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PROTAC MEK1 Degrader-1
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Catalog No. T79144Cas No. 2671004-41-2
PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1].
PROTAC MEK1 Degrader-1
😃Good
Catalog No. T79144Cas No. 2671004-41-2
PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1]. |
| In vitro | PROTAC MEK1 Degrader-1 (Compound 3) induces MEK1 degradation at concentrations of 1 μM and 10 μM over 12 hours, while lower concentrations increase MEK1 and ERK1/2 expression [1]. At 10 μM, it significantly inhibits IL6 secretion over 12 hours and shows anti-proliferative activity against A375 cells from 0 to 72 hours [1]. Significant MEK and ERK1/2 degradation occurs at 5 hours post-treatment with 10 μM, with complete inhibition at 8 hours [1]. |
| Molecular Weight | 1201.17 |
| Formula | C53H66FIN8O11S2 |
| Cas No. | 2671004-41-2 |
| Smiles | N(C1=C(NS(=O)(=O)C2=CC=C(CCC(NCCOCCOCCOCC(N[C@H](C(=O)N3[C@H](C(N[C@@H](C)C4=CC=C(C=C4)C=5SC=NC5C)=O)C[C@@H](O)C3)C(C)(C)C)=O)=O)C=C2)C=C(C)C(=O)N1C)C6=C(F)C=C(I)C=C6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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