产品
编 号:F741617
分子式:C28H25N5O2S
分子量:495.6
产品类型
结构图
CAS No: 2469975-55-9
联系客服
产品详情
生物活性:
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
体内研究:
Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability.Animal Model:Nude mouse hepatoma HepG2 xenograft.
Dosage:10 and 20 mg/kg/day.
Administration:IP, once every day for 15 days.
Result:Lead to substantial suppression of tumor growth.The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.Exhibited almost no influence on the body weight of experimental mice.
体外研究:
Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line).Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner.Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis.Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete).