2077980-83-5
Chemical Structure
(E,E)-GLL398
- CAS No.: 2077980-83-5
- Formula:C25H23BO4
- Molecular Weight:398.26
IUPAC Name: (E)-3-(4-((E)-1-(4-boronophenyl)-2-phenylbut-1-en-1-yl)phenyl)acrylic acid
InChIKey: BINZFDGAOTWQNC-VZBZSUMNSA-N
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
Biological Activity: (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].
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(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. | |||||||||||||||||||||
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