Gefitinib hydrochloride (Synonyms: ZD-1839 hydrochloride)

Name: Gefitinib hydrochloride
Brand: MedChemExpress
SKU: HY-50895A
Rating: 5.0 (142 reviews)

Cat. No.: HY-50895A Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Gefitinib hydrochloride Chemical Structure

CAS No. : 184475-55-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
1 g	USD 90	In-stock	Estimated Time of Arrival: December 31
5 g	USD 180	In-stock	Estimated Time of Arrival: December 31
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Based on 142 publication(s) in Google Scholar

Other Forms of Gefitinib hydrochloride:

Gefitinib In-stock
Gefitinib dihydrochloride Get quote

132 Publications Citing Use of MCE Gefitinib hydrochloride

Cell Viability Assay

: Gefitinib hydrochloride purchased from MedChemExpress. Usage Cited in: Kaohsiung J Med Sci. 2023 Apr 14. [Abstract]; Gefitinib (0-20 μM; 24 h) significantly inhibits the viability of A549 cells.

: 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.

: 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.

: 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.

: 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).

: 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.

: 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.

: 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.

: 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).

: 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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References
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Description

IC₅₀ & Target^[1]

EGFR

In Vitro

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.

In Vivo

Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts^[3]. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

483.36

Formula

C₂₂H₂₅Cl₂FN₄O₃

CAS No.

184475-55-6

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0689 mL	10.3443 mL	20.6885 mL
5 mM	0.4138 mL	2.0689 mL	4.1377 mL
10 mM	0.2069 mL	1.0344 mL	2.0689 mL

View the 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.

* 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.85%

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Data Sheet (283 KB) SDS (394 KB)

COA (252 KB) LCMS (94 KB)

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]

Cell Assay ^[3]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]^[4]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

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.

Gefitinib hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gefitinib184475-55-6ZD-1839ZD1839ZD 1839EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Gefitinib hydrochloride (Synonyms: ZD-1839 hydrochloride)

Customer Review

Other Forms of Gefitinib hydrochloride:

Gefitinib hydrochloride Related Antibodies

132 Publications Citing Use of MCE Gefitinib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Gefitinib hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Gefitinib hydrochloride Related Classifications

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