Information ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. Targets BRD2-BD2 (Cell-free assay); BRD3-BD2 (Cell-free assay); BRD4-BD2 (Cell-free assay); BRD3-BD1 (Cell-free assay); BRD4-BD1 (Cell-free assay) 32850,4.7 nM(Kd); 7.6 nM(Kd); 7.6 nM(Kd); 8.3 nM(Kd); 9.6 nM(Kd) In vitro ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis. In vivo ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model. Cell Research(from reference) Cell lines：22Rv1 cells, VCaP cells, LnCaP95 cells Concentrations：1-300 nM Incubation Time：24 h, 72 h
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ARV-771
CAS number：1949837-12-0 molecular formula：C49H60ClN9O7S2
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| Chinese alias | - | ||
| English alias | JQ1-VHL | ||
| CAS number | 1949837-12-0 | molecular formula | C49H60ClN9O7S2 |
| molecular weight | 986.64 g/mol | Exact mass | - |
| PSA | 259.000 Ų | logp | 5.9 |
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1949837-12-0 | ARV-771.pdf
