VZ185
- Product Name
- VZ185
- CAS No.
- 2306193-61-1
- Chemical Name
- VZ185
- Synonyms
- VZ185;(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)pentyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide;(2S,4R)-N-[(2-{[5-(4-{[2,6-dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)phenyl]methyl}piperazin-1-yl)pentyl]oxy}-4-(4-methyl-1,3-thiazol-5-yl)phenyl)methyl]-1-[(2S)-2-[(1-fluorocyclopropyl)formamido]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide
- CBNumber
- CB65821299
- Molecular Formula
- C53H67FN8O8S
- Formula Weight
- 995.21
- MOL File
- 2306193-61-1.mol
VZ185 Property
- Boiling point:
- 1116.1±65.0 °C(Predicted)
- Density
- 1.34±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 200 mg/mL (200.96 mM; Need ultrasonic)
- pka
- 13.79±0.20(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- SML2934
- Product name
- VZ185
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $246.05
- Updated
- 2025/07/31
- Product number
- SML2934
- Product name
- VZ185
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $832
- Updated
- 2025/07/31
- Product number
- 6936
- Product name
- VZ185
- Purity
- ≥98%(HPLC)
- Packaging
- 5
- Price
- $259
- Updated
- 2021/12/16
- Product number
- CS-0082100
- Product name
- VZ185
- Purity
- >97.0%
- Packaging
- 1mg
- Price
- $393
- Updated
- 2021/12/16
VZ185 Chemical Properties,Usage,Production
Uses
VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively[1].
Biological Activity
VZ185 is a potent and selective bromodomain proteins BRD7 and BRD9 degrader th at 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).
IC 50
BRD7: 4.5 nM (DC50); BRD9: 1.8 nM (DC50)
storage
Store at -20°C
References
[1] Zoppi V, et al. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. J Med Chem. 2019 Jan 24;62(2):699-726. DOI:10.1021/acs.jmedchem.8b01413
VZ185 Preparation Products And Raw materials
Raw materials
Preparation Products
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