R162 是谷氨酸脱氢酶 (GDH1/GLUD1) 抑制剂,具有抗癌的活性。
产品描述
R162 is an effective glutamate dehydrogenase 1 (GDH1) inhibitor.
体外活性
R162 decreased intracellular fumarate levels attenuated GPx activity by inhibited GDH1 activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells. R162 inhibits tumor growth potential and cell proliferation of human cancer cells.
体内活性
In xenograft tumor mouse models, R162 (30 mg/kg/day, i.p.) does not cause a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties. Compared with control mice, R162 (20 mg/kg/day) markedly decreases tumor growth and masses and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice.
Cas No.
64302-87-0
分子式
C17H12O3
分子量
264.28
别名
R162
储存和溶解度
DMSO:100 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years