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ARV-825

Cat. No. M6206
ARV-825 Structure
Size Price Availability Quantity
1mg USD 75  USD75 In stock
5mg USD 167  USD167 In stock
10mg USD 265  USD265 In stock
25mg USD 485  USD485 In stock
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Quality Control & Documentation
Biological Activity

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 µM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors.

Protocol (for reference only)
Cell Experiment
Cell lines SKO-007(J3) cells
Preparation method Lysates of SKO-007(J3) cells, untreated or treated with ARV-825 (0.2 μM), lenalidomide (10 μM), or the combination of the two drugs for 24 h, were subjected to Western blotting using anti-BRD4 or anti-p85 antibodies.
Concentrations 0.2 μM
Incubation time 48 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 923.43
Formula C46H47ClN8O9S
CAS Number 1818885-28-7
Solubility (25°C) DMSO 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Saenz DT, et al. Leukemia. Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.

[2] Abruzzese MP, et al. J Hematol Oncol. Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells: role of cMYC-IRF4-miR-125b interplay.

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