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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-126275 |
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| Réf. fabricant | 18796346 |
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| Nom chimique ou matériau | 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 |
|---|
| Quantité | 5 mg |
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| Cible | Active Degraders |
|---|
| Formule moléculaire | C<sub>38</sub>H<sub>43</sub>N<sub>11</sub>O<sub>11</sub> |
|---|
| Pureté | 0.98 |
|---|
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