Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-149 is an orally bioavailable compound that acts as a full antagonist of estrogen receptor α (ERα) with an IC50 of 0.053 nM. It is also classified as a selective estrogen receptor degrader (SERD). GNE-149 holds potential for research in the field of breast cancer.
产品描述 | GNE-149 is an orally bioavailable compound that acts as a full antagonist of estrogen receptor α (ERα) with an IC50 of 0.053 nM. It is also classified as a selective estrogen receptor degrader (SERD). GNE-149 holds potential for research in the field of breast cancer. |
靶点活性 | ERα:0.053 nM (IC50) |
体外活性 | GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC 50 s of 0.66 and 0.69 nM, respectively[1]. GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC 50 s of 0.053 and 0.031 nM, respectively[1]. |
体内活性 | 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 nu mice (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 | 503.586 |
分子式 | C28H33F4N3O |
CAS No. | 1953132-75-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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