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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.68%
- Fòrmula: C35H38N4O6S2
- Peso molecular:674.83
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Almacenamiento: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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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
Descripciòn
IC50 & Target
[1]|
PLK1 |
eRF3a/GSPT1 |
eRF3b/GSPT2 |
In Vitro
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.
Chemical Information
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Appearance Solid
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Peso molecular 674.83
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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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. 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 Related Classifications
HY-150259 Related Classifications
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