SML2934

VZ185

≥98% (HPLC)

• Synonym(s): (2S,4R)-N-(2-(5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyloxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide, VZ 185, VZ-185
• Empirical Formula (Hill Notation): C₅₃H₆₇FN₈O₈S
• CAS Number: 2306193-61-1
• Molecular Weight: 995.21
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C

Description

Biochem/physiol Actions

VZ185 is a potent and selective bromodomain proteins BRD7 and BRD9 degrader that targets BRD7/9 for von Hippel-Lindau (VHL) ubiquitin ligase complex-mediated degradation. VZ185 effectively induces cellular BRD7/9 degradation (by 90% BRD7 & 86% BRD9 in 4 h in HeLa cells, by 84% BRD7 in 2 h in RI-1 cells; BRD7/9 IC50 = 4.5/1.76 nM in 8 h in RI-1 cells) and exerts potent cytotoxicity in BRD9-dependent cancer cultures (IC50 = 3.389 nM/EOL-1 & 39.81 nM/A-204 post 7-day treatment).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable