by 3 h and were almost completely depleted by 24 h.
Mechanistic studies demonstrated that the degradation of GSPT1/2, MYC, and PLK1 all depended on CRBN, ubiquitination, and proteasome activity, and was not accompanied by changes in their corresponding mRNA levels.
化学情報
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性状 Solid
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分子量 674.83
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分子式 C35H38N4O6S2
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Color Light yellow to yellow
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SMILES
O=C(C1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)NCCCCCCCCN(C/4=O)C(SC4=C/C5=CC=C(C(C)C)C=C5)=S
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 116.67 mg/mL (172.89 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 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
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 |
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| DMSO | 1 mM | 1.4819 mL | 7.4093 mL | 14.8185 mL | 37.0464 mL |
| 5 mM | 0.2964 mL | 1.4819 mL | 2.9637 mL | 7.4093 mL | |
| 10 mM | 0.1482 mL | 0.7409 mL | 1.4819 mL | 3.7046 mL | |
| 15 mM | 0.0988 mL | 0.4940 mL | 0.9879 mL | 2.4698 mL | |
| 20 mM | 0.0741 mL | 0.3705 mL | 0.7409 mL | 1.8523 mL | |
| 25 mM | 0.0593 mL | 0.2964 mL | 0.5927 mL | 1.4819 mL | |
| 30 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2349 mL | |
| 40 mM | 0.0370 mL | 0.1852 mL | 0.3705 mL | 0.9262 mL | |
| 50 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7409 mL | |
| 60 mM | 0.0247 mL | 0.1235 mL | 0.2470 mL | 0.6174 mL | |
| 80 mM | 0.0185 mL | 0.0926 mL | 0.1852 mL | 0.4631 mL | |
| 100 mM | 0.0148 mL | 0.0741 mL | 0.1482 mL | 0.3705 mL |
MDEG-541 関連分類
HY-150259 関連分類
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