产品
编 号：F748071
分子式：C28H33F4N3O
分子量：503.57
分子式：C28H33F4N3O
分子量：503.57
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1953132-75-6
产品详情
生物活性：
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
体内研究：
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).Animal Model:Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor
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.
体外研究：
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.
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.
体内研究：
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).Animal Model:Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor
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.
体外研究：
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.
产品资料
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