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].

Product Specifications

CAS Number

[3026420-38-9]

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-brd4-degrader-8.html

Purity

99.45

Solubility

DMSO : 90 mg/mL (ultrasonic)

Smiles

O[C@H](C[C@H]1C(NCC2=CC=C(C=C2)C3=C(N=CS3)C)=O)CN1C([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

Molecular Formula

C53H61F2N9O11S2

Molecular Weight

1102.23

References & Citations

[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.