ARQ092盐酸盐
| CAS号 | 1313883-00-9 | 货号 | BCP25709 |
| 中文名 | ARQ092盐酸盐 | ||
| 英文名 | Miransertib HCl | ||
| 中文别名 | Miransertib盐酸盐; | ||
| 英文别名 | Miransertib hydrochloride; ARQ092 HCl; ARQ-092 HCl; ARQ 092 HCl; | ||
| 分子式 | C27H25ClN6 | 分子量 | 468.99 |
| 生物活性 | Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma. | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | AKT | ||
结构式
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