OXFBD04

Names

[ Name ]:
OXFBD04

Biological Activity

[Description]:

OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4:166 nM (IC50)

[In Vitro]

OXFBD04 (0.01-100 μM; 48 hours) inhibits cancer cell lines growth[1]. OXFBD04 (10 µM; for 10, 24, or 48 hours) induces MYC suppression in MCF7 breast cancer cells[1]. Cell Viability Assay[1] Cell Line: A498 (renal), HT-29 (colon), and MCF7 (breast) cancer cell lines Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 48 hours Result: Inhibited cancer cell lines growth.

[In Vivo]

OXFBD04 has optimised physicochemical properties (LE=0.43; LLE=5.74; SFI=5.96), and good metabolic stability (t1/2=388 min). OXFBD04 has CLint of 3.57 µL/min/mg[1].

[References]

[1]. Jennings LE, et al. BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability. Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₆N₂O₃

[ Molecular Weight ]:
296.32

Related Compounds

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