GNE-149,1953132-75-6

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GNE-149

CAS No. : 1953132-75-6

MCE 国际站：GNE-149

产品活性：GNE-149 是一种有效的，具有口服活性的雌激素受体 α (ERα; IC₅₀=0.053 nM) 拮抗剂。GNE-149 也是一种选择性的雌激素受体降解剂 (SERD)。GNE-149 可用于乳腺癌的研究。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

In Vitro: GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC₅₀s of 0.66 and 0.69 nM, respectively.
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC₅₀s of 0.053 and 0.031 nM, respectively.

In Vivo: GNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant.
GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno).

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