ARV-825
CAS No. : 1818885-28-7
| Size | Price | Stock |
|---|---|---|
| 5mg | $132 | In-stock |
| 10mg | $161 | In-stock |
| 25mg | $275 | In-stock |
| 50mg | $330 | In-stock |
| 100mg | $551 | In-stock |
| 250mg | $1102 | In-stock |
| 500 mg | Get quote | |
| 1 g | Get quote | |
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| Cat. No. : | HY-16954 |
| M.Wt: | 923.43 |
| Formula: | C46H47ClN8O9S |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 50 mg/mL |
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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