Gefitinib hydrochloride
Based on 206 publication(s) in Google Scholar
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.77%
- CAS No.: 184475-55-6
- 화학식: C22H25Cl2FN4O3
- 분자량:483.36
-
보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Gefitinib hydrochloride
More- Signal Transduct Target Ther. 2019 Dec 13;4:60. [Abstract]
- Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]
- Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. [Abstract]
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- Cell Res. 2021 Jun;31(6):631-648. [Abstract]
- Cell Res. 2020 Oct;30(10):833-853. [Abstract]
- Mol Cell. 2025 Mar 21:S1097-2765(25)00194-7. [Abstract]
- Cancer Res. 2023 Jul 5;83(13):2187-2207. [Abstract]
- Nat Commun. 2026 Jan 21;17(1):1902. [Abstract]
- Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]
- Nat Commun. 2024 Sep 10;15(1):7923. [Abstract]
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- Nat Commun. 2023 Jun 15;14(1):3560. [Abstract]
- Nat Commun. 2023 Apr 24;14(1):2342. [Abstract]
- Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
- Sci Transl Med. 2021 Sep;13(609):eabb3738. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
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- J Exp Clin Cancer Res. 2019 Mar 15;38(1):129. [Abstract]
- J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. [Abstract]
- Redox Biol. 2026 Apr:91:104093. [Abstract]
- J Control Release. 2024 Dec:376:829-841. [Abstract]
- EBioMedicine. 2023 Jan:87:104410. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cell Rep Med. 2023 Sep 19;4(9):101177. [Abstract]
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- J Exp Med. 2022 Jan 3;219(1):e20210789. [Abstract]
- Pharmacol Res. 2019 Jun:144:79-89. [Abstract]
- Cancer Lett. 2025 Apr 10:217715. [Abstract]
- Nat Struct Mol Biol. 2024 May 20. [Abstract]
- Int J Biol Sci. 2021 Apr 12;17(7):1671-1681. [Abstract]
- Adv Healthc Mater. 2024 Nov 25:e2402884. [Abstract]
- Cell Death Dis. 2023 Oct 11;14(10):671. [Abstract]
- Cell Death Dis. 2020 Nov 11;11(11):969. [Abstract]
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- Sci Rep. 2025 Jul 6;15(1):24100. [Abstract]
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- J Biol Chem. 2022 Nov;298(11):102511. [Abstract]
- Oncol Rep. 2020 Aug;44(2):698-710. [Abstract]
- Fish Shellfish Immunol. 2020 Jul;102:211-217. [Abstract]
- Oncol Rep. 2018 Oct;40(4):2242-2250. [Abstract]
- Cancer Res Treat. 2023 Jul;55(3):778-803. [Abstract]
- Cell Signal. 2024 Oct:122:111307. [Abstract]
- Mol Med Rep. 2026 Feb;33(2):77. [Abstract]
- Transl Lung Cancer Res. 2025 Jun 30;14(6):2159-2179. [Abstract]
- Transl Lung Cancer Res. 2024 Oct 31;13(10):2698-2712. [Abstract]
- Viruses. 2020 Aug 24;12(9):927. [Abstract]
- Exp Cell Res. 2017 Dec 15;361(2):246-256. [Abstract]
- Mol Med Rep. 2017 Sep;16(3):3475-3481. [Abstract]
- Toxicol Appl Pharmacol. 2026 Mar 4:511:117777. [Abstract]
- Food Nutr Res. 2018 Dec 6:62. [Abstract]
- Endocrinology. 2023 Mar 13;164(5):bqad042. [Abstract]
- Front Oncol. 2022 Sep 8:12:944537. [Abstract]
- Front Oncol. 2020 Dec 23:10:597434. [Abstract]
- Front Oncol. 2020 Oct 5;10:542007. [Abstract]
- Int J Med Sci. 2022 May 13;19(5):878-892. [Abstract]
- Kaohsiung J Med Sci. 2023 Jul;39(7):699-709. [Abstract]
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- Breast Cancer Res Treat. 2025 Jun;211(2):467-478. [Abstract]
- FEBS Lett. 2021 Nov;595(21):2665-2674. [Abstract]
- Mol Pharmacol. 2019 Dec;96(6):862-870. [Abstract]
- Genes (Basel). 2024 Dec 19;15(12):1624. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
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- Infect Immun. 2021 Jul 15;89(8):e0014121. [Abstract]
- J Cancer Res Clin Oncol. 2020 Jul;146(7):1737-1749. [Abstract]
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Cell Proliferation/Viability Assay
-
WB
-
IF
-
WB
-
WB
All EGFR Isoforms
More
Biological Activity
|
EGFR |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 184475-55-6
-
Appearance Solid
-
분자량 483.36
-
화학식 C22H25Cl2FN4O3
-
Color White to off-white
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SMILES
ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F.[H]Cl
-
Synonyms
ZD-1839 hydrochloride
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (206)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
TGIF2 promotes the progression of lung adenocarcinoma by bridging EGFR/RAS/ERK signaling to cancer cell stemness. [Abstract]2019 Dec 13;4:60. PMID: 31871777 -
Cancer Cell
A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213 -
Cancer Cell
Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. [Abstract]2018 Jun 11;33(6):1061-1077.e6. PMID: 29894692
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. [Abstract]
WT mice are either treated with vehicle or Gefitinib (100 mg/kg/day) starting one day prior to DEN injection (100 mg/kg). Livers are collected at 3 and 48 hr after DEN injection and subjected to IB analyses with the indicated antibodies.
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Cell
ErbB family receptor dimerization dynamics and dysregulation via long-term single-molecule imaging. [Abstract]2026 May 28;189(11):3413-3431.e19. PMID: 42054992 -
Mol Cancer
LSD1 inhibition attenuates targeted therapy-induced lineage plasticity in BRAF mutant colorectal cancer. [Abstract]2025 Apr 23;24(1):122. PMID: 40264166 -
Mol Cancer
A positive feedback loop between PFKP and c-Myc drives head and neck squamous cell carcinoma progression. [Abstract]2024 Jul 9;23(1):141. PMID: 38982480 -
Adv Mater
Highly Specific Cytokine Receptor-Targeting Chimeras for Targeted Membrane Protein Degradation and Sensitization of Osimertinib in EGFR-Mutated Non-Small-Cell Lung Cancer. [Abstract]2025 May 22:e2504050. PMID: 40401615 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Cell Res
2021 Jun;31(6):631-648. PMID: 33782530 -
Cell Res
Three-dimensional bioprinted glioblastoma microenvironments model cellular dependencies and immune interactions. [Abstract]2020 Oct;30(10):833-853. PMID: 32499560
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Res. 2020 Oct;30(10):833-853. [Abstract]
Western blot showing EGFR phosphorylation (Y1173 and Y1068) as a biomarker of EGFR activation following treatment with erlotinib or gefitinib (0.2-1 μM) for 24 hours in sphere culture at the indicated concentrations.
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Res. 2020 Oct;30(10):833-853. [Abstract]
Immunofluorescence showing phospho-EGFR (Y1173) expression in GSCs in 3D tetracultures following treatment with 1μM of erlotinib or gefitinib for 24 hours. Scale bar, 25μm.
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Mol Cell
Amplified dosage of the NKX2-1 lineage transcription factor controls its oncogenic role in lung adenocarcinoma. [Abstract]2025 Mar 21:S1097-2765(25)00194-7. PMID: 40139189 -
Cancer Res
Metabolic reprogramming driven by IGF2BP3 promotes acquired resistance to EGFR inhibitors in non-small cell lung cancer. [Abstract]2023 Jul 5;83(13):2187-2207. PMID: 37061993 -
Nat Commun
An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]2026 Jan 21;17(1):1902. PMID: 41565660 -
Nat Commun
PPARα-mediated lipid metabolism reprogramming supports anti-EGFR therapy resistance in head and neck squamous cell carcinoma. [Abstract]2025 Feb 1;16(1):1237. PMID: 39890801 -
Nat Commun
2024 Sep 10;15(1):7923. PMID: 39256387 -
Nat Commun
Therapeutic potential of the secreted Kazal-type serine protease inhibitor SPINK4 in colitis. [Abstract]2024 Jul 12;15(1):5874. PMID: 38997284 -
Nat Commun
CNK2 promotes cancer cell motility by mediating ARF6 activation downstream of AXL signalling. [Abstract]2023 Jun 15;14(1):3560. PMID: 37322019 -
Nat Commun
TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. [Abstract]2023 Apr 24;14(1):2342. PMID: 37095176 -
Nat Commun
AURKB as a target in non-small cell lung cancer with acquired resistance to anti-EGFR therapy. [Abstract]2019 Apr 18;10(1):1812 PMID: 31000705 -
Sci Transl Med
Oncogenic switch and single-agent MET inhibitor sensitivity in a subset of EGFR-mutant lung cancer. [Abstract]2021 Sep;13(609):eabb3738. PMID: 34516823 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
2026 Feb 3:e16660. PMID: 41632021 -
Adv Sci (Weinh)
Real-Time Visualization of Isoform-Specific RAF-KRAS Interactions in Living Cells Using FRET-BRET Hybrid Biosensors. [Abstract]2026 Feb 12:e15654. PMID: 41674298 -
Theranostics
Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]2018 Jul 30;8(15):4262-4278. PMID: 30128052
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]
BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefitinib at 2.5 µM, SU 11248 at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.
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Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
J Exp Clin Cancer Res
Co-administration of 20(S)-protopanaxatriol (g-PPT) and EGFR-TKI overcomes EGFR-TKI resistance by decreasing SCD1 induced lipid accumulation in non-small cell lung cancer. [Abstract]2019 Mar 15;38(1):129. PMID: 30876460 -
J Exp Clin Cancer Res
GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. [Abstract]2018 Nov 29;37(1):295. PMID: 30497501 -
Redox Biol
PP4 modulates macrophage-neutrophil crosstalk to restrict CCL5 -driven NETosis in sepsis. [Abstract]2026 Apr:91:104093. PMID: 41723906 -
J Control Release
Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment. [Abstract]2024 Dec:376:829-841. PMID: 39491626 -
EBioMedicine
Immunological profiles of human oligodendrogliomas define two distinct molecular subtypes. [Abstract]2023 Jan:87:104410. PMID: 36525723 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cell Rep Med
Tumor-associated monocytes promote mesenchymal transformation through EGFR signaling in glioma. [Abstract]2023 Sep 19;4(9):101177. PMID: 37652019 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
J Exp Med
2022 Jan 3;219(1):e20210789. PMID: 34825915 -
Pharmacol Res
Cordycepin Inhibits Drug-resistance Non-small Cell Lung Cancer Progression by Activating AMPK Signaling Pathway. [Abstract]2019 Jun:144:79-89. PMID: 30974169 -
Cancer Lett
2025 Apr 10:217715. PMID: 40220852 -
Nat Struct Mol Biol
RNAi screens identify HES4 as a regulator of redox balance supporting pyrimidine synthesis and tumor growth. [Abstract]2024 May 20. PMID: 38769389 -
Int J Biol Sci
MUC3A induces PD-L1 and reduces tyrosine kinase inhibitors effects in EGFR-mutant non-small cell lung cancer. [Abstract]2021 Apr 12;17(7):1671-1681. PMID: 33994852 -
Adv Healthc Mater
Antitumor Activity of a Bispecific Chimera Targeting EGFR and Met in Gefitinib-Resistant Non-Small Cell Lung Cancer. [Abstract]2024 Nov 25:e2402884. PMID: 39586988 -
Cell Death Dis
PTPN23 ubiquitination by WDR4 suppresses EGFR and c-MET degradation to define a lung cancer therapeutic target. [Abstract]2023 Oct 11;14(10):671. PMID: 37821451 -
Cell Death Dis
The mechanism of m6A methyltransferase METTL3-mediated autophagy in reversing gefitinib resistance in NSCLC cells by β-elemene. [Abstract]2020 Nov 11;11(11):969. PMID: 33177491 -
Cell Death Dis
AXL degradation in combination with EGFR-TKI can delay and overcome acquired resistance in human non-small cell lung cancer cells. [Abstract]2019 May 1;10(5):361. PMID: 31043587 -
Cell Death Dis
EGFR-PI3K-PDK1 pathway regulates YAP signaling in hepatocellular carcinoma: the mechanism and its implications in targeted therapy. [Abstract]2018 Feb 15;9(3):269. PMID: 29449645
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269. [Abstract]
WB is used to detect the effect of EGF treatment for 4 h on the expression of YAP with the inhibitors of EGFR or its downsream members, including Gefitinib, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, GSK1120212, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.
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J Pharm Anal
Increasing the tumour targeting of antitumour drugs through anlotinib-mediated modulation of the extracellular matrix and the RhoA/ROCK signalling pathway. [Abstract]2024 Aug;14(8):100984. PMID: 39258171 -
Dev Cell
Stress-induced pro-inflammatory glioblastoma stem cells secrete TNFAIP6 to enhance tumor growth and induce suppressive macrophages. [Abstract]2025 May 15:S1534-5807(25)00287-4. PMID: 40403724 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
Phytomedicine
Paeoniflorin alleviates anxiety-like behaviors in sleep-deprived male mice by suppressing inflammation of the paraventricular nucleus of the hypothalamus. [Abstract]2026 Jun:155:158111. PMID: 41931995 -
Phytomedicine
Yifei Sanjie pill combined with gefitinib reduces the progression of EGFR-TKIs-resistant non-small cell lung cancer via YAP/ANKRD1 axis. [Abstract]2026 Jun:155:158003. PMID: 41865688 -
Phytomedicine
Tougu Xiaotong capsules inhibit lung cancer and gefitinib-resistant cells by blocking ERBB2/PI3K-AKT-mTOR signaling and triggering ferroptosis. [Abstract]2025 Dec 26:150:157741. PMID: 41477979 -
Phytomedicine
Breviscapine targets EGFR and SRC to abrogate diabetes-driven GPX4 lactylation and ferroptosis resistance in gastric cancer. [Abstract]2025 Oct 8:148:157387. PMID: 41106095 -
Phytomedicine
Flemiphilippinin A induces paraptosis in lung cancer cells via c-Myc-driven endoplasmic reticulum stress and CHOP-mediated mitochondrial dysfunction. [Abstract]2025 Oct:146:157098. PMID: 40716126 -
Phytomedicine
Pedunculoside inhibits epithelial-mesenchymal transition and overcomes Gefitinib-resistant non-small cell lung cancer through regulating MAPK and Nrf2 pathways. [Abstract]2023 Jul 25:116:154884. PMID: 37209605 -
NPJ Precis Oncol
High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]2026 Apr 8;10(1):211. PMID: 41951768 -
Haematologica
2020 Jan;105(1):124-135. PMID: 30948489 -
Cell Syst
Large-scale control over collective cell migration using light-activated epidermal growth factor receptors. [Abstract]2025 Mar 19;16(3):101203. PMID: 40037348 -
Biomed Pharmacother
Enhancement of chemosensitivity by WEE1 inhibition in EGFR-TKIs resistant non-small cell lung cancer. [Abstract]2019 Sep:117:109185. PMID: 31387179 -
Oncogene
Amphiregulin drives EGFR-dependent genome stability in colorectal cancer and represents a targetable vulnerability. [Abstract]2026 Jun 15. PMID: 42298179 -
Oncogene
2021 Jul;40(30):4884-4893. PMID: 34163029 -
Oncogene
Epiregulin confers EGFR-TKI resistance via EGFR/ErbB2 heterodimer in non-small cell lung cancer. [Abstract]2021 Apr;40(14):2596-2609. PMID: 33750895 -
Oncogene
Epigenetic silencing of miR-483-3p promotes acquired gefitinib resistance and EMT in EGFR-mutant NSCLC by targeting integrin β3. [Abstract]2018 Aug;37(31):4300-4312. PMID: 29717264
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Aug;37(31):4300-4312. [Abstract]
Western blot analysis of E-cadherin and vimentin in HCC827 xenograft tumors treated with Gefitinib daily for 6-8 weeks until tumors regrown (resistant) or saline for 1 week (sensitive) (left panel).
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Cell Death Discov
Targeting the up-regulated CNOT3 reverses therapeutic resistance and metastatic progression of EGFR-mutant non-small cell lung cancer. [Abstract]2023 Nov 2;9(1):406. PMID: 37919290 -
Cell Rep
Branched-Chain Amino Acid Metabolic Reprogramming Orchestrates Drug Resistance to EGFR Tyrosine Kinase Inhibitors. [Abstract]2019 Jul 9;28(2):512-525.e6. PMID: 31291585 -
Arch Toxicol
Using the lentiviral vector system to stably express chicken P-gp and BCRP in MDCK cells for screening the substrates and studying the interplay of both transporters. [Abstract]2018 Jun;92(6):2027-2042. PMID: 29725709 -
Clin Transl Med
Multi-omic profiling defines three distinct molecular subtypes of urothelial carcinoma with implications for precision therapy. [Abstract]2026 Mar;16(3):e70638. PMID: 41804750 -
J Med Chem
Dual-Targeting TrxR-EGFR Alkynyl-Au(I) Gefitinib Complex Induces Ferroptosis in Gefitinib-Resistant Lung Cancer via Degradation of GPX4. [Abstract]2025 Mar 13;68(5):5275-5291. PMID: 39968846 -
Anal Chem
Quantum Well-Enhanced Plasmonic Substrate to Enhance Spontaneously Blinking Fluorescence for Single-Molecule Localization Microscopy. [Abstract]2026 Mar 24;98(11):7999-8009. PMID: 41805316 -
Fundam Res
Gefitinib facilitates PINK1/Parkin-mediated mitophagy by enhancing mitochondrial recruitment of OPTN. [Abstract]2022 Mar 3;2(5):807-816. PMID: 38933121 -
Cell Mol Life Sci
IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer. [Abstract]2019 May;76(10):2015-2030. PMID: 30725116 -
Cancer Cell Int
Attenuated expression of SNF5 facilitates progression of bladder cancer via STAT3 activation. [Abstract]2021 Dec 7;21(1):655. PMID: 34876150 -
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J Invest Dermatol
Blue light irradiation induces skin barrier damage through EGFR/ERK/c-Jun signaling pathway. [Abstract]2026 Feb 23:S0022-202X(26)00102-8. PMID: 41740835 -
J Invest Dermatol
LPCAT1 Promotes Cutaneous Squamous Cell Carcinoma via EGFR-Mediated Protein Kinase B/p38MAPK Signaling Pathways. [Abstract]2022 Feb;142(2):303-313.e9. PMID: 34358528 -
Biochem Pharmacol
Lysine methylation-mediated SMYD2 degradation by casticin sensitizes non-small-cell lung cancer cells to osimertinib therapy. [Abstract]2026 Jan;243(Pt 2):117562. PMID: 41314435 -
Biochem Pharmacol
Molecular Dissection of the AHR-AREG driven EGFR-ERK1/2-CyclinD1 axis in acquired lenvatinib resistance of Hepatocellular carcinoma. [Abstract]2025 Jun 6:239:117032. PMID: 40482839 -
Neurobiol Dis
ErbB1-dependent signalling and vesicular trafficking in primary afferent nociceptors associated with hypersensitivity in neuropathic pain. [Abstract]2020 Aug;142:104961. PMID: 32531343 -
Breast Cancer Res
Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade. [Abstract]2017 Aug 4;19(1):90. PMID: 28778177
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90. [Abstract]
The effect of Gefitinib-FTY720 treatment on CD44 expression in TNBC cell lines. HCC1806, Hs578T, and MDA-MB-468 TNBC cell lines at ~40% confluence in 12-well plates are exposed for 24 h to Gefitinib (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.
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Mol Cancer Ther
AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]2023 Sep 5;22(9):1013-1027. PMID: 37302522 -
J Ethnopharmacol
Reduction in gefitinib resistance mediated by Yi-Fei San-Jie pill in non-small cell lung cancer through regulation of tyrosine metabolism, cell cycle, and the MET/EGFR signaling pathway. [Abstract]2023 Oct 5:314:116566. PMID: 37169317 -
Chem Biol Interact
E3 ubiquitin ligase RNF180 reduces sensitivity of triple-negative breast cancer cells to Gefitinib by downregulating RAD51. [Abstract]2022 Feb 25:354:109798. PMID: 34998818 -
Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
Respir Res
Combination of betulinic acid and EGFR-TKIs exerts synergistic anti-tumor effects against wild-type EGFR NSCLC by inducing autophagy-related cell death via EGFR signaling pathway. [Abstract]2024 May 20;25(1):215. PMID: 38764025 -
Int J Mol Sci
Carcinoembryonic Antigen-Related Cell Adhesion Molecule 5 as a Biomarker for Predicting Response to Erlotinib and Gefitinib in Lung Adenocarcinoma: An Integrative Analysis of Transcriptomic Data of PC-9 and Drug-Resistant PC-9 Cell Lines. [Abstract]2026 Mar 28;27(7):3092. PMID: 41977278 -
Int J Oncol
2022 Nov;61(5):139. PMID: 36169178 -
Int J Mol Sci
Tamoxifen Exerts Anticancer Effects on Pituitary Adenoma Progression via Inducing Cell Apoptosis and Inhibiting Cell Migration. [Abstract]2022 Feb 28;23(5):2664. PMID: 35269804 -
Int J Mol Sci
miR-196a Upregulation Contributes to Gefitinib Resistance through Inhibiting GLTP Expression. [Abstract]2022 Feb 4;23(3):1785. PMID: 35163707 -
Int J Mol Sci
2021 Feb 9;22(4):1745. PMID: 33572344 -
Int J Mol Sci
Relevance of Breast Cancer Resistance Protein to Pharmacokinetics of Florfenicol in Chickens: A Perspective from In Vivo and In Vitro Studies. [Abstract]2018 Oct 15;19(10). pii: E3165. PMID: 30326566 -
Cell Oncol (Dordr)
2025 Jul 10. PMID: 40637801 -
Pharmaceuticals (Basel)
β-Elemene Reverses Gefitinib Resistance in NSCLC Cells by Inhibiting lncRNA H19-Mediated Autophagy. [Abstract]2024 May 14;17(5):626. PMID: 38794196 -
Pharmaceuticals (Basel)
Antiproliferative Activity of a New Quinazolin-4(3 H)-One Derivative via Targeting Aurora Kinase A in Non-Small Cell Lung Cancer. [Abstract]2022 Jun 2;15(6):698. PMID: 35745617 -
Cell Oncol (Dordr)
Y-box binding protein 1 (YB-1) promotes gefitinib resistance in lung adenocarcinoma cells by activating AKT signaling and epithelial-mesenchymal transition through targeting major vault protein (MVP). [Abstract]2021 Feb;44(1):109-133. PMID: 32894437 -
Eur J Pharm Sci
Preclinical validation of tetrahydroquinoline derivatives as EGFR inhibitor inducing glioblastoma cell death. [Abstract]2026 Mar 14:107503. PMID: 41839309 -
Int Immunopharmacol
ELK3-SERPINE1-PCBP2 axis promotes gefitinib resistance in lung cancer by inhibiting ferroptosis. [Abstract]2025 Dec 10:169:115963. PMID: 41380194 -
Int Immunopharmacol
CD9 downregulation activates EGFR/ERK/WAVE2 pathway to remodel F-actin and promote proliferation and migration of cholesteatoma epithelial cells. [Abstract]2025 Aug 25:164:115401. PMID: 40858050 -
Bioorg Chem
A pomalidomide-based gefitinib PROTAC degrader effectively inhibits lung cancer progression in EGFR-TKIs-acquired resistant models by targeting EGFR degradation and ETFA-mediated ATP generation. [Abstract]2025 Aug 9:164:108864. PMID: 40815992 -
Bioorg Chem
A novel Quinazoline derivative exerts anti-tumor effects in non-small cell lung cancer through Wnt/β-catenin pathway inhibition. [Abstract]2025 Apr 15:160:108481. PMID: 40253763 -
Eur J Pharmacol
Discovery of 4-((3,4-dichlorophenyl)amino)-2-methylquinolin-6-ol derivatives as EGFR and HDAC dual inhibitors. [Abstract]2023 Dec 5:960:176114. PMID: 37863412 -
Eur J Pharmacol
2021 Nov 5:910:174441. PMID: 34474028 -
Mol Cancer Res
Activation of AXL as a Preclinical Acquired Resistance Mechanism Against Osimertinib Treatment in EGFR-Mutant Non-Small Cell Lung Cancer Cells. [Abstract]2019 Feb;17(2):499-507. PMID: 30463991 -
Front Endocrinol
Nuclear Insulin-Like Growth Factor Binding Protein-3 As a Biomarker in Triple-Negative Breast Cancer Xenograft Tumors: Effect of Targeted Therapy and Comparison With Chemotherapy. [Abstract]2018 Mar 22:9:120. PMID: 29623068 -
Molecules
Facilitating Anti-Cancer Combinatorial Drug Discovery by Targeting Epistatic Disease Genes. [Abstract]2018 Mar 23;23(4). pii: E736. PMID: 29570606 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
J Mol Biol
2025 Jun 2:169261. PMID: 40466906 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Cell Rep Methods
2023 Feb 21;3(2):100411. PMID: 36936075 -
Front Microbiol
EGFR Activation Impairs Antiviral Activity of Interferon Signaling in Brain Microvascular Endothelial Cells During Japanese Encephalitis Virus Infection. [Abstract]2022 Jun 30;13:894356. PMID: 35847084 -
Cancers (Basel)
Triptolide Triggers Protective Autophagy via ROS Induction in NSCLC: Therapeutic Synergy with Autophagy Inhibition. [Abstract]2026 Mar 11;18(6):902. PMID: 41899507 -
Lung Cancer
Chemotherapy-induced PDL-1 expression in cancer-associated fibroblasts promotes chemoresistance in NSCLC. [Abstract]2023 Jul:181:107258. PMID: 37245409 -
Biochim Biophys Acta Mol Basis Dis
FGFR2 upregulates PAI-1 via JAK2/STAT3 signaling to induce M2 polarization of macrophages in colorectal cancer. [Abstract]2023 Apr;1869(4):166665. PMID: 36781088 -
J Cell Mol Med
2021 Jul;25(13):6280-6288. PMID: 34076957 -
J Cell Mol Med
RNA methyltransferase METTL3 induces intrinsic resistance to gefitinib by combining with MET to regulate PI3K/AKT pathway in lung adenocarcinoma. [Abstract]2021 Mar;25(5):2418-2425. PMID: 33491264 -
Drug Dev Res
Proteolysis targeting chimera (PROTAC) for epidermal growth factor receptor enhances anti-tumor immunity in non-small cell lung cancer. [Abstract]2021 May;82(3):422-429. PMID: 33231319 -
J Cell Mol Med
Novel regulation of miR-34a-5p and HOTAIR by the combination of berberine and gefitinib leading to inhibition of EMT in human lung cancer. [Abstract]2020 May;24(10):5578-5592. PMID: 32248643 -
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AAPS PharmSciTech
Solid Dispersions of Gefitinib Prepared by Spray Drying with Improved Mucoadhesive and Drug Dissolution Properties. [Abstract]2022 Jan 4;23(1):48. PMID: 34984564 -
Oncol Rep
Inhibition of primary ciliogenesis enhances efficacy of EGFR‑TKIs against non‑small cell lung cancer cells. [Abstract]2026 Feb;55(2):30. PMID: 41347810 -
Sci Rep
Rosmarinic acid potentiates gefitinib in lung adenocarcinoma by modulating interactions between cancer cells and cancer-associated fibroblasts. [Abstract]2025 Jul 6;15(1):24100. PMID: 40619518 -
Sci Rep
Monolayer culture alters EGFR inhibitor response through abrogation of microRNA-mediated feedback regulation. [Abstract]2024 Mar 27;14(1):7303. PMID: 38538642 -
Oncol Rep
TRIP13 overexpression promotes gefitinib resistance in non‑small cell lung cancer via regulating autophagy and phosphorylation of the EGFR signaling pathway. [Abstract]2023 May;49(5):84. PMID: 36896765 -
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J Biol Chem
SARS-CoV-2 hijacks macropinocytosis to facilitate its entry and promote viral spike-mediated cell-to-cell fusion. [Abstract]2022 Nov;298(11):102511. PMID: 36259516 -
Oncol Rep
2020 Aug;44(2):698-710. PMID: 32627036 -
Fish Shellfish Immunol
Molecular characterization and function of EGFR during viral infectionprocess in Mandarin fishSiniperca chuatsi. [Abstract]2020 Jul;102:211-217. PMID: 32298770 -
Oncol Rep
Efficacy of gefitinib‑celecoxib combination therapy in docetaxel‑resistant prostate cancer. [Abstract]2018 Oct;40(4):2242-2250. PMID: 30066906
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250. [Abstract]
Effects of Gefitinib(G) and SC 58635 (Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, SC 58635 and their combination on ABCB1 (MDR1), FOXM1 and Bcl 2 expression in the PC3/DR and DU145/DR cell lines are determined by a western blot assay.
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Cancer Res Treat
MLL4 Regulates the Progression of Non-Small-Cell Lung Cancer by Regulating the PI3K/AKT/SOX2 Axis. [Abstract]2023 Jul;55(3):778-803. PMID: 36701842 -
Cell Signal
2024 Oct:122:111307. PMID: 39048037 -
Mol Med Rep
ISX promotes tumor migration and invasion in lung cancer by upregulating COL1A1 in vitro. [Abstract]2026 Feb;33(2):77. PMID: 41480691 -
Transl Lung Cancer Res
Development of a 3D-3 co-culture microbead consisting of cancer-associated fibroblasts and human umbilical vein endothelial cells for the anti-tumor drug assessment of lung cancer. [Abstract]2025 Jun 30;14(6):2159-2179. PMID: 40673102 -
Transl Lung Cancer Res
Construction of a lung cancer 3D culture model based on alginate/gelatin micro-beads for drug evaluation. [Abstract]2024 Oct 31;13(10):2698-2712. PMID: 39507032 -
Viruses
The Role of Epidermal Growth Factor Receptor Signaling Pathway during Bovine Herpesvirus 1 Productive Infection in Cell Culture. [Abstract]2020 Aug 24;12(9):927. PMID: 32846937 -
Exp Cell Res
PPARγ agonist efatutazone and gefitinib synergistically inhibit the proliferation of EGFR-TKI-resistant lung adenocarcinoma cells via the PPARγ/PTEN/Akt pathway. [Abstract]2017 Dec 15;361(2):246-256. PMID: 29080795
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256. [Abstract]
Western blot analysis for p21, p-p21, Cyclin D1. Bcl-2, Caspase 3, Cleaved Caspase 3, Caspase 9, Cleaved Caspase 9 and Bax in HCC827-GR and PC-9-GR cells treated with control, Efatutazone alone, Gefitinib alone, or Efatutazone combined with gefitinib for 48 h.
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Mol Med Rep
Dihydroartemisinin and gefitinib synergistically inhibit NSCLC cell growth and promote apoptosis via the Akt/mTOR/STAT3 pathway. [Abstract]2017 Sep;16(3):3475-3481. PMID: 28713965
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3475-3481. [Abstract]
Cyclin B1 and Cdk1 protein expression levels are significantly downregulated in NCI-H1975 cells treated with the combination of DHA (5 µM) and Gefitinib (10 µM).
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Toxicol Appl Pharmacol
MiR-29a/DNMT3A axis participates in Dihydroartemisinin's suppression on lung adenocarcinoma: Implications for overcoming acquired resistance to EGFR-TKIs. [Abstract]2026 Mar 4:511:117777. PMID: 41791429 -
Food Nutr Res
TLR2/4-mediated NF-κB pathway combined with the histone modification regulates β-defensins and interleukins expression by sodium phenyl butyrate in porcine intestinal epithelial cells. [Abstract]2018 Dec 6:62. PMID: 30574051 -
Endocrinology
2023 Mar 13;164(5):bqad042. PMID: 36929849 -
Front Oncol
Co-administration of MDR1 and BCRP or EGFR/PI3K inhibitors overcomes lenvatinib resistance in hepatocellular carcinoma. [Abstract]2022 Sep 8:12:944537. PMID: 36158676 -
Front Oncol
Role of GPX4-Mediated Ferroptosis in the Sensitivity of Triple Negative Breast Cancer Cells to Gefitinib. [Abstract]2020 Dec 23:10:597434. PMID: 33425751 -
Front Oncol
Targeting 14-3-3ζ Overcomes Resistance to Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors in Lung Adenocarcinoma via BMP2/Smad/ID1 Signaling. [Abstract]2020 Oct 5;10:542007. PMID: 33123465 -
Int J Med Sci
Nephronectin promotes cardiac repair post myocardial infarction via activating EGFR/JAK2/STAT3 pathway. [Abstract]2022 May 13;19(5):878-892. PMID: 35693734 -
Kaohsiung J Med Sci
Dihydroartemisinin enhances gefitinib cytotoxicity against lung adenocarcinoma cells by inducing ROS-dependent apoptosis and ferroptosis. [Abstract]2023 Jul;39(7):699-709. PMID: 37057810
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Kaohsiung J Med Sci. 2023 Jul;39(7):699-709. [Abstract]
Gefitinib (0-20 μM; 24 h) significantly inhibits the viability of A549 cells.
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Ren Fail
Dihydromyricetin protects against cisplatin-induced renal injury and mitochondria-mediated apoptosis via the EGFR/HSP27/STAT3 signaling pathway. [Abstract]2025 Dec;47(1):2490202. PMID: 40230054 -
Breast Cancer Res Treat
2025 Jun;211(2):467-478. PMID: 40055251 -
FEBS Lett
MEK/ERK MAP kinase limits poly I:C-induced antiviral gene expression in RAW264.7 macrophages by reducing interferon-beta expression. [Abstract]2021 Nov;595(21):2665-2674. PMID: 34591979 -
Mol Pharmacol
Functional RNAi Screens Define Distinct Protein Kinase Vulnerabilities in EGFR-Dependent HNSCC Cell Lines. [Abstract]2019 Dec;96(6):862-870. PMID: 31554698 -
Genes (Basel)
The Impact of Bevacizumab and miR200c on EMT and EGFR-TKI Resistance in EGFR-Mutant Lung Cancer Organoids. [Abstract]2024 Dec 19;15(12):1624. PMID: 39766891 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
BMC Pulm Med
The combination therapy of isomucronulatol 7-O-beta-glucoside (IMG) and CEP-9722 targeting ferroptosis-related biomarkers in non-small cell lung cancer (NSCLC). [Abstract]2023 May 11;23(1):162. PMID: 37165402 -
Infect Immun
Bartonella henselae Persistence within Mesenchymal Stromal Cells Enhances Endothelial Cell Activation and Infectibility That Amplifies the Angiogenic Process. [Abstract]2021 Jul 15;89(8):e0014121. PMID: 34031126 -
J Cancer Res Clin Oncol
Gefitinib sensitization of cisplatin-resistant wild-type EGFR non-small cell lung cancer cells. [Abstract]2020 Jul;146(7):1737-1749. PMID: 32342201 -
Mol Pain
The upregulation of EGFR in the dorsal root ganglion contributes to chronic compression of dorsal root ganglions-induced neuropathic pain in rats. [Abstract]2019 Jan-Dec:15:1744806919857297. PMID: 31215332 -
J Sep Sci
Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. [Abstract]2017 Oct;40(19):3782-3791. PMID: 28749011 -
Exp Eye Res
SN promote retinal pathological neovascularization through activation of EGFR, IR and IGF-1R. [Abstract]2024 Nov 14:110158. PMID: 39549871 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Cancer Manag Res
Deguelin Restores Paclitaxel Sensitivity in Paclitaxel-Resistant Ovarian Cancer Cells via Inhibition of the EGFR Signaling Pathway. [Abstract]2024 May 28:16:507-525. PMID: 38827785 -
Biomed Res Int
B7-H3-Induced Signaling in Lung Adenocarcinoma Cell Lines with Divergent Epidermal Growth Factor Receptor Mutation Patterns. [Abstract]2020 Dec 24:2020:8824805. PMID: 33426073 -
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Oncol Lett
Atractyloside inhibits gefitinib‑resistant non‑small‑cell lung cancer cell proliferation. [Abstract]2024 Jul 30;28(4):466. PMID: 39119229 -
Oncol Lett
Tumor-associated macrophage-derived exosomes promote EGFR-TKI resistance in non-small cell lung cancer by regulating the AKT, ERK1/2 and STAT3 signaling pathways. [Abstract]2022 Aug 24;24(4):356. PMID: 36168315 -
Anticancer Res
Overexpression of AGR2 Is Associated With Drug Resistance in Mutant Non-small Cell Lung Cancers. [Abstract]2020 Apr;40(4):1855-1866. PMID: 32234873 -
Biomed Chromatogr
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer. [Abstract]2016 Jul;30(7):1150-4. PMID: 26525154 -
Biochem Genet
GSDME Deficiency Suppresses ER Stress-Induced Autophagic Cell Death via mTOR/S6K1 Activation in Hepatobiliary Carcinomas. [Abstract]2025 May 23. PMID: 40407851 -
Am J Transl Res
Therapeutic anti-CD147 antibody sensitizes cells to chemoradiotherapy via targeting pancreatic cancer stem cells. [Abstract]2019 Jun 15;11(6):3543-3554. PMID: 31312365 -
Curr Med Sci
Huaier Aqueous Extract Combined with Gefitinib Promotes ACSL4-Dependent Ferroptosis and Overcomes Gefitinib Resistance in Non-Small Cell Lung Cancer. [Abstract]2026 Feb;46(1):197-211. PMID: 41557244 -
Drug Discov Ther
Development of a simple high-performance liquid chromatography-ultraviolet detection method for selpercatinib determination in human plasma. [Abstract]2025 Jan 14;18(6):387-390. PMID: 39647867 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
Chem Pharm Bull (Tokyo)
Synergistic Activity of an Antimetabolite Drug and Tyrosine Kinase Inhibitors against Breast Cancer Cells. [Abstract]2017 Aug 1;65(8):768-775. PMID: 28539531
Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]
Changes in Bcl-2 protein expression in MCF-7 cells after treatment with 2CdA, BMS-354825 or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.
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bioRxiv
Preservation of Human Colonic Stem Cells Requires an ERK Dynamics Checkpoint Mediated by AKT. [Abstract]2026 Apr 11:2026.04.02.715982. PMID: 41959484 -
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J Physiol Investig
Pectolinarigenin Induces Mitochondrion-dependent Apoptosis, Causes G2/M Arrest, and Inhibits Migration and Invasion in Rheumatoid Arthritis-Fibroblast-like Synoviocytes. [Abstract]2026 Jan 1;69(1):42-56. PMID: 41606826 -
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bioRxiv
2025 Nov 26:2025.11.24.690135. PMID: 41383764 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
bioRxiv
Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]2025 Jun 7:2025.06.04.657911. PMID: 40502048 -
bioRxiv
Cetuximab increases LGR5 expression and augments LGR5-targeting antibody-drug conjugate efficacy in patient-derived colorectal cancer models. [Abstract]2025 Jun 24:2025.06.18.660406. PMID: 40667242 -
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bioRxiv
Development of a new flippase-dependent mouse model for red fluorescence-based isolation of KrasG12D oncogene-expressing tumor cells. [Abstract]2024 Jul 26:2024.07.26.605291. PMID: 41030963 -
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bioRxiv
Large-scale control over collective cell migration using light-controlled epidermal growth factor receptors. [Abstract]2024 May 31:2024.05.30.596676. PMID: 38853934 -
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Res Sq
Mycobacterium tuberculosis resides in lysosome-poor monocyte-derived lung cells during chronic infection. [Abstract]2023 Jun 15:rs.3.rs-3049913. PMID: 37398178 -
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Oxid Med Cell Longev
Carbonic Anhydrase IX Controls Vulnerability to Ferroptosis in Gefitinib-Resistant Lung Cancer. [Abstract]2023 Jan 31:2023:1367938. PMID: 36760347 -
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Cell Insight
Phosphorylated STYK1 restrains the inhibitory role of EGFR in autophagy initiation and EGFR-TKIs sensitivity. [Abstract]2022 Jun 16;1(4):100045. PMID: 37192859 -
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Oncotarget
Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma-an aggressive and fatal disease. [Abstract]2017 Dec 2;8(68):112313-112329. PMID: 29348827 -
Oncotarget
Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlotinib in a nude mouse model. [Abstract]2017 Oct 19;8(58):98771-98781. PMID: 29228726 -
Oncotarget
2016 Oct 25;7(43):69760-69769. PMID: 27626175 -
Oncotarget
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]2015 Oct 13;6(31):31313-22. PMID: 26375053
용액&용해도
H2O : 6.25 mg/mL (12.93 mM; Need ultrasonic)
DMSO : 0.227 mg/mL (0.47 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Cancer cells are seeded in 96-well plates and are treated with different doses of Gefitinib (0.01-20 μM), Metformin or both for 72 hours. Cell proliferation is measured with the MTT assay. The IC50 values are determined by interpolation from the dose-response curves. Results represent the median of 3 separate experiments each conducted in quadruplicate. The results of the combined treatment are analyzed according to the method of Chou and Talalay by using the CalcuSyn software program[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Four- to 6-week old female balb/c athymic (nu+/nu+) mice are acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that has been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter are detected, mice are left untreated or treated with oral administrations of metformin (200 mg/mL metformin diluted in drinking water and present throughout the experiment), gefitinib (150 mg/kg daily orally by gavage), or both for the indicated time periods. Each treatment group consists of 10 mice. Tumor volume is measured using the formula π/6×larger diameter×(smaller diameter)2.
Rats[4]
The rats are randomly assigned to 1 of 4 experimental groups: 1) the unirradiated rats treated with oral administration of vehicle (0.1% Tween 80) once daily; 2) the unirradiated rats treated with oral administration of gefitinib (50 mg/kg/day) once daily; 3) the irradiated rats treated with oral administration of vehicle once daily; 4) the irradiated rats treated with oral administration of gefitinib once daily. Each experimental group comprised 5-6 rats and all treatments are delivered for 14 days.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (283 KB)
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SDS (923 KB)
- English - EN (923 KB)
- Français - FR (923 KB)
- Deutsch - DE (923 KB)
- Norwegian - NO (923 KB)
- Español - ES (923 KB)
- Swedish - SV (923 KB)
- Italian - IT (923 KB)
- Korean - KR (923 KB)
- Portuguese - PT (923 KB)
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Handling Instructions (2659 KB)
References
[1]. Wakeling AE, et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54. [Content Brief]
[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. [Content Brief]
[3]. Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8. [Content Brief]
[4]. Morgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19. [Content Brief]
[5]. Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.0689 mL | 10.3443 mL | 20.6885 mL | 51.7213 mL |
| 5 mM | 0.4138 mL | 2.0689 mL | 4.1377 mL | 10.3443 mL | |
| 10 mM | 0.2069 mL | 1.0344 mL | 2.0689 mL | 5.1721 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.