产品
编 号:F382064
分子式:C18H18O3
分子量:282.33
产品类型
结构图
CAS No: 533884-09-2
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产品详情
生物活性:
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.
体内研究:
Erteberel (5?mg/Kg body weight/day, oral, 28 days) treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model.Erteberel (5?mg/Kg body weight/day, oral, 40-50 days) treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model.Animal Model:Athymic mice (5-7 weeks) inoculated with OVCAR-3 cells
Dosage:5mg/Kg body weight
Administration:Oral, daily for 28 days
Result:Immunohistochemical analysis reveals that Erteberel treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells.
体外研究:
Treatment with Erteberel (0.25-10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro. Erteberel promotes apoptosis of GBM cells. Erteberel modulated several pathways related to apoptosis, cell cycle, and DNA damage response. Erteberel (0-1000 μM) sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide.