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AZD8330
CAS No. : 869357-68-6
MCE 国际站:AZD8330
产品活性:AZD8330 (ARRY-424704) 是一种有效的非竞争性的 MEK1/MEK2 抑制剂,IC50 为 7 nM。
研究领域:MAPK/ERK Pathway
作用靶点:MEK
In Vitro: AZD8330 is a selective allosteric MEK1/ MEK2 inhibitor. Exposing human osteosarcoma cell lines MOS, U2OS, and 143B to a concentration of 0.5 μM of Trametinib, AZD8330 or TAK-733 for 6 hours, leads to loss of ERK phosphorylation indicating effective MEK inhibition.The activity of these three inhibitors is tested using concentration ranges in six osteosarcoma cell lines: MOS, U2OS, KPD, ZK58, 143b and Saos-2. All three inhibitors decrease viability of MOS and U2OS and strongly affect 143b. By contrast, viability of KPD, ZK58 and Saos-2 is not affected by any of the three inhibitors.
In Vivo: In tumour xenograft models, AZD8330 demonstrates dose-dependent tumour growth inhibition of approximately 90% at tolerated doses (1.0 mg/kg once daily [OD]).
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