2077980-83-5

2077980-83-5 structure

Name: GLL398
Chemical Name: (2E)-3-(4-{(1E)-1-[4-(Dihydroxyboryl)phenyl]-2-phenyl-1-buten-1-yl}phenyl)acrylic acid
CAS Number: 2077980-83-5
Molecular Formula: C₂₅H₂₃BO₄
Molecular Weight: 398.259
Create Date: 2021-01-07 11:06:58
Modify Date: 2024-01-06 19:46:10
GLL398 is an Oral Selective Estrogen Receptor Downregulator. GLL398 strongly binds to ERα in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 μg·h/mL) in rats as compared to GW7604 (AUC = 3.35 μg·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation.

Name	(2E)-3-(4-{(1E)-1-[4-(Dihydroxyboryl)phenyl]-2-phenyl-1-buten-1-yl}phenyl)acrylic acid
Synonyms	2-Propenoic acid, 3-[4-[(1E)-1-(4-boronophenyl)-2-phenyl-1-buten-1-yl]phenyl]-, (2E)- (2E)-3-(4-{(1E)-1-[4-(Dihydroxyboryl)phenyl]-2-phenyl-1-buten-1-yl}phenyl)acrylic acid