| Bioactivity | 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 treatment of breast cancer[1]. |
| Invitro | 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]. Cell Cytotoxicity Assay Cell Line: |
| Name | ERα degrader 4 |
| Formula | C42H58O8 |
| Molar Mass | 690.91 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |