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XY221

Chemical Structure : XY221

CAS No.:

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XY221 (Compound 16o)

Catalog No.: PC-23522Not For Human Use, Lab Use Only.

XY221 is a potent, BRD4 BD2-selective inhibitor with IC50 of 5.8 nM, >600-fold selective over BRD4 BD1 and 9–32-fold over BRD2/3/T BD2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

XY221 is a potent, BRD4 BD2-selective inhibitor with IC50 of 5.8 nM, >600-fold selective over BRD4 BD1 and 9–32-fold over BRD2/3/T BD2.
XY221 shows 66-144-fold selectivity over other BET BD2 domains in BLI assays.
XY221 demonstrates good antiproliferation activity in MV4–11 (IC50 = 0.51 μM) and LNCaP (IC50 = 0.68 μM)
XY221 is a valuable candidate for BRD4 BD2 advancing epigenetic research.

Physicochemical Properties

M.Wt 559.64
Formula C32H34FN3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(2-Ethyl-4-(methoxymethyl)-1H-imidazol-5-yl)-7-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-5-methylfuro[3,2-c]pyridin-4(5H)-one

References

1. Li J, et al. J Med Chem. 2024 Nov 27. doi: 10.1021/acs.jmedchem.4c02516.

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