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].

Product Specifications

CAS Number

[3035311-43-1]

UNSPSC

12352100

Target

Estrogen Receptor/ERR; Potassium Channel

Related Pathways

Membrane Transporter/Ion Channel; Vitamin D Related/Nuclear Receptor

Field of Research

Cancer

Smiles

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

Molecular Formula

C28H29F2NO3S

Molecular Weight

497.60

References & Citations

[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.