PROTAC BRD4 Degrader-8 

PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells^[1].

IC50: 1.1 nM (BRD4 BD1), 1.4 nM (BRD4 BD2)^[1]

PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC₅₀ of 28 nM^[1].
PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC₅₀ of 11 nM^[1].
PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC₅₀ of 7.5 nM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1102.23

Solid

C₅₃H₆₁F₂N₉O₁₁S₂

O[[email protected]](C[[email protected]]1C(NCC2=CC=C(C=C2)C3=C(N=CS3)C)=O)CN1C([[email protected]@H](NC(COCCOCCOCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.  [Content Brief]