GNE-149 | ER degrader | Probechem Biochemicals

Chemical Structure : GNE-149

GNE-149 (GNE149)

Catalog No.: PC-20524Not For Human Use, Lab Use Only.

GNE-149 (GNE149) is a potent, full estrogen receptor alpha (ERα) antagonist and degrader with IC50 of 0.053 nM (MCF7, ERα degradation).

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Biological Activity

GNE-149 (GNE149) is a potent, full estrogen receptor alpha (ERα) antagonist and degrader with IC50 of 0.053 nM (MCF7, ERα degradation).
GNE-149 exhibits IC50 value of 0.66 nM and 0.69 nM in MCF-7 and T47D proliferation assays.
GNE-149 (0.3-30 mg/kg) showed dose-dependent efficacy in MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant

Physicochemical Properties

M.Wt	503.59
Formula	C28H33F4N3O
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	C[C@@H]1CC2=C([C@@H](C3=C(F)C=C(OC4CN(CCCF)C4)C=C3F)N1CC(C)(F)C)NC5=C2C=CC=C5

References

1. Liang J, et al. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347.

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GNE-149 (GNE149)

Biological Activity

Physicochemical Properties

References

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