ERα degrader 13

ERα degrader 13 (MR3) (incubated for 2 h) binds to purified ERα protein, with a K_d value of 27.1 nM and a binding affinity relative to raloxifene of 9.1%^[1].
ERα degrader 13 (5 μM; 0-5 min irradiation at 660 nm, intensity = 0.4 W/cm²) generates ROS in a cell-free system under 660 nm light irradiation^[1].
ERα degrader 13 (1.0 μM; 6 h pre-incubation, 1-4 min 660 nm irradiation at 0.4 W/cm²) induces a time-dependent increase in intracellular ROS levels in MCF7 cells under 660 nm irradiation^[1].
ERα degrader 13 (0.1-50.0 μM; 6 h plus 0-72 h incubation, dark or 1-5 min 660 nm irradiation at 0.4 W/cm²) induces concentration- and time-dependent ERα degradation in MCF7 cells only when combined with 660 nm irradiation; this degradation process is mediated by the proteasome system and ROS^[1].
ERα degrader 13 inhibits the proliferation of MCF7 breast cancer cells, with an IC₅₀ of 25.1 μM under light-protected conditions; its activity increases 45-fold (IC₅₀ = 0.55 μM) after 1 min of irradiation with 660 nm light, and the efficacy is further enhanced with prolonged irradiation time; it shows almost no toxicity to MCF10A normal mammary epithelial cells, with an IC₅₀ > 100 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.