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ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $60 | In Stock | In Stock | |
| 5 mg | $147 | In Stock | In Stock | |
| 10 mg | $178 | In Stock | In Stock | |
| 25 mg | $272 | In Stock | In Stock | |
| 50 mg | $372 | In Stock | In Stock | |
| 100 mg | $556 | In Stock | In Stock |
| Description | ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested. |
| Targets&IC50 | BRD4 BD2:28 nM (Kd), BRD4 BD1:90 nM (Kd) |
| In vitro | ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis. |
| Cell Research | Cells (50000/100ul) were seeded in 96-well tissue culture plates followed by addition of ARV-825?at indicated concentration.?After 72 hours, 100 μL per well of reconstituted CellTiter-Glo reagent was added and read on Cytation 3 imaging reader.?Relative cell growth was determined by comparing assay readings of treated cells with control DMSO treated cells.?For apoptosis induction, Caspase-Glo 3/7 Assay was used following manufacturer s instruction. |
| Molecular Weight | 923.43 |
| Formula | C46H47ClN8O9S |
| Cas No. | 1818885-28-7 |
| Smiles | CC=1C2=C(N3C([C@H](CC(NC4=CC=C(OCCOCCOCCOCCNC5=C6C(C(=O)N(C6=O)C7C(=O)NC(=O)CC7)=CC=C5)C=C4)=O)N=C2C8=CC=C(Cl)C=C8)=NN=C3C)SC1C |
| Relative Density. | 1.47 g/cm3 (Predicted) |
| Storage | store under nitrogen,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 127.5 mg/mL (138.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.17 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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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