| Bioactivity | Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5]. | ||||||||||||
| Invitro | 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[2].Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[2].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[3].Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration[3].Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)[4].Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells[6].Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines)[7]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| Name | Gefitinib | ||||||||||||
| CAS | 184475-35-2 | ||||||||||||
| Formula | C22H24ClFN4O3 | ||||||||||||
| Molar Mass | 446.90 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Gefitinib
CAS: 184475-35-2 F: C22H24ClFN4O3 W: 446.90
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefiti
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