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Tocris Bioscience™ a1A-AR Degrader 9c
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Catalog No. 72785
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72-785 5 mg
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Catalog No. 72-785 Supplier Tocris Bioscience™ Supplier No. 7278/5
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Description

Selective α1A adrenergic receptor Degrader (PROTAC™)

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.

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

Specifications

Chemical Name or Material 2-(2-(2-(2-(4-(4-(4-Amino-6,7-dimethoxyquinazolin-2-yl)piperazine-1-carbonyl)-1 H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide
Quantity 5 mg
Target Active Degraders
Molecular Formula C38H43N11O11
Purity 0.98
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