Gefitinib
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].
Product Specifications
CAS Number
[184475-35-2]
Product Name Alternative
ZD1839
UNSPSC
12352005
Hazard Statement
H302, H315, H318, H351, H360, H373, H401, H402, H410
Target
Apoptosis; Autophagy; EGFR
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Gefitinib.html
Purity
99.99
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F
Molecular Formula
C22H24ClFN4O3
Molecular Weight
446.90
Precautions
H302, H315, H318, H351, H360, H373, H401, H402, H410
References & Citations
[1]Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62 (20) :5749-54.|[2]Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93 (8) :915-23. |[3]Muhammad Tariq, et al. Gefitinib inhibits M2-like polarization of tumor-associated macrophages in Lewis lung cancer by targeting the STAT6 signaling pathway. Acta Pharmacol Sin. 2017 Nov;38 (11) :1501-1511. |[4]Mark S Cragg, et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med. 2007 Oct;4 (10) :1681-89; discussion 1690. |[5]Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122 (8) :1722-9. |[6]Tomoya Takenaka, et al. Effects of gefitinib treatment on cellular uptake of extracellular vesicles in EGFR-mutant non-small cell lung cancer cells. Int J Pharm. 2019 Dec 15;572:118762. |[7]Amin Li, et al. Gefitinib sensitization of cisplatin-resistant wild-type EGFR non-small cell lung cancer cells. J Cancer Res Clin Oncol. 2020 Jul;146 (7) :1737-1749.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
EGFR/ErbB1/HER1
Citation 01
AAPS PharmSciTech. 2022 Jan 4;23 (1) :48.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Adv Mater. 2025 May 22:e2504050.|Adv Ther. 2024 Jul 18.|Am J Transl Res. 2019 Jun 15;11 (6) :3543-3554.|Anticancer Res. 2020 Apr;40 (4) :1855-1866.|Aquaculture. 2021, 539: 736614.|Arch Toxicol. 2018 Jun;92 (6) :2027-2042.|Azhar Int J Pharm Med Sci. 2021;1 (1) :66-72.|Biochem Genet. 2025 May 23.|Biochem Pharmacol. 2025 Jun 6:239:117032.|Biochem Pharmacol. 2026 Jan;243 (Pt 2) :117562.|Biochim Biophys Acta Mol Basis Dis. 2023 Apr;1869 (4) :166665.|Biol Methods Protoc. 2025 Feb 13;10 (1) :bpaf012.|Biomaterials. 2022 Oct:289:121800.|Biomed Chromatogr. 2016 Jul;30 (7) :1150-4. |Biomed Pharmacother. 2019 Sep:117:109185.|Biomed Res Int. 2020 Dec 24:2020:8824805.|Bioorg Chem. 2025 Apr 15:160:108481.|Bioorg Chem. 2025 Aug 9:164:108864.|bioRxiv. 2024 Feb 12.|bioRxiv. 2024 July 26.|bioRxiv. 2024 June 12.|bioRxiv. 2024 May 31:2024.05.30.596676.|bioRxiv. 2024 October 24.|bioRxiv. 2024 October 29.|bioRxiv. 2025 Jul 12:2025.07.08.663754.|bioRxiv. 2025 Jun 24:2025.06.18.660406.|bioRxiv. 2025 Jun 7:2025.06.04.657911.|bioRxiv. 2025 May 10.|bioRxiv. 2025 Nov 26:2025.11.24.690135.|BMC Pulm Med. 2023 May 11;23 (1) :162.|Breast Cancer Res Treat. 2025 Jun;211 (2) :467-478.|Breast Cancer Res. 2017 Aug 4;19 (1) :90. |Cancer Cell Int. 2021 Dec 7;21 (1) :655.|Cancer Cell. 2018 Jun 11;33 (6) :1061-1077.e6. |Cancer Cell. 2025 Jul 25:S1535-6108 (25) 00310-1.|Cancer Lett. 2025 Apr 10:217715.|Cancer Manag Res. 2024 May 28:16:507-525.|Cancer Res Treat. 2023 Jul;55 (3) :778-803.|Cancer Res. 2023 Jul 5;83 (13) :2187-2207.|Cell Death Dis. 2018 Feb 15;9 (3) :269. |Cell Death Dis. 2020 Nov 11;11 (11) :969.|Cell Death Dis. 2023 Oct 11;14 (10) :671.|Cell Death Dis. 2019 May 1;10 (5) :361. |Cell Death Discov. 2023 Nov 2;9 (1) :406.|Cell Insight. 2022 Jun 16;1 (4) :100045.|Cell Mol Life Sci. 2019 May;76 (10) :2015-2030.|Cell Oncol (Dordr) . 2021 Feb;44 (1) :109-133.|Cell Oncol (Dordr) . 2025 Jul 10.|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Cell Rep Med. 2023 Sep 19;4 (9) :101177.|Cell Rep Med. 2025 Apr 2:102053.|Cell Rep Methods. 2023 Feb 21;3 (2) :100411.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.|Cell Rep. 2019 Jul 9;28 (2) :512-525.e6. |Cell Res. 2020 Oct;30 (10) :833-853. |Cell Res. 2021 Jun;31 (6) :631-648.|Cell Signal. 2024 Oct:122:111307.|Cell Syst. 2025 Mar 19;16 (3) :101203.|Chem Biol Interact. 2022 Feb 25:354:109798.|Chem Pharm Bull (Tokyo) . 2017 Aug 1;65 (8) :768-775.|Dev Cell. 2025 May 15:S1534-5807 (25) 00287-4.|Drug Dev Res. 2021 May;82 (3) :422-429.|Drug Discov Ther. 2025 Jan 14;18 (6) :387-390.|EBioMedicine. 2023 Jan:87:104410.|Endocrinology. 2023 Mar 13;164 (5) :bqad042.|Eur J Pharm Med Res. 2024, 11 (7), 136-153.|Eur J Pharmacol. 2021 Nov 5:910:174441.|Eur J Pharmacol. 2023 Dec 5:960:176114.|Exp Cell Res. 2017 Dec 15;361 (2) :246-256. |Exp Eye Res. 2024 Nov 14:110158.|FEBS Lett. 2021 Nov;595 (21) :2665-2674.|Fish Shellfish Immunol. 2020 Jul;102:211-217.|Food Biosci. 2025 Jul.|Food Nutr Res. 2018 Dec 6:62.|Front Endocrinol. 2018 Mar 22:9:120.|Front Microbiol. 2022 Jun 30;13:894356.|Front Oncol. 2020 Dec 23:10:597434.|Front Oncol. 2020 Oct 5;10:542007.|Front Oncol. 2022 Sep 8:12:944537.|Fundam Res. 2022 Mar 3;2 (5) :807-816.|Genes (Basel) . 2024 Dec 19;15 (12) :1624.|Genes Dis. 2025 Nov 25.|Haematologica. 2020 Jan;105 (1) :124-135. |Harvard Medical School LINCS LIBRARY|Indiana University. 2025.|Infect Immun. 2021 Jul 15;89 (8) :e0014121.|Int Immunopharmacol. 2025 Aug 25:164:115401.|Int J Biol Sci. 2021 Apr 12;17 (7) :1671-1681.|Int J Med Sci. 2022 May 13;19 (5) :878-892.|Int J Mol Sci. 2021 Feb 9;22 (4) :1745.|Int J Mol Sci. 2022 Feb 28;23 (5) :2664.|Int J Mol Sci. 2022 Feb 4;23 (3) :1785.|Int J Mol Sci. 2018 Oct 15;19 (10) . pii: E3165. |Int J Oncol. 2022 Nov;61 (5) :139.|J Anal Test. 2025 Sep 25.|J Biol Chem. 2022 Nov;298 (11) :102511.|J Cancer Res Clin Oncol. 2020 Jul;146 (7) :1737-1749.|J Cell Mol Med. 2020 May;24 (10) :5578-5592.|J Cell Mol Med. 2021 Jul;25 (13) :6280-6288.|J Cell Mol Med. 2021 Mar;25 (5) :2418-2425.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100.|J Control Release. 2024 Dec:376:829-841.|J Ethnopharmacol. 2023 Oct 5:314:116566.|J Exp Clin Cancer Res. 2019 Mar 15;38 (1) :129.|J Exp Clin Cancer Res. 2018 Nov 29;37 (1) :295.|J Exp Clin Cancer Res. 2019 Mar 15;38 (1) :129. |J Exp Med. 2022 Jan 3;219 (1) :e20210789.|J Funct Foods. 2025 Apr.|J Funct Foods. April 2022, 104997.|J Invest Dermatol. 2022 Feb;142 (2) :303-313.e9.|J Med Chem. 2025 Mar 13;68 (5) :5275-5291.|J Mol Biol. 2025 Jun 2:169261.|J Pharm Anal. 2024 Apr 25:100984.|J Sep Sci. 2017 Oct;40 (19) :3782-3791.|Kaohsiung J Med Sci. 2023 Jul;39 (7) :699-709.|Lung Cancer. 2023 Jul:181:107258.|Mol Cancer Res. 2019 Feb;17 (2) :499-507. |Mol Cancer Ther. 2023 Sep 5;22 (9) :1013-1027.|Mol Cancer. 2024 Jul 9;23 (1) :141.|Mol Cancer. 2025 Apr 23;24 (1) :122.|Mol Cell. 2025 Apr 3;85 (7) :1311-1329.e16.|Mol Med Rep. 2017 Sep;16 (3) :3475-3481.|Mol Pain. 2019 Jan-Dec:15:1744806919857297.|Mol Pharmacol. 2019 Dec;96 (6) :862-870.|Molecules. 2018 Mar 23;23 (4) . pii: E736.|Nat Biomed Eng. 2018 Aug;2 (8) :578-588.|Nat Commun. 2023 Apr 24;14 (1) :2342.|Nat Commun. 2023 Jun 15;14 (1) :3560.|Nat Commun. 2024 Jul 12;15 (1) :5874.|Nat Commun. 2024 Sep 10;15 (1) :7923.|Nat Commun. 2025 Feb 1;16 (1) :1237.|Nat Commun. 2019 Apr 18;10 (1) :1812|Nat Struct Mol Biol. 2024 May 20.|Neurobiol Dis. 2020 Aug;142:104961.|Oncogene. 2018 Aug;37 (31) :4300-4312. |Oncogene. 2021 Apr;40 (14) :2596-2609.|Oncogene. 2021 Jul;40 (30) :4884-4893.|Oncol Lett. 2022 Aug 24;24 (4) :356.|Oncol Lett. 2024 Jul 30;28 (4) :466.|Oncol Rep. 2018 Oct;40 (4) :2242-2250. |Oncol Rep. 2020 Aug;44 (2) :698-710.|Oncol Rep. 2023 May;49 (5) :84.|Oncotarget. 2015 Oct 13;6 (31) :31313-22. |Oncotarget. 2016 Oct 25;7 (43) :69760-69769.|Oncotarget. 2017 Dec 2;8 (68) :112313-112329.|Oxid Med Cell Longev. 2023 Jan 31:2023:1367938.|Pharmaceuticals (Basel) . 2022 Jun 2;15 (6) :698.|Pharmaceuticals (Basel) . 2024 May 14;17 (5) :626.|Pharmacol Res. 2019 Jun:144:79-89.|Phytomedicine. 2023 Jul 25:116:154884.|Phytomedicine. 2025 Oct 8:148:157387.|Phytomedicine. 2025 Oct:146:157098.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Princeton University. 2025.|Ren Fail. 2025 Dec;47 (1) :2490202.|Res Sq. 2023 Jun 15:rs.3.rs-3049913.|Res Sq. 2025 Jul 20.|Research Square Preprint. 2023 May 4.|Research Square Print. December 9th, 2022.|Research Square Print. October 18th, 2022.|Respir Res. 2024 May 20;25 (1) :215.|Sci Rep. 2024 Mar 27;14 (1) :7303.|Sci Rep. 2025 Jul 6;15 (1) :24100.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2021 Sep;13 (609) :eabb3738.|Signal Transduct Target Ther. 2019 Dec 13;4:60. |SSRN. 2025 Sep 25.|SSRN. 31 Aug 2021.|Stem Cell Reports. 2017 Dec 12;9 (6) :1948-1960.|Theranostics. 2018 Jul 30;8 (15) :4262-4278.|Transl Lung Cancer Res. 2024 Oct 31;13 (10) :2698-2712.|Transl Lung Cancer Res. 2025 Jun 30;14 (6) :2159-2179.|University of New York. 2025.|University of Otago. 2025 Oct 7.|Viruses. 2020 Aug 24;12 (9) :927.|Adv Healthc Mater. 2024 Nov 25:e2402884.|Oncotarget. 2017 Oct 19;8 (58) :98771-98781.
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