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ARV-825

Chemical Structure : ARV-825

CAS No.: 1818885-28-7

ARV-825 (ARV 825, ARV825)

Catalog No.: PC-45097Not For Human Use, Lab Use Only.

ARV-825 is a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 via the proteasome.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ARV-825 (ARV825) is a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 via the proteasome.
ARV-825 shows more significant and longer lasting c-MYC suppression than small molecule inhibitors (JQ1, OTX015).
ARV-825 treatment leads to a superior effect on BL cells proliferation suppression.

Physicochemical Properties

M.Wt 923.4316
Formula C46H47ClN8O9S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((S)-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-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide

References

1. Lu J, et al. Chem Biol. 2015 Jun 18;22(6):755-63.

2. Abruzzese MP, et al. J Hematol Oncol. 2016 Dec 1;9(1):134.

3. Saenz DT, et al. Leukemia. 2017 Jan 31. doi: 10.1038/leu.2016.393.

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