(E,E)-GLL398 is a selective estrogen receptor degrader that exhibits strong binding affinity for estrogen receptor alpha (ERα) with an IC50 of 1.14 nM. This compound is capable of effectively degrading ERα in MCF-7 breast cancer cells, demonstrating an IC50 of 0.21 μM. The incorporation of a boronic acid moiety enhances its oral bioavailability, achieving an AUC of 36.9 μg·h/mL in rat models, supporting its potential for therapeutic applications in hormone-dependent cancers.
(E,E)-GLL398 is a selective estrogen receptor degrader that exhibits strong binding affinity for estrogen receptor alpha (ERα) with an IC50 of 1.14 nM. This compound is capable of effectively degrading ERα in MCF-7 breast cancer cells, demonstrating an IC50 of 0.21 μM. The incorporation of a boronic acid moiety enhances its oral bioavailability, achieving an AUC of 36.9 μg·h/mL in rat models, supporting its potential for therapeutic applications in hormone-dependent cancers.
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