GNE-149

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GNE-149

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1953132-75-6

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。

生物活性

GNE-149 is an orally bioavailable full antagonist ofestrogen receptorα(ERα;IC₅₀=0.053 nM). GNE-149 is a selectiveestrogen receptordegrader (SERD). GNE-149 can be used for the research of breastcancer^[1].

IC₅₀& Target^[1]

ERα

0.053 nM (IC₅₀)

体外研究
(In Vitro)

GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC₅₀s of 0.66 and 0.69 nM, respectively^[1].
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC₅₀s of 0.053 and 0.031 nM, respectively^[1].

体内研究
(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^[1].
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)^[1].

Animal Model:	Female Crl:NU Foxn1^numice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor^[1]
Dosage:	0.3, 1, 3, 10, and 30 mg/kg
Administration:	Orally q.d. for 21 days
Result:	Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.

分子量

503.57

Formula

C₂₈H₃₃F₄N₃O

CAS 号

1953132-75-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.