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Synonyms:


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $125 | In Stock | In Stock | |
| 5 mg | $313 | In Stock | In Stock | |
| 10 mg | $522 | In Stock | In Stock | |
| 25 mg | $987 | In Stock | In Stock | |
| 50 mg | $1,660 | In Stock | In Stock | |
| 100 mg | $2,390 | In Stock | In Stock |
| Description | PROTAC BRD4 ligand-1 is a PROTAC and a BRD4-targeted inhibitor with BET inhibitory activity. This ligand is cell-permeable and is used for the synthesis of PROTAC GNE-987, possessing antitumor potential. |
| Targets & IC50 | BRD 4 BD1:41.8 nM, EOL-1 AML cells:0.03 nM (DC50) |
| In vitro | Methods: Degradation assays were performed in the EOL-1 AML cell line to evaluate the degradation activity of PROTAC GNE-987 synthesized from PROTAC BRD4 ligand-1. Results: The half-degradation concentration (DC50) of PROTAC GNE-987 was 0.03 nM.[1] |
| Molecular Weight | 500.47 |
| Formula | C23H18F2N4O5S |
| Cas No. | 2313230-51-0 |
| Smiles | Cn1cc2-c3cc(CS(C)(=O)=O)c(cc3N(Cc3c[nH]c(c23)c1=O)c1ncc(F)cc1F)C(O)=O |
| Relative Density. | 1.68 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | DMSO: 4.5 mg/mL (8.99 mM), Sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||
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.
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.
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