PROTAC BRD4 Degrader-9

PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively[1].

Product Specifications

CAS Number

[2417370-42-2]

UNSPSC

12352203

Hazard Statement

H315, H319, H320

Target

Epigenetic Reader Domain; PROTACs

Type

ADC Related

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-brd4-degrader-9.html

Purity

98.98

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C59H71F2N9O15S4

Molecular Weight

1312.50

Precautions

H315, H319, H320

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.