ERα degrader 4 

ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC₅₀ of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer^[1].

IC₅₀: 0.31 μM (ERα) in MDA-MB-231, 0.41 μM (ERα) in MCF-7, 0.48 μM (ERα) in MCF-7/ADR^[1]

ERα degrader 4 (compound 16a) (0-10 μM; 48 hours) has the high activity (IC₅₀: 0.31-0.48 μM) against all tested cancer cell lines^[1].
ERα degrader 4 (1 μM; 24 hours) increases ERα degradation and relative binding affinity in MCF-7 cancer cells^[1].
ERα degrader 4 (0.5, 1 and 2 μM; 24 hours) decreases the number and size of MCF-7 cells colonies at 0.5 μM, and completely suppresses colony formation with 2 μM^[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) increases the early-stage apoptosis of MCF-7 cells with a dose-dependent manner^[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) can induce the accumulation of reactive oxygen species (ROS) which contributes to the apoptosis of MCF-7 cells^[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) induces apoptosis in MCF-7 cancer cells by decreasing the mitochondrial membrane potential^[1].

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

690.91

C₄₂H₅₈O₈

[H][C@]12C[C@]3(CC[C@]([C@H](/C=C\C=C/C(OCCOCCOCCOC(CC45CC6CC(C5)CC(C6)C4)=O)=O)C)([C@@]3(C/C=C([C@@]1(C(C=C2C)=O)[H])/C=O)[H])[H])C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Liang JJ, et al. Design and synthesis of marine sesterterpene analogues as novel estrogen receptor α degraders for breast cancer treatment. Eur J Med Chem. 2022;229:114081.  [Content Brief]