Gefitinib (ZD1839) (Synonyms: ZD1839) |
| Catalog No.GC16737 |
Gefitinib (ZD1839), is a potent EGFR-TKI (EGFR tyrosine kinase inhibitor) with IC50 of 0.033 µM, selectively inhibits EGF-stimulated tumor cell growth with IC50 of 0.054 µM and that blocks EGF-stimulated EGFR (epidermal growth factor receptor) autophosphorylation in tumor cells[1].
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 184475-35-2
Sample solution is provided at 25 µL, 10mM.
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Gefitinib (ZD1839), is a potent EGFR-TKI (EGFR tyrosine kinase inhibitor) with IC50 of 0.033 µM, selectively inhibits EGF-stimulated tumor cell growth with IC50 of 0.054 µM and that blocks EGF-stimulated EGFR (epidermal growth factor receptor) autophosphorylation in tumor cells[1].
In vitro, the NR6wtEGFR and NR6M cell lines had low levels of PLC-γ phosphorylations but the level in the NR6M cell line was more resistant to inhibition by gefitinib (IC50 of 43 and 369 nm, respectively)[2]. A gefitinib concentration above 0.1 µm decreases the colony-forming ability of NR6W and NR6wtEGFR cells and a concentration of 1.5 µm completely abolishes the ability of these cell lines to form colonies[2]. The IC50 values of four NSCLC cells for gefitinib were 18.90 µmol/L, 16.40 µmol/L, 1.794 µmol/L and 15.99 µmol/L for A549, H1975, PC9, and PC9/GR, respectively[3]. In addition, a small concentration of gefitinib (0.62 µmol/L) significantly inhibited IL-13-induced M2-like polarization of macrophages[4].
In vivo, C57BL/6 mice were treated with 20, 40 and 80 mg/kg, once-daily for 18 days, intragastrically significantly inhibited lung metastases compared with lung tumor metastatic model mice, further indicating that the lung tissue had a reduced number of metastatic lesions and cancer cells[5]. In vivo, the growth of D341 and Daoy (medulloblastoma cell lines) xenografts treated with gefitinib at 150 mg/kg per day was inhibited by approximately 50%. Ectopically overexpressed HER2 in Daoy cells significantly increased sensitivity to gefitinib's antitumor effects in vivo (tumor volume inhibition = 78%)[6].
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.
[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]. Sun C, et al. FGL1 regulates acquired resistance to Gefitinib by inhibiting apoptosis in non-small cell lung cancer. Respir Res. 2020 Aug 10;21(1):210.
[4]. Tariq M, 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.
[5]. Fan Q, et al. Pedunculoside inhibits epithelial-mesenchymal transition and overcomes Gefitinib-resistant non-small cell lung cancer through regulating MAPK and Nrf2 pathways. Phytomedicine. 2023 Jul 25;116:154884.
[6]. Meco D, et al. Antitumor effect in medulloblastoma cells by gefitinib: Ectopic HER2 overexpression enhances gefitinib effects in vivo. Neuro Oncol. 2009 Jun;11(3):250-9.
| Cell experiment [1]: | |
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Cell lines |
PC-9 or PC-9/GR cells |
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Preparation Method |
A549 (2 × 103/100 µL/well), PC-9 (3 × 103/100 µL/well) or PC-9/GR cells (3 × 103/100 µL/well) were plated into each well of 96-well plates. After incubating 24 h, several concentrations of W2014-S, W2014-R, gefitinib, and/or culture supernatants were added to each well, and incubation was continued for another 72 h. Cell proliferation and IC50 values of gefitinib at different concentrations for 72 h were measured in PC-9 (0 - 600 nM) and PC-9/GR (0 - 120 nM) cells. |
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Reaction Conditions |
0 - 600 nM; 0 - 120 nM; 72 h |
|
Applications |
PC-9 cells harboring EGFR activating mutations were sensitive to gefitinib with an IC50 at 32 nM. While PC-9 acquired resistance to gefitinib after continuous exposure to gefitinib at low concentration for a long time, and then it was termed as PC-9/GR with an IC50 at 6.547 µM. |
| Animal experiment [2]: | |
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Animal models |
nude mice |
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Preparation Method |
PC9/GR and A549/GR cells stably transfected with sh-NC or sh-SNHG17#1 were inoculated into nude mice (male, 6 weeks old). After 4 days of inoculation, the mice were treated with gefitinib (oral gavage, 5 days per week at 25 mg/kg). After 28 days of inoculation, all mice developed tumours. |
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Dosage form |
25 mg/kg; p.o. |
|
Applications |
LncRNA SNHG17 knockdown or treatment with gefitinib could decrease the tumour volume and weight. |
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References: Zheng Q, et al. A novel STAT3 inhibitor W2014-S regresses human non-small cell lung cancer xenografts and sensitizes EGFR-TKI acquired resistance. Theranostics. 2021 Jan 1;11(2):824-840. |
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| Cas No. | 184475-35-2 | SDF | |
| Sinónimos | ZD1839 | ||
| Chemical Name | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 | ||
| Formula | C22H24ClFN4O3 | M.Wt | 446.9 |
| Solubility | ≥ 22.3mg/mL in DMSO, ≥ 2.48 mg/mL in EtOH with ultrasonic | Storage | Store at 2-8°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2376 mL | 11.1882 mL | 22.3764 mL |
| 5 mM | 0.4475 mL | 2.2376 mL | 4.4753 mL |
| 10 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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