Chemical Structure : ARV-825
CAS No.: 1818885-28-7
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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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.
M.Wt | 923.4316 | |
Formula | C46H47ClN8O9S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
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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