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ARV-825
Catalog No. T5434Cas No. 1818885-28-7
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.
ARV-825
Catalog No. T5434Cas No. 1818885-28-7
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $60 | In Stock | |
| 5 mg | $147 | In Stock | |
| 10 mg | $178 | In Stock | |
| 25 mg | $272 | In Stock | |
| 50 mg | $372 | In Stock | |
| 100 mg | $556 | In Stock |
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Purity:98%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| Storage | store at low temperature,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. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (54.15 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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