α1A-AR Degrader 9c

Tocris Bioscience | Catalog # 7278

Selective α1A adrenergic receptor Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Selective α1A adrenergic receptor Degrader (PROTAC®)
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Product Description

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.

Product Specifications for α1A-AR Degrader 9c

Molecular Weight

829.83

Formula

C38H43N11O11

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

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Background References

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

Product Documents for α1A-AR Degrader 9c

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for α1A-AR Degrader 9c

For research use only

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