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ARV-825

🥰Excellent
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

ARV-825

🥰Excellent
Purity: 98%
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 SizePriceAvailabilityQuantity
1 mg$60In Stock
5 mg$147In Stock
10 mg$178In Stock
25 mg$272In Stock
50 mg$372In Stock
100 mg$556In Stock
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Purity:98%
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Product Introduction

Bioactivity
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 BD1:90 nM (Kd), BRD4 BD2:28 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.
Chemical Properties
Molecular Weight923.43
FormulaC46H47ClN8O9S
Cas No.1818885-28-7
SmilesCC=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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.0829 mL5.4146 mL10.8292 mL54.1460 mL
5 mM0.2166 mL1.0829 mL2.1658 mL10.8292 mL
10 mM0.1083 mL0.5415 mL1.0829 mL5.4146 mL
20 mM0.0541 mL0.2707 mL0.5415 mL2.7073 mL
50 mM0.0217 mL0.1083 mL0.2166 mL1.0829 mL

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