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PROTAC BRD4 Degrader-15

Catalog No. T40074   CAS 2417370-67-1
Synonyms: PROTAC BRD4 Degrader-15

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.

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PROTAC BRD4 Degrader-15 Chemical Structure
PROTAC BRD4 Degrader-15, CAS 2417370-67-1
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 BRD4 BD2:8.1 nM (IC50), BRD4 BD1:7.2 nM (IC50)
In vitro PROTAC BRD4 Degrader-15 (compound 13) effectively reduces MYC gene expression in MV4-11 AML cells within 4 hours, demonstrating significant potency with an IC50 of 15 nM[1]. Additionally, over a period of 6 days, this compound substantially inhibits the growth of HL-60 and PC3-S1 cells, displaying IC50 values of 4.2 nM and 91 nM, respectively[1].
Synonyms PROTAC BRD4 Degrader-15
Molecular Weight 1149.3
Formula C57H62F2N10O10S2
CAS No. 2417370-67-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

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