HKI-357

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HKI-357 是一种不可逆的 EGFR 和 ERBB2 双重抑制剂（IC50：34 nM 和 33 nM）。 HKI-357 抑制 EGFR 自身磷酸化（位于 Y1068）以及 AKT 和 MAPK 磷酸化。

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.(In Vitro):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. 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.

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.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. Western Blot Analysis 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.

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Angiogenesis

EGFR

PEGs

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848133-17-5

574.05

C31H29ClFN5O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (174.20 mM)

CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C

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(-20℃)

With Ice Pack

≥ 2 years