1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. HKI-357 dimaleate

HKI-357 dimaleate是 EGFRERBB2 的不可逆双重抑制剂,IC50 分别为 34 nM 和 33 nM。HKI-357 dimaleate 抑制 EGFR 自磷酸化 (检测位点为 Y1068),及 AKT 和 MAPK 磷酸化。

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HKI-357 dimaleate Chemical Structure

HKI-357 dimaleate Chemical Structure

CAS No. : 915942-25-5

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HKI-357 dimaleate 的其他形式现货产品:

Other Forms of HKI-357 dimaleate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1].

体外研究
(In Vitro)

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[1].
HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NCI-H1975 bronchoalveolar cell line
Concentration: 0.01, 0.01, 0.1, 1 and 10 μM
Incubation Time:
Result: Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation.
分子量

806.19

Formula

C39H37ClFN5O11

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HKI-357 dimaleate
目录号:
HY-103443A
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