3035311-43-1
Chemical Structure
ER degrader 10
- CAS No.: 3035311-43-1
- Formula:C28H29F2NO3S
- Molecular Weight:497.60
InChIKey: BKDGYCGJTOTOOY-LEAFIULHSA-N
SMILES: FC(C=C1)=CC(OC)=C1[C@H]2CSC3=CC(O)=CC=C3[C@H]2C4=CC=C(OCCN5CC(CF)C5)C=C4
Biological Activity: ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model[1].
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ER degrader 10 | ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model. | |||||||||||||||||||||
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Keywords
