PKI-179
规格
| Cas Number | 1197160-28-3 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| Action Type | 抑制剂 |
| Mechanism Of Action | PI3 激酶 p110-α 亚基抑制剂 |
| 简短描述 | 一种有效的抗mTOR和PI 3-K抑制剂 |
| 英文简短描述 | a potent inhibitor against mTOR and PI 3-K |
| 过滤标签 | mTOR,PI3K,PI3K/Akt/mTOR |
| 储存温度 | 2-8°C储存 |
| 运输条件 | 冰袋运输 |
| 描述 |
PKI-179是一种细胞可渗透的三嗪基-苯基-吡啶基脲化合物，可作为抗mTOR（IC50 = 0.42 nM）和PI 3-K（IC50 = 8、24、74、77、14和11 nM的有效抑制剂）异构体α，β，γ，δ，αE545K突变体和αH1047R突变体）的活性，对361种其他激酶（IC50> 50 µM），细胞色素CYP亚型或hERG的活性降低或降低。据报道，由于Akt / mTOR途径的抑制，PKI-179可通过凋亡诱导有效地抑制体外培养物中癌症的生长（分别针对MDA361和PC3mm2，IC50分别 |
| 英文描述 |
PKI-179 is a cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC50 = 0.42 nM) and PI 3-K (IC50 = 8, 24, 74, 77, 14, and 11 nM against isoform α, β, γ, δ, α E545K mutant, and α H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC50 >50 μM), Cytochrome CYP isoforms, or hERG. PKI-179 is reported to effectively suppress cancer growth in cultures in vitro (IC50 = 22 and 29 nM, respectively, against MDA361 and PC3mm2) via apoptosis induction as a result of Akt/mTOR pathway inhibition. |