Gefitinib hydrochloride (ZD-1839 hydrochloride) is an orally active selective and potent tyrosine kinase (EGFR) inhibitor. Gefitinib hydrochloride exhibits antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, improves lung dysfunction, and inhibits inflammation. Gefitinib hydrochloride has antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, ameliorates lung dysfunction, and inhibits the progression of inflammation and fibrosis.

Calu3 (cells):2 μM, GLC82 cells:2 μM, non-transformed cells:20 nM

Gefitinib hydrochloride（0.01-0.1 mM）通过促使EGFRvIII二聚化，增加受体的磷酸酪氨酸负荷，增强ERK信号传导，并刺激细胞增殖及锚定独立生长，尤其是在长期暴露于EGFRvIII表达细胞时。相反，Gefitinib hydrochloride（1-2 mM）显著降低EGFRvIII的磷酸酪氨酸负荷，抑制EGFRvIII介导的增殖和锚定独立生长。[1]
Gefitinib hydrochloride 以IC50为20 nM抑制由EGF驱动的非转化细胞的单层生长。[2]
Gefitinib hydrochloride还可抑制CALU-3和GLC82细胞的增殖，IC50为2 μM。[3]

Gefitinib hydrochloride （150 mg/kg，口服）与二甲双胍联合使用显著抑制了H1299或CALU-3 GEF-R细胞在裸鼠皮下移植形成的肿瘤异种移植物的生长。[3]
在接受放射治疗的大鼠中，Gefitinib hydrochloride 的应用加剧了肺部的炎症反应，包括炎症细胞的浸润以及促炎因子的增加，而Gefitinib hydrochloride 通过抑制肺成纤维细胞的增殖起到了减缓肺部纤维化重塑的作用。[4]