(E,E)-GLL398 [2077980-83-5]

MedChem Express

(E,E)-GLL398 [2077980-83-5]

9

2077980-83-5

Research Use Only

C25H23BO4

398.26

(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERalpha (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERalpha in MCF-7 breast cancer cells (IC50 = 0.21 microM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 microg h/mL in rats, which is significantly higher than that of GW7604[1].

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

12352200