TargetMol

PROTAC BRD4 Degrader-13

Product Code:
 
TAR-T40075
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (PROTAC), linking ligands for von Hippel-Lindau and BRD4 proteins. In the context of PC3 prostate cancer cells, this compound effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies. The degradation of BRD4 protein is achieved with remarkable potency, exhibiting a DC 50 of 0.025 nM and 6.0 nM when combined with STEAP1 and CLL1 antibodies, respectively.
CAS:
2417370-71-7
Molecular Weight:
1492.55
Purity:
0.98
SMILES:
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@H](CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)c2cc3N(Cc4c[nH]c5c4c(cn(C)c5=O)-c3cc2CS(C)(=O)=O)c2ncc(F)cc2F)C(C)(C)C)OP(O)(=O)OP(O)(=O)OCCNC(=O)CCCCCN2C(=O)C=CC2=O)cc1 |c:103|

References

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.