Gefitinib

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

一种有效的、选择性的、口服活性的 EGFR 抑制剂，IC50 为 23 nM；抑制 EGF 刺激的 KB 细胞增殖，IC50 为 80 nM。

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM; inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM; blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM; significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth; has been used to treat advanced (or recurrent) non-small cell lung cancer.Lung Cancer Approved(In Vitro):Gefitinib (0.01-0.1? μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth.Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.Gefitinib (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 (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration.Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells).Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells.Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines).(In Vivo):Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model.Gefitinib (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 (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358R xenograft.

Gefitinib (GMP) abolishes the effect of EGF-induced dedifferentiation of astrocytes into astrocyte precursor cells (APCs).Gefitinib (3 μM) can produce a subgroup of EGFR-mutant NSCLC cell lines (Gefitinib-resistant cells) that undergo cellular reprogramming, such as HCC827 cells.

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ZD-1839

Angiogenesis

EGFR

Tyr1173 (NR6W cells)| Tyr1173 (NR6wtEGFR cells)| Tyr992 (NR6W cells)| Tyr992 (NR6wtEGFR cells)

Cancer

Lung Cancer

184475-35-2

446.9024

C22H24ClFN4O3

>98% (HPLC)

DMSO: ≥ 30 mg/mL

COC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4

4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-

(-20℃)

With Ice Pack

≥ 2 years