ARV-825

ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.Formal Name: 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)phenyl)acetamide. CAS Number: 1818885-28-7. Molecular Formula: C46H47ClN8O9S. Formula Weight: 923.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 1 mg/ml. lambdamax: 247, 409 nm. SMILES: CC1=NN=C2[C@H](CC(NC3=CC=C(OCCOCCOCCOCCNC4=C(C(N(C5C(NC(CC5)=O)=O)C6=O)=O)C6=CC=C4)C=C3)=O)N=C(C7=CC=C(Cl)C=C7)C8=C(SC(C)=C8C)N21. InChi Code: InChI=1S/C46H47ClN8O9S/c1-26-27(2)65-46-39(26)41(29-7-9-30(47)10-8-29)50-35(42-53-52-28(3)54(42)46)25-38(57)49-31-11-13-32(14-12-31)64-24-23-63-22-21-62-20-19-61-18-17-48-34-6-4-5-33-40(34)45(60)55(44(33)59)36-15-16-37(56)51-43(36)58/h4-14,35-36,48H,. InChi Key: RWLOGRLTDKDANT-TYIYNAFKSA-N.