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α1A-AR Degrader 9c

Cat. No. 7278 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Selective α1A adrenergic receptor Degrader (PROTAC®)
化学名： 2-(2-(2-(2-(4-(4-(4-Amino-6,7-dimethoxyquinazolin-2-yl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for α1A-AR Degrader 9c

α1A-AR Degrader 9c is a selective α1A-adrenergic receptor Degrader (PROTAC®; DC50 = 2.86 µM, 94% α1A-adrenoceptor degradation at 10 µM for 12 h). It comprises the α-adrenoceptor antagonist Prazosin (Cat. No. 0623), joined by a linker to a cereblon ligand Pomalidomide (Cat. No. 6302). α1A-AR Degrader 9c selectively downregulates α1A-adrenoceptor levels, but not α1B-AR and α1D-AR in HEK293 cells. α1A-AR Degrader 9c shows concentration-dependent antiproliferative activity in PC-3 prostate cancer cells (IC50 = 6.12 µM) in vitro, and PC-3 tumor xenografts in vivo.

α1 AR antibody validated for Western Blot also available: Catalog # MAB10298.

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

技术数据 for α1A-AR Degrader 9c

分子量 829.83
公式 C38H43N11O11
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2863635-02-1
InChI Key SFODRSARUJDQSA-UHFFFAOYSA-N
Smiles NC1=NC(N2CCN(C(C3=CN(CCOCCOCCOCC(NC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)N=N3)=O)CC2)=NC7=CC(OC)=C(OC)C=C71

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for α1A-AR Degrader 9c

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 82.98 100

制备储备液 for α1A-AR Degrader 9c

以下数据基于产品分子量 829.83。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.21 mL 6.03 mL 12.05 mL
5 mM 0.24 mL 1.21 mL 2.41 mL
10 mM 0.12 mL 0.6 mL 1.21 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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产品说明书 for α1A-AR Degrader 9c

分析证书/产品说明书
化学品安全技术说明书

参考文献 for α1A-AR Degrader 9c

参考文献是支持产品生物活性的出版物。

Li et al (2020) First small-molecule PROTACs for G protein-coupled receptors: inducing α1A-adrenergic receptor degradation. Acta.Pharm.Sin.B 10 1669 PMID: 33088687

If you know of a relevant reference for α1A-AR Degrader 9c, please let us know.

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia