ARV-825 Chemical Properties

Density 

1.47±0.1 g/cm3(Predicted)

storage temp. 

2-8°C(protect from light)

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)

color 

Light yellow to yellow

Safety Information

HS Code 

2933998090

ARV-825 Usage And Synthesis

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.

Uses

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.

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

< td class="border-bottom: 1px dotted #ccc;padding: 5px;"> 28 nM(Kd)

Target	Value
BRD4 BD2 (Cell-free assay)
BRD4 BD1 (Cell-free assay)	90 nM(Kd)

References

[1] Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. DOI:10.1016/j.chembiol.2015.05.009

ARV-825(1818885-28-7)Related Product Information

• ARV110
• ARCC-4
• ARV-771
• ARV-471