HKI-357 是 EGFR 和 ERBB2 的不可逆双重抑制剂，IC50 分别为 34 nM 和 33 nM。HKI-357 抑制 EGFR 自磷酸化 (检测位点为 Y1068)，及 AKT 和 MAPK 磷酸化。
| 生物活性 |
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation. |
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| 体外研究 |
HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells. Western Blot Analysis
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| 分子式 |
C31H29N5O3FCl
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| 分子量 |
574.05
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| CAS号 |
848133-17-5
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 临床试验 |
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纯度： 98%
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