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Proteins and Peptides

ER degrader 10

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HY-170377-1EACH
About this Product
SKU:
HY-170377
CAS Number:
3035311-43-1
Extra Details:
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].
Molecular Weight:
497.60
References:
[1]Zhang D, et al., Discovery of Thiochroman Derivatives as Potent, Oral Selective Estrogen Receptor Degraders and Antagonists for the Treatment of Endocrine-Resistant Breast Cancer. J Med Chem. 2024 Dec 12;67(23):21545-21567.
Research Area:
Cancer
Shipping Conditions:
Ambient
Type:
Proteins, Peptides, Small Molecules & Other Biomolecules: Small Molecules
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