| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Gefitinib (formerly ZD1839, ZD-1839 or trade name: Iressa) is a potent and orally bioavailable EGFR inhibitor with potential anticancer activity. In the NR6wtEGFR and NR6W cells, it inhibits EGFR Tyr1173, Tyr992, Tyr1173, and Tyr992 with IC50 values of 37 nM, 37 nM, 26 nM, and 57 nM, respectively. A variety of human tumor types, such as head and neck, prostate, breast, ovarian, colon, small-cell lung, and non-small-cell lung cancer, show anti-angiogenic properties when treated with gefitinib. The FDA authorized gefitinib in May 2003 for the treatment of non-small cell lung cancer (NSCLC). As a third-line therapy, it was authorized for use as monotherapy in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) following the failure of both platinum-based and docetaxel chemotherapies.
| Targets |
Tyr1173 (IC50 = 26 nM); Tyr1173 (IC50 = 37 nM); Tyr992 (IC50 = 37 nM); Tyr992 (IC50 = 57 nM)
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| ln Vitro |
Gefitinib effectively inhibits all EGFR tyrosine phosphorylation sites in cell lines that express EGFR, including NR6, NR6M, and NR6W cell lines, as well as high and low-EGFR-expressing cell lines. Tyr992 and Tyr1173, two phosphorylation sites, are less sensitive and require greater concentrations of Gefitinib to inhibit. With an IC50 of 27 nM, gefitinib efficiently prevents PLC-γ phosphorylation in NR6W cells. PLC-γ phosphorylation is low in the NR6wtEGFR and NR6M cell lines, but it is more resistant to gefitinib inhibition in the latter, with IC50 values of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations in the low-EGFR- and EGFRvIII-expressing cell lines, with IC50 values of 220 and 263 nM, respectively. When administered at doses ranging from 0.1 to 0.5μM, gefitinib significantly promotes NR6M cell colony formation as opposed to inhibiting it. On the other hand, Gefitinib totally prevents NR6M colony formation at a concentration of 2 μM. In both the high- and low-EGFR-expressing cell lines, gefitinib quickly and dose-dependently inhibits EGFR and ERK phosphorylation for up to 72 hours following EGF stimulation.[1] These EGF-driven untransformed MCF10A cells grow monolayerically when exposed to gefitinib, with an IC50 of 20 nM. [2] When paired with irradiation, Gefitinib (0.2 μM and 0.5 μM) significantly inhibited the growth of LoVo cells in comparison to radiation alone.[3]
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| ln Vivo |
Gefitinib (100 mg/kg) enhances radiation therapy's anti-tumor efficaciousness in LoVo tumor xenografts.[3] When established human GEO colon cancer xenografts are given to nude mice bearing these tumors, gefitinib treatment results in a reversible dose-dependent inhibition of tumor growth, as GEO tumors eventually resume the growth rate of controls.[4]
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| Enzyme Assay |
Gefitinib hydrochloride is an inhibitor with an IC50 value of 2-37 nM in NR6wtEGFR cells that selectively binds to and inhibits the EGFR tyrosine kinase. With an IC50 of 27 nM, gefitinib efficiently prevents PLC-γ phosphorylation in NR6W cells. PLC-γ phosphorylation is low in the NR6wtEGFR and NR6M cell lines, but it is more resistant to gefitinib inhibition in the latter, with IC50 values of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations in the low-EGFR- and EGFRvIII-expressing cell lines, with IC50 values of 220 and 263 nM, respectively.
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| Cell Assay |
Exponentially growing cells, such as NR6, NR6M, NR6M, and NR6W cells, are seeded in 96-well plates at a density of 2000 cells/well, allowed to adhere, and then washed in PBS before being incubated overnight in medium containing 0.5% FCS. After that, cells are exposed to different concentrations (0–2 μM) of either gefitinib or the solute controls, DMSO and EGF. Since NR6wtEGFR and NR6W cells can proliferate best at a known EGF concentration, 10 nM and 0.1 nM EGF, respectively, are added to NR6wtEGFR and NR6W cells. NR6 and NR6M cells do not receive additional EGF. An MTT proliferation assay is used to quantify the number of cells after 72 hours.
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| Animal Protocol |
Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
100 mg/kg Once daily by oral administration (0.1 mL/10 g body weight) for 14 days |
| References |
| Molecular Formula |
C22H24CLFN4O3
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|---|---|---|
| Molecular Weight |
446.90
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| Exact Mass |
446.15
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| Elemental Analysis |
C, 59.13; H, 5.41; Cl, 7.93; F, 4.25; N, 12.54; O, 10.74
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| CAS # |
184475-35-2
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
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| InChi Key |
XGALLCVXEZPNRQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
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| Chemical Name |
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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| Synonyms |
Gefitinib; ZD-1839; ZD1839; ZD 1839; Brand name: Iressa
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03292133 | Active Recruiting |
Drug: EGF816 Drug: Gefitinib |
Lung Cancer | Massachusetts General Hospital | October 31, 2017 | Phase 2 |
| NCT03122717 | Active Recruiting |
Drug: Gefitinib Drug: Osimertinib |
Non-Small Cell Lung Cancer | Dana-Farber Cancer Institute | May 9, 2017 | Phase 1 Phase 2 |
| NCT03758287 | Active Recruiting |
Drug: Gefitinib Drug: CT053PTSA |
Non-small Cell Lung Cancer | Sunshine Lake Pharma Co., Ltd. | November 2016 | Phase 1 Phase 2 |
| NCT03849768 | Active Recruiting |
Drug: Gefitinib Drug: HS-10296 |
Non Small Cell Lung Cancer | Jiangsu Hansoh Pharmaceutical Co., Ltd. |
February 1, 2019 | Phase 3 |
| NCT02856893 | Active Recruiting |
Drug: Gefitinib Drug: Osimertinib |
NSCLC | European Organisation for Research and Treatment of Cancer - EORTC |
October 10, 2017 | Phase 2 |
A, effect of metformin (MET) alone and in combination with gefitinib (GEF) on cell proliferation, on anchorage-independent growth ability of NSCLC cell lines, and on the induction of apoptosis in CALU-3, CALU-3 GEF-R, and H1299 cell lines.Clin Cancer Res.2013 Jul 1;19(13):3508-19. |
Effects on the downstream pathway by combined treatment of metformin and gefitinib. Western blotting of EGFR, MAPK, AKT p70S6K, and S6 activation following treatment with the indicated concentration of metformin and gefitinib in CALU-3 and CALU-3 GEF-R cell lines. β-Actin was included as a loading control.Clin Cancer Res.2013 Jul 1;19(13):3508-19. |
Effects of the combination treatment of metformin and gefitinib on NSCLC tumor xenografts.Clin Cancer Res.2013 Jul 1;19(13):3508-19. |
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