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Gefitinib hydrochloride

CAS No. : 184475-55-6

MCE 站：Gefitinib hydrochloride

产品活性：Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效，选择性和口服活性的 EGFR 酪氨酸激酶抑制剂，IC₅₀ 为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC₅₀ 为 54 nM)，并阻断 EGF 刺激的肿瘤细胞中 EGFR 自磷酸化。Gefitinib hydrochloride 还可诱导细胞自噬 (autophagy)，并具有抗肿瘤活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC₅₀ of 20 nM. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC₅₀ of 2 μM.

In Vivo: Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation.

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