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Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages.
Chin Med. 2025 Jan 03.
Aidi injection inhibits the migration and invasion of gefitinib-resistant lung adenocarcinoma cells by regulating the PLAT/FAK/AKT pathway
Gefitinib purchased from AbMole
Cancer Cell Int. 2023 Jul 2;23(1):129.
Exosome-derived circKIF20B suppresses gefitinib resistance and cell proliferation in non-small cell lung cancer
Gefitinib purchased from AbMole
Clin Transl Oncol. 2023 May;25(5):1425-1435.
ADAM12 promotes gemcitabine resistance by activating EGFR signaling pathway and induces EMT in bladder cancer
Gefitinib purchased from AbMole
Endocrinology. 2020 May 30;bqaa086.
RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice
Gefitinib purchased from AbMole
Clin Cancer Res. 2018 Nov 15;24(22):5658-5672.
Increased Synthesis of MCL-1 Protein Underlies Initial Survival of EGFR-Mutant Lung Cancer to EGFR Inhibitors and Provides a Novel Drug Target.
Gefitinib purchased from AbMole
Clin Cancer Res. 2018 Jan 1;24(1):197-208.
Epithelial-to-mesenchymal transition antagonizes response to targeted therapies in lung cancer by suppressing BIM
Gefitinib purchased from AbMole
Sci Rep. 2017 May 8;7(1):1578.
Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wallmediated lipolysis, inflammation and dysglycemia
Gefitinib purchased from AbMole
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Source | Clinical Cancer Research (2018 Nov). Figure 1. Gefitinib (Abmole Bioscience) |
| Method | Apoptosis and cell cycle analysis | |
| Cell Lines | EGFR mutant NSCLC cell lines | |
| Concentrations | 50 nM | |
| Incubation Time | 72 h | |
| Results | However, re-exposure to gefitinib over an additional 72 hrs period was inadequate to induce robust apoptosis in PC9 cells, and by the third cycle HCC827 cells also lost their ability to undergo apoptosis. |
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Source | Clin Cancer Res (2017). Figure 2. Gefitinib (Abmole Bioscience) |
| Method | apoptosis quantified | |
| Cell Lines | HCC4006 and H1975 cells | |
| Concentrations | 1μM | |
| Incubation Time | 72 h | |
| Results | We found directly inducing EMT by exogenous TWIST activation (Fig. 2) or chronic TGF- β treatment (Sup. Fig. 2) led to depressed levels of BIM resulting in suppression of EGFRi-induced apoptosis and resistance to EGFRi (WZ4002 and gefitinib). |
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Source | Clin Cancer Res (2017). Figure 2. Gefitinib (Abmole Bioscience) |
| Method | apoptosis quantified | |
| Cell Lines | HCC4006 and H1975 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 72 h | |
| Results | We found directly inducing EMT by exogenous TWIST activation (Fig. 2) or chronic TGF- β treatment (Sup. Fig. 2) led to depressed levels of BIM resulting in suppression of EGFRi-induced apoptosis and resistance to EGFRi (WZ4002 and gefitinib). |
 |
Source | Sci Rep (2017). Figure 7. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | TKI gefitinib inhibits RIPK2-mediated dysglycemia in vivo. | |
| Cell Lines | C57Bl/6J (WT) and RIPK2−/− mice | |
| Concentrations | 100 mg/kg | |
| Incubation Time | 4 days | |
| Results | Pre-treatment with gefitinib attenuated lower blood glucose at 6 h post-FK565 injection. At the time of the glucose tolerance test (GTT, 24 h after FK565 injection) gefitinib pre-treatment did not alter fasting blood glucose. |
 |
Source | Sci Rep (2017). Figure 6. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | TKI gefitinib inhibits RIPK2-mediated inflammation in vivo. | |
| Cell Lines | RIPK2−/− mice | |
| Concentrations | 5–200 mg/kg | |
| Incubation Time | 4 days | |
| Results | Our results show that treatment with gefitinib at doses equal or greater than 50 mg/kg attenuated Nod1 mediated Cxcl1 protein levels in the circulation of mice in a dose-dependent manner. |
 |
Source | Sci Rep (2017). Figure 5. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | C57Bl/6J (WT) and RIPK2−/− mice | |
| Cell Lines | HEK293 cells | |
| Concentrations | 1 or 5 μM | |
| Incubation Time | ||
| Results | We assessed FK565- versus LPS-induced NF-κB activity using HEK293 cells stably over-expressing Nod1 or Tlr4. Consistent with cytokine secretion in adipocytes and macrophages, we find that treatment of HEK Nod1 cells with FK565 (10 μg/mL) increases NF-κB activation, which is attenuated in a dose-dependent manner by pre-incubation with gefitinib at 1 and 5 μM. |
 |
Source | Sci Rep (2017). Figure 4. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | ||
| Cell Lines | bacterial cell | |
| Concentrations | 0.2, 1 or 5 μM | |
| Incubation Time | 1 h | |
| Results | Time course of FK565-stimulated Cxcl1 secretion in BMDMs (B) n = 4–12. Levels of Cxcl1 released from WT (left panel) or RIPK2−/−(right panel) BMDMs after stimulation with the Tlr4 ligand LPS (0.5 μg/mL) for 48 h and pre-incubated for 1 h with 0.2, 1 or 5 μM gefitinib or SB203580 (C) n = 4–12. |
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Source | Sci Rep (2017). Figure 3. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | Westen Blot | |
| Cell Lines | bacterial cell | |
| Concentrations | 5 μM | |
| Incubation Time | 1 h | |
| Results | Quantitative comparison was conducted between samples from 4 different blots derived from the same experiment and processed in parallel. (n = 8 total (n = 2/condition per blot). |
 |
Source | Sci Rep (2017). Figure 2. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | TKIs inhibit cytokine response | |
| Cell Lines | bacterial cell | |
| Concentrations | 1 or 5 μM | |
| Incubation Time | 1 h | |
| Results | Our results show that pre-incubation with 1–5 μM gefitinib or 1–5 μM SB203580, but not 1–5 μM imatinib significantly attenuated FK565-induced Cxcl1 and Il6 release in a dose-dependent manner in adipocytes. |
 |
Source | Sci Rep (2017). Figure 1. Gefitinib (AbMole Bioscience, Houston, TX) |
| Method | bacterial cell wall-induced lipolysis | |
| Cell Lines | Murine 3T3-L1 preadipocytes | |
| Concentrations | 5 μM | |
| Incubation Time | 48 h | |
| Results | Only 1 or 5 μM gefitinib and 1 or 5 μM SB203580 dose dependently attenuated the increased rate of glycerol release induced by FK565. |
| Cell Experiment | |
|---|---|
| Cell lines | MDA-361, SKBR-3, MDA-453 and BT-474 cells |
| Preparation method | Monolayer Growth and Anchorage-independent Growth Assays. For monolayer growth, cells were seeded at a density of 3–4 104 cells in 12-well plates. Twenty-four h later, ZD1839 was added to the cells. Fresh medium ZD1839 was replaced on day 3. On day 5, cells were harvested by trypsinization and counted with a Zeiss Coulter Counter (Beckman Coulter, Miami, FL). Colony-forming assays in soft agarose were performed as described previously (30). Tumor cell colonies measuring 50 m were counted after 7 days using an Omnicon 3800 colony counter and Tumor Colony Analysis V2.IIA software (Imaging Products International, Inc.). |
| Concentrations | 0.1–10 µ M |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | BT-474 cells Xenograft in Athymic Mice |
| Formulation | 0.05% Tween 80 |
| Dosages | 200 mg/kg/day for 28 days |
| Administration | oral gavage |
| Molecular Weight | 446.90 |
| Formula | C22H24ClFN4O3 |
| CAS Number | 184475-35-2 |
| Solubility (25°C) | DMSO 68 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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