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α1A-AR Degrader 9c

Catalog #: 7278 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7278/5
α1A-AR Degrader 9c | CAS No. 2863635-02-1 | Active Degraders
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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%

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Biological Activity

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

M.Wt:
829.83
Formula:
C38H43N11O11
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2863635-02-1

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.

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