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Gefitinib dihydrochloride

CAS No. : 184475-56-7

MCE 站：Gefitinib dihydrochloride

产品活性：Gefitinib dihydrochloride (ZD 1839 dihydrochloride) 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 dihydrochloride 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 dihydrochloride还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，可用于癌症相关的研究，如肺癌和乳腺癌。

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

作用靶点：EGFR  |  Autophagy  |  Apoptosis

In Vitro: Gefitinib dihydrochloride (0.010.1 μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK ａnd stimulation of proliferation ａnd anchorage-independent growth.
Gefitinib dihydrochloride (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation ａnd anchorage-independent growth.
Gefitinib dihydrochloride (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway.
Gefitinib dihydrochloride (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion ａnd migration.
Gefitinib dihydrochloride (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 ａnd HCC827 cells).
Gefitinib dihydrochloride (100 nM, 24 h) suppresses macropinocytosis ａnd increases the cellular uptake of extracellular vesicles( EVs) in HCC827 ａnd A549 cells.
Gefitinib dihydrochloride (1.5-60 μM, 48 h) increases inhibition of proliferation in H358^R ａnd A549^R cells (Cisplatin-resistant wtEGFR NSCLC cell lines).

In Vivo: Gefitinib dihydrochloride (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model.
Gefitinib dihydrochloride (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 ａnd HER3 ａnd signaling through MAPK ａnd Akt in lobular hyperplasias ａnd carcinomas, increases MAPK activity ａnd cytokine production in splenocytes ａnd lymph nodes.
Gefitinib dihydrochloride (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358^R xenograft.

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