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^[1].

497.60

C₂₈H₂₉F₂NO₃S

3035311-43-1

FC(C=C1)=CC(OC)=C1[C@H]2CSC3=CC(O)=CC=C3[C@H]2C4=CC=C(OCCN5CC(CF)C5)C=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]