4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
详情描述
GNE-502 是一种口服有效的雌激素受体 (ER) 降解剂。GNE-502 可用于乳腺癌研究。
产品详情
GNE-502 是一种口服有效的雌激素受体 (ER) 降解剂。GNE-502 可用于乳腺癌研究。
生物活性
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.
性状
Solid
IC50 & Target[1][2]
ER
体内研究(In Vivo)
GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model.
GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.
溶解度数据
In Vitro: DMSO : 100 mg/mL (212.05 mM; Need ultrasonic)配制储备液
[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.