ARV 771 is a potent BET bromodomain PROTAC™ degrader (DC50 = < 1nM). Comprises a BRD4-binding moiety joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Degrades BRD2/3/4 in castration-resistant prostate cancer (CRPC) cell lines. Reduces androgen receptor levels and induces apoptosis in CRPC cells
in vitro
. Down-regulates BRD4 and induces tumor regression in CRPC xenografts in mice. Also reduces leukemia burden in a mouse model. Induces degradation of BRD-tagged CAR (chimeric antigen receptor) in T cells.
PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license
Caractéristiques techniques
| Marque | Tocris |
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| Réf. B-LABO | BL-RE-125785 |
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| Réf. fabricant | 18726196 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-2-(tert-Butyl)-15-(-4-(4-chlorophenyl)-2,3,9-trimethyl-6 H-thieno[3,2-f][1,2,4 ]triazolo[4,3-a][1,4 ]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-(-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carbox |
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| CAS | 1949837-12-0 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>49</sub>H<sub>60</sub>ClN<sub>9</sub>O<sub>7</sub>S<sub>2</sub> |
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| Pureté | 0.98 |
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