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Gefitinib (Iressa)

Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

Catalog No.S1025

11 Reviews 28 Product Citations

: Tel: +1-832-582-8158[email protected]

Gefitinib (Iressa) Chemical Structure
Molecular Weight: 446.90

Validation & Quality Control

Product Citations(28)

Nature, 2012, 483(7387), 100-103

Cell, 2012, 151(5):937-50

Mol Syst Biol, 2011, 7, 486

Cell Death Differ, 2012, 19(12):1908-16

Oncogene, 2011, 30(6), 737-750
Ann Oncol, 2013, 24(2):362-9

Oncogene, 2012, ahead of print

Int J Cancer, 2012, 131(12):2961-9

Int J Cancer, 2012, 131(2):334-43

Carcinogenesis, 2010, 31(11), 1948-1955
Int J Proteomics, 2011, 2011, 215496

Mol Oncol, 2013, 7(1):121-9

Cancer Lett, 2012, 321(2), 187-194

Biochem Pharmacol, 2012, 84(4):425-31

Cancer Res Treat, 2012, 44(3):202-9
Antiviral Res, 2011, 89(1), 64-70

PLoS One, 2012, 7(9):e42441

PLoS One, 2012, 7(12), e51549

Mol Biosyst, 2011, 7(12):3223-33

Cancer Sci, 2012, 103(1):7-16
J Immunother, 2011, 34(4):372-81

Cancer Discov, 2011, 1(7):608-25

Cancer Discov, 2012, 2(10), 934-947

Int J Mol Sci, 2012, 13(9):12000-16

Exp Mol Pathol, 2011, 91(1):400-10
Exp Mol Pathol, 2013, ahead of print

Vet Comp Oncol, 2011, ahead of print

Oncotarget, 2012, 2(12), 1134-1144

Customer Reviews(11) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

Gefitinib (Iressa) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Chemotherapeutic Agent Library (96-well) FDA Approved Drug Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

Compare EGFR Inhibitors

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Research Area

Cat.No.	Product Name	Solubility (25°C)
S1023	Erlotinib HCl	<1 mg/mL	3 mg/mL	<1 mg/mL
S1025	Gefitinib (Iressa)	<1 mg/mL	89 mg/mL	4 mg/mL
S1028	Lapatinib Ditosylate (Tykerb)	<1 mg/mL	185 mg/mL	<1 mg/mL
S1011	Afatinib (BIBW2992)	<1 mg/mL	97 mg/mL	15 mg/mL
S1143	AG-490	<1 mg/mL	59 mg/mL	6 mg/mL
S2111	Lapatinib	<1 mg/mL	100 mg/mL	<1 mg/mL
S1167	CP-724714	<1 mg/mL	94 mg/mL	94 mg/mL
S2727	Dacomitinib (PF299804,PF-00299804)	<1 mg/mL	19 mg/mL	<1 mg/mL
S2728	AG-1478 (Tyrphostin AG-1478)	<1 mg/mL	25 mg/mL	13 mg/mL
S1019	CI-1033 (Canertinib)	<1 mg/mL	2 mg/mL	9 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S2150	Neratinib (HKI-272)	<1 mg/mL	2 mg/mL	<1 mg/mL
S1173	WZ4002	<1 mg/mL	13 mg/mL	<1 mg/mL
S1392	Pelitinib (EKB-569)	<1 mg/mL	13 mg/mL	<1 mg/mL
S2192	AZD8931	<1 mg/mL	40 mg/mL	<1 mg/mL
S2185	AST-1306	<1 mg/mL	124 mg/mL	<1 mg/mL
S2752	Arry-380	<1 mg/mL	114 mg/mL	<1 mg/mL
S1079	PD153035 HCl	<1 mg/mL	0.5 mg/mL	<1 mg/mL
S2755	ARRY334543	<1 mg/mL	6 mg/mL	<1 mg/mL
S2867	WHI-P154	<1 mg/mL	75 mg/mL	<1 mg/mL
S1179	WZ8040	<1 mg/mL	96 mg/mL	3 mg/mL
S2205	OSI-420	2 mg/mL	83 mg/mL	<1 mg/mL
S1056	BMS-599626 (AC480)	<1 mg/mL	113 mg/mL	20 mg/mL
S1486	AEE788 (NVP-AEE788)	<1 mg/mL	88 mg/mL	<1 mg/mL
S2784	TAK-285	<1 mg/mL	110 mg/mL	54 mg/mL
S2826	Desmethyl Erlotinib (CP-473420)	<1 mg/mL	11 mg/mL	5 mg/mL
S8009	AG 18 (Tyrphostin 23)	<1 mg/mL	37 mg/mL	37 mg/mL
S1170	WZ3146	<1 mg/mL	93 mg/mL	<1 mg/mL
S2895	Tyrphostin 9 (SF 6847)	<1 mg/mL	56 mg/mL	56 mg/mL
S2922	Icotinib	<1 mg/mL	78 mg/mL	7 mg/mL

Combination Therapy

Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	Gefitinib (Iressa, ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
Targets	Tyr1173 (NR6wtEGFR cells)	Tyr992 (NR6wtEGFR cells)	Tyr1173 (NR6W cells)	Tyr992 (NR6W cells)
IC50	37 nM	37nM	26 nM	57 nM ^[1]
In vitro	Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. ^[1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. ^[2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. ^[3]
In vivo	Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. ^[3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. ^[4]
Clinical Trials	Gefitinib has entered in a phase II clinical trial in the treatment of non small cell lung cancer.
Features	Gefitinib is a potent EGFR tyrosine kinase inhibitor.

Protocol(Only for Reference)

Cell Assay: ^[1]

Cell lines	NR6, NR6M and NR6W cells
Concentrations	0-2 μM
Incubation Time	72 hours
Method	Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.

Animal Study: ^[3]

Animal Models	Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
Formulation	0.5% polysorbate
Dosages	100 mg/kg
Administration	Once daily by oral administration (0.1 mL/10 g body weight) for 14 days

References

Chemical Information

Download Gefitinib (Iressa) SDF

Molecular Weight (MW)	446.90
Formula	C₂₂H₂₄ClFN₄O₃
CAS No.	184475-35-2, 184475-55-6 (HCl)
Synonyms	ZD-1839

Solubility (25°C) DMSO 89 mg/mL Water <1 mg/mL Ethanol 4 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (11)

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Rating

Source

Mol Biosyst, 2011, 7(12), 3223-33. Gefitinib (Iressa) purchased from Selleck

Method

Immunoprecipitation/Western blotting

Cell Lines

Concentrations

5 μM

Incubation Time

0-1 h

Results

In the presence of the EGFR tyrosine kinase inhibitor Z D1839 (Iressa) revealed that the observed increase in binding between PCM1 and Azi1 is specific to EGFs timulation and requires E GFR activation.

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Rating

Source

J Immunother, 2011, 34(4), 372-81.. Gefitinib (Iressa) purchased from Selleck

Method

Cytotoxicity assay

Cell Lines

NK-92 cells/ lung cancer cells

Concentrations

10 μM

Incubation Time

24 h

Results

Susceptibility of lung cancer cells to cytolytic activity of NK cells was significantly increased by treatment with EGFR inhibitors (erlotinib/gefitinib) and was reversed by blocking step using mAb against NKG2D before the assay in all lung cancer cells.

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Rating

Source

Int J Proteomics , 2011, 2011, Article ID 215496. Gefitinib (Iressa) purchased from Selleck

Method

CEER assay

Cell Lines

H358 cell line

Concentrations

0.01-10 μM

Incubation Time

4 h

Results

HER1 and/or HER2 pathway-activated cell lines, H358 , had their activation blocked by the HER1/2 kinase inhibitors Gefitinib.

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Rating

Source

Antiviral Res, 2010, 89, 64-70. Gefitinib (Iressa) purchased from Selleck

Method

Proliferation assay, Plaque reduction test, Western blot, Real-time PCR

Cell Lines

Hep2 cells

Concentrations

0.01-1000 μM

Incubation Time

Results

While for Gefitinib concentrations between 100 μM and 0.01 μM the proliferation rate was almost 100% of the controls, only at concentrations of 1000 μM a slight (24%) decline in proliferation was observed (Fig.A). IC50 values of Gefitinib for plaque size reduction were calculated by dividing plaque size by total size of one tissue culture plate well for each compound concentration. A non-linear regression fit curve analysis from the calculated values revealed for plaque size reduction an IC50 value of 4.93μM for Gefitinib(Fig. B).The analysis of phosphorylated EGFR and of the downstream signaling kinases ERK1/2 in cell lysates of the assay confirmed the dose dependency of the antiviral effect of Gefitinib. Kinase activ-ities were completely suppressed at concentrations above 1μM as determined by Western blot analysis. VACV proteins were not detectable between 10 μM and 100 μM in Western blot analysis anymore (Fig. C).

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Rating

Source

Carcinogenesis, 2010, 31, 1948–1955. Gefitinib (Iressa) purchased from Selleck

Method

Luciferase assay

Cell Lines

LNCaP-AI cells, LNCaP cells

Concentrations

20 μM

Incubation Time

24 h

Results

EGF significantly stimulates the promoter activity of sPLA2-IIa gene in both LNCaP and LNCaP-AI cells (shown in LNCaP-AI cells), whereas Gefitinib and other inhibitors all tested downregulated the promoter activity both at the basal level (shown in LNCaP cells) and in response to EGF stimulation (shown in LNCaP-AI cells)

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Rating

Source

Dr Zhang of Tianjin Medical University. Gefitinib (Iressa) purchased from Selleck

Method

Western blot

Cell Lines

Breast cancer cells

Concentrations

0-5 nM

Incubation Time

24 h

Results

Click to enlarge

Rating

Source

Dr Vicky Tin from University of Hong Kong. Gefitinib (Iressa) purchased from Selleck

Method

MTT assay

Cell Lines

H1299 cells, H358 cells, H25 cells, HCC827 cells

Concentrations

0-400 nM

Incubation Time

72 h

Results

Click to enlarge

Rating

Source

Mol Syst Biol , 2011, 7, 486. Gefitinib (Iressa) purchased from Selleck

Method

qPCR analysis

Cell Lines

glioblastoma cell lines

Concentrations

5 μM, 50 ng/ml

Incubation Time

6 h

Results

We perturbed the activity of the EGFR by activating it using one of its ligands (EGF) and inhibiting it with a selective EGFR inhibitor (Gefitinib). As readout, we measured the transcriptional effect on SOCS2 (a modulator of STAT signaling), NR2E1(also known as TLX , a transcription factor believed to be important for neural stem cell renewal), yielding results compatible with a coupling between hub perturbation and transcriptional response.

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Rating

Source

Oncogene, 2010, 30, 737-750. Gefitinib (Iressa) purchased from Selleck

Method

Western blot

Cell Lines

MEFs

Concentrations

1 μM

Incubation Time

48 h

Results

We found that gefitinib, a specific EGFR inhibitor, almost completely recapitulated the results obtained by genistein (Figure a). Consistent with these results, we observed increased EGFR phosphorylation within 2 days of RECK depletion , with insignificant change in its protein amount (Figure b).

Click to enlarge

Rating

Source

Antiviral Res, 2010, 89, 64-70. Gefitinib (Iressa) purchased from Selleck

Method

Immunofluorescence

Cell Lines

Hep2 cells

Concentrations

0.01-1000 nM

Incubation Time

96 h

Results

As shown in Fig. A, an immunofluorescent staining of a plaque reduction test was performed 96 h after viral infection. VACV infected cells were treated with 1000 μM, 1 μM or 0.01 μM Gefitinib and compared to uninfected cells after 96 h incubation. At concentrations of 1000 μM Gefitinib virus induced plaques were rarely found in cell culture and infected cells only could be identified by fluorescent staining of orthopoxvirus proteins (green) but not by light microscopy. At this Gefitinib concentration EGFR phosphorylation was completely suppressed in the cells and even the uninfected, untreated control cells show a stronger pEGFR signal (control, red). Occasionally found plaques, visible by flourescence microscopy only, showed a very compact shape with minimal disruption in its center. At the lower Gefitinib concentrations plaques showed an increasing number of infected and pEGFR positive cells (merge, yellow) and a surround-ing small zone of solely pEGFR positive cells (red). The lower the Gefitinib concentration the more plaques with a disrupted center were observed (1μM and 0.01μM). Most of the cells localized in the center of the plaque were positive for orthopoxvirus infection but negative for pEGFR ( Fig. B).

Click to enlarge

Rating

Source

Carcinogenesis, 2010, 31, 1948–1955. Gefitinib (Iressa) purchased from Selleck

Method

ELISA

Cell Lines

LNCaP-AI cells

Concentrations

20 μM

Incubation Time

24 h

Results

Lapatinib, LY294002 and Bortezomib significantly inhibited sPLA2-IIa secretion, whereas Erlotinib, Gefitinib and CI-1033 had a moderate effect in LNCaP-AI cells .

Product Citations (28)

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. [Prahallad A, et al. Nature 2012;483(7387), 100-103]
PubMed: 22281684
MED12 controls the response to multiple cancer drugs through regulation of TGF-β receptor signaling. [Huang S, et al. Cell 2012;151(5):937-50]
PubMed: 23178117
Network modeling of the transcriptional effects of copy number aberrations in glioblastoma. [Jornsten R, et al. Mol Syst Biol 2011;7, 486]
PubMed: 21525872

Control of FLIPL expression and TRAIL resistance by the extracellular signal-regulated kinase1/2 pathway in breast epithelial cells. [Yerbes R, et al. Cell Death Differ 2012;19(12):1908-16]
PubMed: 22722337
Reversion-inducing cysteine-rich protein with Kazal motifs interferes with epidermal growth factor receptor signaling. [Kitajima S, et al. Oncogene 2011;30(6), 737-750]
PubMed: 20890302
ADAM-17: a novel therapeutic target for triple negative breast cancer. [McGowan PM, et al. Ann Oncol 2013;24(2):362-9]
PubMed: 22967992
Oncogenic KRAS-induced epiregulin overexpression contributes to aggressive phenotype and is a promising therapeutic target in non-small-cell lung cancer. [Sunaga N, et al. Oncogene 2012;ahead of print]
PubMed: 22964644
EGFR activation is a potential determinant of primary resistance of hepatocellular carcinoma cells to sorafenib. [Ezzoukhry Z, et al. Int J Cancer 2012;131(12):2961-9]
PubMed: 22514082
The intrinsic fusogenicity of glioma cells as a factor of transformation and progression in the tumor microenvironment. [Mercapide J, et al. Int J Cancer 2012;131(2):334-43]
PubMed: 21858806
Secretory phospholipase A2-IIa is involved in prostate cancer progression and may potentially serve as a biomarker for prostate cancer. [Dong Z, et al. Carcinogenesis 2010;31(11), 1948-1955]
PubMed: 20837598
Signatures of drug sensitivity in nonsmall cell lung cancer. [Gong HC, et al. Int J Proteomics 2011;2011, 215496]
PubMed: 22091388
EGFR mediates LPA-induced proteolytic enzyme expression and ovarian cancer invasion: Inhibition by resveratrol. [Jeong KJ, et al. Mol Oncol 2013;7(1):121-9]
PubMed: 23127547
The decrease of cell membrane fluidity by the non-steroidal anti-inflammatory drug Licofelone inhibits epidermal growth factor receptor signalling and triggers apoptosis in HCA-7 colon cancer cells. [Tavolari S, et al. Cancer Lett 2012;321(2), 187-194]
PubMed: 22343320
Cyclosporin A suppresses prostate cancer cell growth through CaMKKβ/AMPK-mediated inhibition of mTORC1 signaling. [Lee CR, et al. Biochem Pharmacol 2012;84(4):425-31]
PubMed: 22634404
Epidermal growth factor receptor: is it a feasible target for the treatment of osteosarcoma?. [Lee JA, et al. Cancer Res Treat 2012;44(3):202-9]
PubMed: 23091447
Inhibition of poxvirus spreading by the anti-tumor drug Geﬁtinib (IressaTM). [Langhammer S, et al. Antiviral Res 2011;89(1), 64-70]
PubMed: 21094187
An In Vivo C. elegans Model System for Screening EGFR-Inhibiting Anti-Cancer Drugs. [Bae YK, et al. PLoS One 2012;7(9):e42441]
PubMed: 22957020
Epithelial mesenchymal transition is required for acquisition of anoikis resistance and metastatic potential in adenoid cystic carcinoma. [Jia J, et al. PLoS One 2012;7(12), e51549]
PubMed: 23272116
Characterization of ubiquitination dependent dynamics in growth factor receptor signaling by quantitative proteomics [Akimov V, et al. Mol Biosyst 2011;7(12):3223-33]
PubMed: 21956701
Susceptibility to natural killer cell-mediated lysis of colon cancer cells is enhanced by treatment with epidermal growth factor receptor inhibitors through UL16-binding protein-1 induction. [Bae JH, et al. Cancer Sci 2012;103(1):7-16]
PubMed: 21951556
EGFR inhibitors enhanced the susceptibility to NK cell-mediated lysis of lung cancer cells. [Kim H, et al. J Immunother 2011;34(4):372-81]
PubMed: 21499124
Amplification of CRKL Induces Transformation and Epidermal Growth Factor Receptor Inhibitor Resistance in Human Non–Small Cell Lung Cancers. [Cheung HW, et al. Cancer Discov 2011;1(7):608-25]
PubMed: 22586683
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. [Ercan D, et al. Cancer Discov 2012;2(10), 934-947]
PubMed: 22961667
Anti-Epidermal Growth Factor Receptor (EGFR) Antibodies Overcome Resistance of Ovarian Cancer Cells to Targeted Therapy and Natural Cytotoxicity. [Gottschalk N, et al. Int J Mol Sci 2012;13(9):12000-16]
PubMed: 23109896
Small molecule inhibitors of the host cell COX/AREG/EGFR/ERK pathway attenuate cytomegalovirus-induced pathogenesis. [Melnick M, et al. Exp Mol Pathol 2011;91(1):400-10]
PubMed: 21565184
Cytomegalovirus-induced Salivary Gland Pathology: AREG, FGF8, TNF-α, and IL-6 Signal Dysregulation and Neoplasia. [Melnick M, et al. Exp Mol Pathol 2013;ahead of print]
PubMed: 23399805
Met interacts with EGFR and Ron in canine osteosarcoma. [McCleese JK, et al. Vet Comp Oncol 2011;ahead of print]
PubMed: 22235915
PIM kinase isoform specific regulation of MIG6 expression and EGFR signaling in prostate cancer cells. [Siu A, et al. Oncotarget 2012;2(12), 1134-1144]
PubMed: 22193779

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Related EGFR Inhibitors

Afatinib (BIBW2992)

BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively.
CI-1033 (Canertinib)

CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
BMS-599626 (AC480)

BMS-599626 (AC480) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, respectively.
PD153035 HCl

PD153035 is a potent and specific inhibitor of EGFR with K_i and IC50 of 5.2 pM and 29 pM, respectively.
XL647
XL647 is a novel spectrum-selective kinase inhibitor for EGFR, ErbB2, KDR, Flt-4 and EphB4 with IC50 of 0.3 nM, 16 nM, 1.5 nM, 8.7 nM and 1.4 nM, respectively.
AG-490
AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.
CP-724714

CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM and also inhibits EGFR with IC50 of 6.4 μM.
WZ3146

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM, respectively.
WZ4002

WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR^L858R and EGFR^L858R/T790M with IC50 of 2 nM and 8 nM, respectively.
WZ8040

WZ8040 is a novel mutant-selective irreversible EGFR^T790M inhibitor.

RTKs and Angiogenesis Related Products

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Gefitinib (Iressa) + Paclitaxel(Taxol)	Coadministration of Gefitinib, as with anti-EGFR, will enhance the efficacy of cytotoxic agents against human vulvar (A431), lung (A549 and SK-LC-16 NSCL and LX-1), and prostate (PC-3 and TSU-PR1) tumors. Although Paclitaxel or Docetaxel, as single agents markedly inhibits the growth of A431, LX-1, SK-LC-16, TSU-PR1, and PC-3, when combined with Gefitinib, partial or complete regression is usually seen. ^[5]
Gefitinib (Iressa) + Adriamycin	Against A549, the growth inhibition of Doxorubicin is increased 10-fold (>99%) with Gefitinib. ^[5]
Gefitinib (Iressa) + Docetaxel(Taxotere)	Coadministration of Gefitinib, as with anti-EGFR, will enhance the efficacy of cytotoxic agents against human vulvar (A431), lung (A549 and SK-LC-16 NSCL and LX-1), and prostate (PC-3 and TSU-PR1) tumors. Although Paclitaxel or Docetaxel, as single agents markedly inhibits the growth of A431, LX-1, SK-LC-16, TSU-PR1, and PC-3, when combined with Gefitinib, partial or complete regression is usually seen. ^[5]

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Gefitinib (Iressa)

Validation & Quality Control

Product Citations(28)

Customer Reviews(11) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

Gefitinib (Iressa) is available in the following compound libraries:

Product Information

Compare EGFR Inhibitors

Research Area

Combination Therapy

Product Description

Biological Activity

Protocol(Only for Reference)

Cell Assay: ^[1]

Animal Study: ^[3]

References

Chemical Information

Research Area

Customer Reviews (11)

Product Citations (28)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

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RTKs and Angiogenesis Related Products

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S8009	AG 18 (Tyrphostin 23)	<1 mg/mL	37 mg/mL	37 mg/mL
S1170	WZ3146	<1 mg/mL	93 mg/mL	<1 mg/mL
S2895	Tyrphostin 9 (SF 6847)	<1 mg/mL	56 mg/mL	56 mg/mL
S2922	Icotinib	<1 mg/mL	78 mg/mL	7 mg/mL

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Gefitinib (Iressa)

Validation & Quality Control

Product Citations(28)

Customer Reviews(11) in vivo invitation

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Combination Therapy

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Cell Assay: [1]

Animal Study: [3]

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Cell Assay: ^[1]

Animal Study: ^[3]