| Description | Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies. |
| In vitro | Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC 50 s of 0.3. 6.0, 2.2 nM, respectively[1]. Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC 50 s of 0.3. 19.6, 12.7 nM, respectively[1]. Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1]. |
| In vivo | Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft[1].Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose[1]： T max (h) C max (ng/mL) AUC last (hr× ng/mL) AUC inf_obs (hr×ng/mL) T 1/2 (h) 4.00 343 7582 9804 26 Animal Model: Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft[1]Dosage: 50mg/kg Administration: p.o. for 28 days Result: Showed 56% tumor growth inhibition compared to vehicle group after 28 days. |
| molecular weight | 477.527 |
| Molecular formula | C29H26F3NO2 |
| CAS | 2505067-70-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Ranjan Kumar Pal, et al, Selective estrogen receptor degrader. WO2021014386 A1. 2. WHO Drug Information, Vol. 35, No. 4, 2021. Geneva: World Health Organization; 2022. |