ARV-771 (C09-1504-760)

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 Specifications and Purity: 98% Molecular Formula: C49H60ClN9O7S2 Molecular Weight: 986.64 PubChem CID: 126619980 Isomeric SMILES: CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NCCOCCCOCC(=O)N[C@H](C(=O)N4C[C@@H](C[C@H]4C(=O)N[C@@H](C)C5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C