Network Version
ARV-825 Data Sheet
| Product Name: | ARV-825 |
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|---|---|---|
| CAS No.: | 1818885-28-7 | |
| Cat. No.: | HY-16954 | |
| MWt: | 923.43 | |
| Formula: | C46H47ClN8O9S | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 50 mg/mL | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds 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]. | ||
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