1818885-28-7
1818885-28-7 structure
- Name: ARV-825
- Chemical Name: ARV-825
- CAS Number: 1818885-28-7
- Molecular Formula: C46H47ClN8O9S
- Molecular Weight: 923.432
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2018-01-27 16:14:01
- Modify Date: 2024-01-06 22:15:37
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ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
| Name | ARV-825 |
|---|---|
| Synonyms |
2-[(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-[4-(2-{2-[2-(2-{[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethoxy}ethoxy)phenyl]acetamide
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[4-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)- |
| Description | ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. |
|---|---|
| Related Catalog | |
| 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]. |
| Kinase Assay | Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C46H47ClN8O9S |
| Molecular Weight | 923.432 |
| Exact Mass | 922.287537 |
| LogP | 2.72 |
| Index of Refraction | 1.701 |
| Storage condition | 2-8℃ |