(E, E) -GLL398
(E, E) -GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM) . (E, E) -GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM) . The introduced boronic acid group of (E, E) -GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604[1].
Product Specifications
CAS Number
[2077980-83-5]
UNSPSC
12352005
Target
Estrogen Receptor/ERR
Type
Reference compound
Related Pathways
Vitamin D Related/Nuclear Receptor
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/e-e-gll398.html
Smiles
O=C(/C=C/C1=CC=C(C=C1)/C(C2=CC=C(C=C2)B(O)O)=C(CC)/C3=CC=CC=C3)O
Molecular Formula
C25H23BO4
Molecular Weight
398.26
References & Citations
[1]Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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