ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

BRD4(2):7.6 nM (Kd), BRD2(2):4.7 nM (Kd), BRD2(1):34 nM (Kd), BRD3(1):8.3 nM (Kd), BRD4(1):9.6 nM (Kd), BRD3(2):7.6 nM (Kd)

C49H60ClN9O7S2

986.64

CC=1C2=C(N3C([C@H](CC(NCCOCCCOCC(N[C@H](C(=O)N4[C@H](C(N[C@@H](C)C5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

DMSO: 250 mg/mL (253.39 mM), Sonication is recommended.

>98.00%