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Gefitinib (ZD1839)

  Cat. No.:  DC2103   Featured
Chemical Structure
184475-35-2
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Field of application
Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 184475-35-2
Chemical Name: Gefitinib
Synonyms: N-(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
SMILES: ClC1=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
Formula: C22H24ClFN4O3
M.Wt: 446.9024
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC1091 PF-299804 (Dacomitinib,PF-00299804) PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.
DC7225 Pelitinib (EKB-569; WAY-EKB 569) Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.
DC11900 Lazertinib Lazertinib (YH25448, GNS-1480) is a highly potent, mutant-selective, irreversible, brain-penetrant and orally active EGFR tyrosine-kinase inhibitors for both the T790M mutation and activating EGFR mutations
DC2103 Gefitinib (ZD1839) Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
DC3139 Erlotinib hydrochloride Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.
DC2101 Erlotinib free base Erlotinib (OSI-744; NSC 718781; R1415) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
DC7106 Rociletinib (CO-1686) CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM).
DC3138 Canertinib dihydrochloride Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
DC8462 AZD-9291 mesylate (Osimertinib，Mereletinib) AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).
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