ER Degrader 10 is a selective orally active degrader and antagonist of the estrogen receptor (ER), demonstrating a DC50 of 0.43 nM and an IC50 of 0.56 nM. This compound effectively inhibits the proliferation of ER-positive cancer cells, with IC50 values ranging from 0 to 15 nM. While it shows minimal inhibitory activity against the hERG channel (IC50 > 40 μM), ER Degrader 10 is capable of crossing the blood-brain barrier, with a brain/plasma ratio of 3.05. Additionally, it has demonstrated significant antitumor efficacy in mouse models, making it a valuable tool for cancer research.
ER Degrader 10 is a selective orally active degrader and antagonist of the estrogen receptor (ER), demonstrating a DC50 of 0.43 nM and an IC50 of 0.56 nM. This compound effectively inhibits the proliferation of ER-positive cancer cells, with IC50 values ranging from 0 to 15 nM. While it shows minimal inhibitory activity against the hERG channel (IC50 > 40 μM), ER Degrader 10 is capable of crossing the blood-brain barrier, with a brain/plasma ratio of 3.05. Additionally, it has demonstrated significant antitumor efficacy in mouse models, making it a valuable tool for cancer research.
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