Molecular Formula | C16H17FIN3O4 |
Molar Mass | 461.23 |
Density | 1.732 |
Storage Condition | -20℃ |
In vitro study | AZD8330 can effectively inhibit MEK 1/2. In the pERK system AZD8330 can achieve ultra-micromolar potency in MEK 1/2 inhibitor-sensitive cell line function (amplification) in the experiment, the effectiveness of the low to the micro Molar level can be achieved. The MEK inhibitor AZD8330 specifically inhibits mitogen-activated protein kinase kinase 1(MEK or MAP/ERK kinase 1), inhibition of growth factor-regulated cell signaling processes and inhibition of tumor cell proliferation. |
In vivo study | In the Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model, a single oral dose of 1.25 mg/kg of AZD8330, the phosphorylation of ERK can be inhibited by more than 90% in 4 to 8 hours. In the transplanted tumor model of nude mice Calu-6, the once-daily dose of 0.4 mg/kg could completely inhibit the tumor growth by more than 80%. In the Calu-6 model, AZD8330 inhibited tumor growth in a dose-dependent manner at 0.3 mg/kg and 1.0 mg/kg once daily. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.168 ml | 10.841 ml | 21.681 ml |
5 mM | 0.434 ml | 2.168 ml | 4.336 ml |
10 mM | 0.217 ml | 1.084 ml | 2.168 ml |
5 mM | 0.043 ml | 0.217 ml | 0.434 ml |