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PROTAC BRD4 Degrader-15

Names

[ CAS No. ]:
2417370-67-1

[ Name ]:
PROTAC BRD4 Degrader-15

Biological Activity

[Description]:

PROTAC BRD4 Degrader-15 is a potent BRD4 degrader, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PROTAC >> PROTAC
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4 BD1:7.2 nM (IC50)

BRD4 BD2:8.1 nM (IC50)


[In Vitro]

PROTAC BRD4 Degrader-15 (compound 13) (4 h) inhibits suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 15 nM[1]. PROTAC BRD4 Degrader-15 (6 days) inhibits the proliferation of HL-60 and PC3-S1 cells, with an IC50 of 4.2 nM and 91 nM[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C57H62F2N10O10S2

[ Molecular Weight ]:
1149.29

[ Storage condition ]:
2-8°C

Related Compounds