R162 性质
| 熔点 | 120-120.5 °C(Solv: acetone (67-64-1)) |
|---|---|
| 沸点 | 459.0±34.0 °C(Predicted) |
| 密度 | 1.308±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 可溶于DMSO（高达10mg/ml）或乙醇（高达5mg/ml） |
| 形态 | 固体 |
| 酸度系数(pKa) | 7.43±0.20(Predicted) |
| 颜色 | 橙色 |
| 稳定性 | 自购买之日起，稳定期为 1 年。 其DMSO 或乙醇溶液可在 -20°C 下保存长达 3 个月。 |
R162 用途与合成方法
Inhibition of GDH1 activity by R162 treatment results in decreased intracellular fumarate levels, attenuated GPx activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells, which can be significantly rescued by methyl-α-KG treatment as well as by antioxidant NAC. R162 inhibits cell proliferation and tumor growth potential of human cancer cells.
R162 (30 mg/kg/day, i.p.) does not result in a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties in xenograft tumor mouse models. R162 (20 mg/kg/day) results in significantly decreased tumor growth and masses in mice compared with control mice and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice.
