ARV-825
CAS No. : 1818885-28-7

ARV-825
Cat. No. : CS-4776
M. Wt. : 923.43
Size Stock Price Quantity Add to Cart Quotation Online
5mg In-stock $180.0
10mg In-stock $276.0
50mg In-stock $840.0
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  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: ARV-825; 
Cat. No. : CS-4776
CAS No. : 1818885-28-7
Formula: C46H47ClN8O9S
M. Wt. : 923.43
Solubility: 10 mM in DMSO

Activity:

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. IC50 & Target: Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)[1] In Vitro: 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[1].

Protocol:

Kinase Assay: [1]Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[1].

References:

Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

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    • CS-4776 20243
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