ERα degrader-2 is a selective estrogen receptor degrader ( SERD ) with potent binding affinity with ERα ( IC 50 =17.1 nM), good degradation efficacy ( EC 50 =0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent druggability, can be used for HER + breast cancer research.

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.

2235396-63-9

C29H27F3N2O2

492.53

ERα degrader-2

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years