(E,E)-GLL398

• UNSPSC Description:

  (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].

• Target Antigen:

  Estrogen Receptor/ERR

• Type:

  Reference compound

• Related Pathways:

  Vitamin D Related/Nuclear Receptor

• 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 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

• Clinical Information:

  No Development Reported

• CAS Number:

  2077980-83-5