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α1A-AR Degrader 9c

Cat. No. 7278 Submit a Review Datasheet / COA / SDS
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Description: Selective α1A adrenergic receptor Degrader (PROTAC®)
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Technical Data for α1A-AR Degrader 9c

M. Wt 829.83
Formula C38H43N11O11
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for α1A-AR Degrader 9c

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 82.98 100

Preparing Stock Solutions for α1A-AR Degrader 9c

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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Product Datasheets for α1A-AR Degrader 9c

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for α1A-AR Degrader 9c

References are publications that support the biological activity of the product.

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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Citations for α1A-AR Degrader 9c

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Literature in this Area

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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