PROTAC BRD4 Degrader linker conjugate 

PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC₅₀ values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845))^[1].\n

PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein in PC3 prostate cancer cells, with DC₅₀ values of 0.86 nM and 7.6 nM, respectively^[1].

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

1312.50

C₅₉H₇₁F₂N₉O₁₅S₄

2417370-42-2

Solid

White to off-white

CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@H](CN3C([C@@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)OC(OCC(C)(C)SS(C)(=O)=O)=O)=O)C=C2

Room temperature in continental US; may vary elsewhere.

• [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;64(5):2576-2607.  [Content Brief]