VZ 185

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Cat.No. 6936 - VZ 185 | C53H67FN8O8S | CAS No. 2306193-61-1
说明: Potent and selective BRD7/9 Degrader (PROTAC®)
化学名: (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
纯度: ≥98% (HPLC)
文献 (4)

生物活性 for VZ 185

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) also available.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.


Sold under licence from the University of Dundee.

技术数据 for VZ 185

分子量 995.23
公式 C53H67FN8O8S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2306193-61-1
PubChem ID 138454768
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


Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for VZ 185

溶剂 最高浓度 mg/mL 最高浓度 mM
DMSO 99.52 100

制备储备液 for VZ 185

以下数据基于产品分子量 995.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1 mL 5.02 mL 10.05 mL
5 mM 0.2 mL 1 mL 2.01 mL
10 mM 0.1 mL 0.5 mL 1 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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产品说明书 for VZ 185


参考文献 for VZ 185


Zoppi et al (2019) 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. 62 699 PMID: 30540463

Riching et al (2021) Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation. Curr.Res.Chem.Biol. 1 100009

If you know of a relevant reference for VZ 185, please let us know.

关键词: VZ 185, VZ 185 supplier, VZ185, potent, selective, VHL, active, degraders, degrades, PROTACs, protac, BRD7, BRD9, targeted, protein, degradation, tpd, Active, Degraders, Bromodomains, 6936, Tocris Bioscience

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