ER degrader 10 - CAS 3035311-43-1

ER degrader 10 (Compound 51) is an orally active estrogen receptor (ER) selective degrader and antagonist, with a DC50 of 0.43 nM and an IC50 of 0.56 nM. It inhibits the proliferation of ER-positive cells, with an IC50 ranging from 0 to 15 nM. ER degrader 10 exhibits weak inhibitory activity on the hERG channel, with an IC50 greater than 40 μM. It has blood-brain barrier permeability, with a brain/plasma ratio (Kp) of 3.05. In mouse models, ER degrader 10 demonstrates antitumor activity.

Estrogen Receptor/ERR, Potassium Channel

Endocrinology/Hormones, Membrane transporter/Ion channel

3035267

C28H29F2NO3S

497.597

O(C)C1=C([C@@H]2[C@@H](C=3C(SC2)=CC(O)=CC3)C4=CC=C(OCCN5CC(CF)C5)C=C4)C=CC(F)=C1

-20°C

Ice Packs

Small Compound