PROTAC BRD4 Degrader-15

TargetMol
Product Code: TAR-T40074
Supplier: TargetMol
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TAR-T40074-100mg100mgEnquire
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TAR-T40074-500mg500mgEnquire
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C

Images

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Further Information

Bioactivity:
PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2. Additionally, PROTAC BRD4 Degrader-15 demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells.
CAS:
2417370-67-1
Molecular Weight:
1149.3
Purity:
0.98
SMILES:
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)COCCc2cc(N)cc(OCCNC(=O)c3cc4N(Cc5c[nH]c6c5c(cn(C)c6=O)-c4cc3CS(C)(=O)=O)c3ncc(F)cc3F)c2)C(C)(C)C)cc1 |@@:75|

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.