ARQ092盐酸盐

  • 化学数据
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
  • 用途
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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