VZ 185
Tocris Bioscience, part of Bio-Techne | Catalog # 6936
Potent and selective BRD7/9 Degrader (PROTAC®)
Key Product Details
Description
Potent and selective BRD7/9 Degrader (PROTAC®)
Product Description
VZ 185 is a potent and selective VHL-based dual Degrader (PROTAC®) of BRD7/9 (DC50 values are 4 and 34 nM for BRD7 and BRD9, respectively). Exhibits selectivity for BRD7/9 degradation over other bromodomain-containing proteins and other BAF/PBAF subunits. Displays cytotoxicity towards EOL-1 and A-204 cancer cell lines.Negative control cis VZ 185 (Cat. No. 6939) and BRD7 antibody validated for Western Blot also available: Catalog # NBP1-28727.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under licence from the University of Dundee.Product Specifications
Molecular Weight
995.23
Formula
C53H67FN8O8S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(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
CAS Number
2306193-61-1
PubChem ID
138454768
InChI Key
ZAGCLFXBHOXXEN-JPTLTNPLSA-N
SMILES
CN(C(C1=C2C=CN=C1)=O)C=C2C3=CC(OC)=C(C(OC)=C3)CN4CCN(CC4)CCCCCOC5=CC(C6=C(N=CS6)C)=CC=C5CNC([C@@H]7C[C@H](CN7C([C@H](C(C)(C)C)NC(C8(CC8)F)=O)=O)O)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 99.52 | 100 |
Preparing Stock Solutions
for VZ 185
The following data is based on the product molecular weight 995.23
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.00 mL | 5.02 mL | 10.05 mL |
| 5 mM | 0.20 mL | 1.00 mL | 2.01 mL |
| 10 mM | 0.10 mL | 0.50 mL | 1.00 mL |
| 50 mM | 0.02 mL | 0.10 mL | 0.20 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Riching Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation. Curr.Res.Chem.Biol.
- Zoppi 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 PMID: 30540463
Product Specific Notices for VZ 185
For research use only
Loading...
Loading...