HKI-357

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HKI-357  纯度: ≥99.0%

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。

HKI-357

HKI-357 Chemical Structure

CAS No. : 848133-17-5

规格 价格 是否有货
10 mg ￥9500 询问价格 & 货期

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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[1].

IC50 & Target[1]

EGFR

34 nM (IC50)

ErbB2

33 nM (IC50)

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].

Shanghai Jinpan Biotech Co Ltd 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.

Clinical Trial

分子量

574.05

Formula

C31H29ClFN5O3
CAS 号

848133-17-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70.

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