DC Chemicals · Product datasheet

Gefitinib (ZD1839) — Datasheet

CAT. NO. DC2103

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ParameterValue
Chemical NameGefitinib
CAS No.184475-35-2
SynonymsN-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine;GEFITINIB;AKOS 91371;n-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine;ZD 1839;4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-;Gefitinib(TINIBS);Gefitinib (ZD1839);Gefitinib (ZD1839, Iressa®);Iressa;N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; Irressat;ZD-1839;Gefinitib;Getfitnib;Gifitinib;Ji Fei Ji;Gefitinib WS;ZD1839;Gefitinib, >=99%;Gefitinib iMpurity;N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine;4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline;N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholiny
FormulaC22H24ClFN4O3
M.Wt446.9024
SMILESClC1=C(C([H])=C([H])C(=C1[H])N([H])C1C2C(=C([H])C(=C(C=2[H])OC([H])([H])C([H])([H])C([H])([H])N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])OC([H])([H])[H])N=C([H])N=1)F
Purity99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.

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[1]. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM[2]. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM[3].

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[3]. 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[4].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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