α1A-AR Degrader 9c

Name: α1A-AR Degrader 9c
Brand: Tocris Bioscience
SKU: 7278

Tocris Bioscience, part of Bio-Techne | Catalog # 7278

COA / SDS

Selective α1A adrenergic receptor Degrader (PROTAC®)

Key Product Details

Description:	Selective α_1A 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)
Molecular Weight:	829.83

View Full Technical Details for α1A-AR Degrader 9c

Technical Data
Citations

Biological Activity for α1A-AR Degrader 9c

α1A-AR Degrader 9c is a selective α_1A-adrenergic receptor Degrader (PROTAC^®; DC₅₀ = 2.86 µM, 94% α_1A-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 α_1A-adrenoceptor levels, but not α_1B-AR and α_1D-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 for α1A-AR Degrader 9c

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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	0.60 mL	1.21 mL
50 mM	0.02 mL	0.12 mL	0.24 mL

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References for α1A-AR Degrader 9c

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

Li First small-molecule PROTACs for G protein-coupled receptors: inducing α_1A-adrenergic receptor degradation. Acta.Pharm.Sin.B 2020 PMID: 33088687