Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&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. |
細胞研究 | 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. |
分子量 | 923.43 |
分子式 | C46H47ClN8O9S |
CAS No. | 1818885-28-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (54.15 mM)
You can also refer to dose conversion for different animals. 詳細
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ARV-825 1818885-28-7 Chromatin/Epigenetic Epigenetic Reader Domain ARV 825 inhibit PROTACs Inhibitor ARV825 inhibitor