生物活性 | |||
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靶点 |
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描述 | Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2[1]. In vitro, Onatasertib has capability to inhibit markers of mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] across a range of IC50 values: 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1, and 11 to 150 nM for pAKT(S473)][1]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
human PC3 cells | Function assay | 1 h | Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr, IC50=0.01 μM | 26083478 | |
human PC3 cells | Function assay | 1 h | Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr | 26083478 | |
human PC3 cells | Function assay | 1 h | Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr | 26083478 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.16mL 5.03mL 2.52mL |
参考文献 |
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