ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent druggability, can be used for HER+ breast cancer research[1].
ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells[1].
ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice[1].
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%[1].
| Animal Model: | MCF-7 human breast cancer xenograft model in nude mice[1] |
| Dosage: | 2 mg/kg; 6 mg/kg |
| Administration: | Oral administration; 2-6 mg/kg; QD; 21 days |
| Result: | Exhibited in vivo efficacy in breast cancer xenograft model. |
[1]. Xiaomeng Zhang, et al. Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer. J Med Chem