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ARV-825

Cat. No. M6206
ARV-825 Structure
Size Price Availability Quantity
1mg USD 100 In stock
5mg USD 230 In stock
10mg USD 360 In stock
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Quality Control
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 923.43
Formula C46H47ClN8O9S
CAS Number 1818885-28-7
Purity 99.91%
Solubility DMSO 45 mg/mL
Storage at -20°C
References

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.
Saenz DT, et al. Leukemia. 2017 Sep;31(9):1951-1961. PMID: 28042144.

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.
Abruzzese MP, et al. J Hematol Oncol. 2016 Dec 1;9(1):134. PMID: 27903272.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ARV-825 supplier, Epigenetic Reader Domain, inhibitors

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