| Identification | Back Directory | [Name]
ARV-825 | [CAS]
1818885-28-7 | [Synonyms]
ARV-825
AVR-825
CS-2252
ARV-825;ARV 825;ARV825
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)- | [Molecular Formula]
C46H47ClN8O9S | [MDL Number]
MFCD29472237 | [MOL File]
1818885-28-7.mol | [Molecular Weight]
923.43 |
| Chemical Properties | Back Directory | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO:5.0(Max Conc. mg/mL);5.41(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);5.41(Max Conc. mM)
Water:0.0(Max Conc. mg/mL);0.0(Max Conc. mM) | [form ]
A crystalline solid | [pka]
10.74±0.40(Predicted) |
| Hazard Information | Back Directory | [Description]
ARV-825 is a PROTAC molecule composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety. ARV-825 recruits BRD4 to E3 ubiquitin ligase cereblon, resulting in the degradation of BRD4. | [Biological Activity]
ARV-825 is a BRD4 inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, causing rapid, efficient and sustained degradation of BRD4 protein and sustained downregulation of MYC levels. | [in vivo]
In the mouse model transplanted with human leukemia cells, the leukemia burden of the mice in the ARV-825 experimental group was significantly lower than that in the control group, and their survival time was also longer than that in the control group. | [target]
| Target | Value | BRD4 BD2
(Cell-free assay) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 28 nM(Kd) BRD4 BD1
(Cell-free assay) | 90 nM(Kd) |
| [storage]
Store at -20°C |
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