Gefitinib (ZD1839)

Catalog No.S1025

Gefitinib (ZD1839) Chemical Structure

Molecular Weight(MW): 446.90

Gefitinib (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.

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Cited by 91 Publications

12 Customer Reviews

  • Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1.

    Mol Syst Biol 2011 7, 486. Gefitinib (ZD1839) purchased from Selleck.

    Effects of shRNA-mediated RECK depletion on EGFR signaling in MEFs. (a) Immunoblotting (IB) of the indicated proteins in wild-type MEFs transduced with the indicated shRNAs and cultured for 48 h in the presence of 0.1% dimethyl sulfoxide (DMSO; vehicle) or 1 mM gefitinib (S1025, Selleck Chemicals,Houston, TX, USA). (b) Immunoprecipitation from whole lysates of cells from panel a with an anti-phosphorylated tyrosine (pTyr) antibody. Precipitates from 500 mg protein in whole cell lysates (upper) or 20 mg protein in whole cell lysates (lower) were analyzed by IB with anti-EGFR antibody.

    Oncogene 2010 30, 737-750. Gefitinib (ZD1839) purchased from Selleck.

  • (B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 μg). The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 lM) and Bortezomib (20 μM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.

    Carcinogenesis 2010 31, 1948–1955 . Gefitinib (ZD1839) purchased from Selleck.

    LNCaP-AI cells were starved in 1% stripped medium for 24 h. The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) for 24 h. Cell culture medium was collected from each sample and subjected to ELISA for sPLA2-IIa. The condition medium samples were diluted 10 times for ELISA. Average of duplicate samples was converted to nanogram per milliliter against standard curve. The data represent one of five repeated experiments.

     

     

    Carcinogenesis 2010 31, 1948–1955. Gefitinib (ZD1839) purchased from Selleck.

  • Susceptibility of lung cancer cells to cytolytic activity of NK-92 cells after treatment with EGFR inhibitors. Three lung cancer cells were untreated (open circle) or treated with 10 μM erlotinib or gefitinib (black filled square or black filled triangle) for 24 hours. The lung cancer cells were cocultured with NK-92 cells at indicated effector to target ratio (E:T ratio). To determine the specificity of NKG2D-mediated cytolysis of lung cancer cells, NK-92 cells were preincubated with blocking mAb against NKG2D before the assay (gray filled square and triangle) and correspond-ing isotype mAb (open square and triangle).

    J Immunother 2011 34(4), 372-81. Gefitinib (ZD1839) purchased from Selleck.

    Suppression of EGFR signaling by Gefitinib is dose dependent and non- toxic at millimolar concentrations.Results from plaque reduction tests of Hep2 cells infected with VACV(12.5pfu/well) treated with a serial dilution of Gefitinib (1000-0.01 m) and analyzed for (A)proliferation as indicator of cytotoxicity,(B) IC50 of plaque size inhibition, (C)dose dependent inhibition of EGFR-ERK1/2signaling and VACV proteins by Western blot analysis (pEGFR detection was obtained from a different experiment with identicals ettings) and (D)dose dependent inhibition of orthopoxvirus genome replication by real-time PCR.Untreated VACV infectedcells and uninfected cells are shown as controls in the right panel.

    Antiviral Res 2010 89, 64-70. Gefitinib (ZD1839) purchased from Selleck.

  • A circular zone of EGFR activated but uninfected cells facilitate virus induced plaque development , efficiently blocked by Gefitinib. (A)Immun of luorescent staining of aplaque reduction tests with Hep2 cells 24,48,72 and 96 h after VACV infection (6.25pfu/chamber). VACV infected cells(green) were visualized by human IgG directed to orthopoxviruses (VIG) detected with a secondary FITC labelled antibody. Uninfected cells with activated EGFR signaling(red) are detected with a secondary Cy3labelled antibody. Positive cells for both , VACV and phosphorylated EGFR are shown in yellow(merge). Cellular nuclei are counterstained with DAPI. (B)Immunofluorescent staining of a plaque reduction test as described for (A) and treated with three different Gefitinib concentrations (1000 nM, 1 nM, and 0.01 nM) . The test was analyzed 96h afterVACV infection.Uninfected cells are shown as controls. Magnification100×.(For interpretation of the references to color in this figure legend , the reader is referred to the web version of the article.)

     

     

    Antiviral Res 2010 89, 64-70. Gefitinib (ZD1839) purchased from Selleck.

    The EGF-dependent increased association of PCM1 and AZI1 requires EGFR kinase activity. ZD1839 (Iressa)—EGFR tyrosine kinase inhibitor.

    Mol Biosyst 2011 7, 3223-33. Gefitinib (ZD1839) purchased from Selleck.

  • Reduction of GPER expression in HCC1806 cells after treatment with gefitinib. (A) Concentration dependence. HCC1806 cells were treated with 50-500 nM gefitinib for 48 h. GPER was detected by western blotting. (B) Time dependence. HCC1806 cells were treated with 200 nM gefitinib for 24-96 h. ap<0.05 vs. control; bp<0.001 vs. control. Mean values and SE of three independent experiments are shown. (C) Representative western blotting of concentration dependence. (D) Representative western blotting of time dependence

    Oncol Rep, 2017, 37(2):1212-1218. Gefitinib (ZD1839) purchased from Selleck.

    Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.

    Int J Proteomics 2011 215496. Gefitinib (ZD1839) purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  Gefitinib for 24 hours.

     

     

    2010 Dr. Zhang of Tianjin Medical University. Gefitinib (ZD1839) purchased from Selleck.

    MTT assay result. 0-500nM Gefitinib treated with H1299, H358, H25 and HCC827 cell lines by 72h, Proliferation rate was tested.

     

     

    2010 Dr. Vicky Tin from University of Hong Kong. Gefitinib (ZD1839) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Gefitinib (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.
Features A potent EGFR tyrosine kinase inhibitor.
Targets
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB M4fu[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[wZ2RKSzVyPUCuNFU1KM7:TR?= NVjBWJJvOTZ3MU[0O|M>
NIH3T3 MYDGeY5kfGmxbjDBd5NigQ>? M{HSb|AvOiEQvF2= MmKxNkBp MmLsSG1UVw>? NYXwUnRoUW6qaXLpeIlwdiCxZjDFS2Yhe3SrbYXsZZRm\CCqdX3hckBmemKEMTDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxOFQh|ryP MlTsNVY1QDB{OES=
COS7 NILrVZNHfW6ldHnvckBCe3OjeR?= M{S5Vlk3KM7:TR?= NYDoRZZTUW6qaXLpeIlwdiCxZjDoeY1idiCMQVuyJHY3OTeIIH31eIFvfCCneIDy[ZN{\WR? NWXZVFZrOTdzN{i3NlI>
A549 NWD2W|Z4S3m2b4TvfIlkKEG|c3H5 M33JSFk3KGh? NHvSS5dFVVOR M1:0Z2lEPTB;MUOuOVkh|ryP NWfvdXYxOTh|MUO4NFc>
K562 NF\sW5FEgXSxdH;4bYMhSXO|YYm= MY[5OkBp NGHvUmxFVVOR NHX1eZdKSzVyPUmuN|Yh|ryP MmDJNVg{OTN6MEe=
MDA-MB-231 MXfDfZRwfG:6aXOgRZN{[Xl? M{fRW|k3KGh? NUTZ[HdGTE2VTx?= M2nQXmlEPTB;M{[uOlEh|ryP MUmxPFMyOzhyNx?=
MOLT4 MVzDfZRwfG:6aXOgRZN{[Xl? NEf3U206PiCq M{joU2ROW09? MWTJR|UxRTF3LkCyJO69VQ>? NWPsNlJ6OTh|MUO4NFc>
MCF7 M4PFWWN6fG:2b4jpZ{BCe3OjeR?= MU[1NEDPxE1? NXLOdZJXPzJiaB?= MULJR|UxRTF{LkC1JO69VQ>? NVvaTIFTOTh5N{G4NVk>
BT474 NES5d2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfZW4w4OiCq NUHFWVFOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFVmJjOiC5aYToJGVEPTBib3[gNE4{KM7:TR?= M4T3RlE6ODJ6NEK0
HN5 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH1O|IhcA>? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIIfpeIghTUN3MDDv[kAxNjBzIN88US=> MUCxPVAzQDR{NB?=
BA/F3 MYjDfZRwfG:6aXOgRZN{[Xl? NITZTHg4OiCq MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJibYX0ZY51KHerdHigTWM2OCCxZjCwMlAyODhizszN NFTMWFIyQTJ|OUKyPS=>
NIH3T3 NFG2eFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlKxO|IhcA>? M{X3U2dzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUC9|VEOgZ4VtdHNiZYjwdoV{e2mwZzDldmIzKGenbnWge4l1cCCLQ{WwJI9nKDBwNUSg{txO NYjrXGtmOTl4NkWzO|c>
MCF7 MX MkDGSpVv[3Srb36gRZN{[Xl? M4nZW|MxKG2rbh?= MVfJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzLkGg{txO M{PINlE6QTN{OU[w
A431 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HyWlExKM7:TR?= MmPSO|IhcA>? NXPOV|VUT0l3ME2wMlUyPCEQvF2= MV:xPVk3QTR4NR?=
A431 NHXhbJhMcW6jc3WgRZN{[Xl? NV74N3R4OC5zIN88US=> NGfqZmEyKGh? M{LqcWlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44> MkTjNVk6Pjl2NkW=
A431 MWjLbY5ie2ViQYPzZZk> M2\JdlExOCEQvF2= NYXXTlB1OTBibXnu MVHQdo9td26pZXSgbY5pcWKrdH;yfUBi[3Srdnn0fUBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvci=> NIO2[Y4yQTl4OUS2OS=>
Sf9 NX\PXZZYU2mwYYPlJGF{e2G7 Mn7XNVAhdWmw MnTPSG1UVw>? NHLhdYFKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN M{f4U|IxODV4NEK1
NCI-H1975 NXWwboFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnKOUDPxE1? MWG3NkBp NVftZZJyUUN3ME24MlI3KM7:TR?= NXfseFVTOjBzNUG2O|A>
NCI-H1975 NGT2WXpMcW6jc3WgRZN{[Xl? MWSxNEDPxE1? Mm\RTY5pcWKrdHnvckBw\iCHR1\SJIF2fG:yaH;zdIhwenmuYYTpc44> MXGyNFE2OTZ5MB?=
NCI-H1975 MlK2SpVv[3Srb36gRZN{[Xl? Ml20NVAh|ryP MonkTY5pcWKrdHnvckBw\iCHUlLCNkBifXSxcHjvd5Bpd3K7bHH0bY9v NEDJRm4zODF3MU[3NC=>
NCI-H1975 MU\GeY5kfGmxbjDBd5NigQ>? NEH5cWQ2KM7:TR?= M37YUVQ5KGh? M4m3OGlv\HWldHnvckBw\iCjcH;weI9{cXNiYYPz[ZN{\WRiYYOgZYN1cX[jdHnvckBw\iClYYPwZZNmNTN? MXyyNFE2OTZ5MB?=
A375 NX3uTZVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi0PEBp MnfYTWM2OD1{MD61OUDPxE1? M4nWOVIxOzB2NUO3
SMMC7721 M4j4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm0PEBp M2X6NGlEPTB;M{OuNVIh|ryP NXHNOFRHOjB|MES1N|c>
DU145 NULJVo1KS3m2b4TvfIlkKEG|c3H5 M4LMRVUh\A>? MYDEUXNQ M17LR2lEPTB;NEKuNVch|ryP Ml;kNlA1PjZ3NUW=
MIAPaCa2 MWjDfZRwfG:6aXOgRZN{[Xl? NEeweY82KGR? MWXEUXNQ M{PzUWlEPTB;NUCuOlIh|ryP M{TTUFIxPDZ4NUW1
PANC1 MUDDfZRwfG:6aXOgRZN{[Xl? M2GwbVUh\A>? MWLEUXNQ NGDjbYRKSzVyPUSwMlQzKM7:TR?= Ml7ONlA1PjZ3NUW=
PC9 NEXaeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGryW4tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVITlJvZHXmbYNq\W62IHj1cYFvKFCFOTDj[YxteyC5aYToJGVEPTBib3[gNE4xOTdizszN M{\5fVIyOjB6OECy
PC9 NFvjN|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfyc5d1cC2{ZYPpd5RidnRiaIXtZY4hWEN7IHPlcIx{KGW6cILld5NqdmdiRVfGVkBGPzR4X1G3OVAwXDd7MF2gcZV1[W62IIfpeIghTUN3MDDv[kA4KM7:TR?= NF;0TIQzOTJyOEiwNi=>
PC3 NVyxOo52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nmPVExKM7:TR?= MmDFO|IhcA>? NHfPcFdFVVOR NW\1epl2UUN3ME23MlQh|ryP MmniNlE{PTN3NE[=
MDA-MB-468 Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj4e2VLOTByIN88US=> NVmzSpJSPDhiaB?= NEi4NnFFVVOR M3nCRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5 MX2yNVQzQTZ|Mh?=
Plasmodium falciparum NEjzbJRyUFSVIIDyc4ZqdGmwZzDmc5IhcW6qaXLpeI9zeyCxZjDQcIF{dW:maYXtJIZidGOrcHHyeY0heHKxbHnm[ZJifGmxbh?= NE\xSIMzOThzN{C0OS=>
NCI-H1993 NVvBdlR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLxO|IhcA>? Ml7qSG1UVw>? M{OzeWlEPTB;MD6xJO69VQ>? M3PnZ|IyQTF4NEOz
NCI-H292 MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWm3NkBp NY\v[WhmTE2VTx?= MkTuTWM2OD1yLkCyJO69VQ>? MV6yNVkyPjR|Mx?=
A431 NGfDVmpMcW6jc3WgRZN{[Xl? MX[yJIg> MU\EUXNQ NHfHem1KdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIFG0N|Ehf2m2aDDJR|UxKG:oIECuNFAyKM7:TR?= MnvENlIyODFzM{K=
MCF7 M3nGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTaNVAxyqEQvHevcWw> NHfaS3g1QCCq NWnlS2R2TE2VTx?= MkTCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKg[4Vv\SC5aYToJGlEPTBib3[gNVIvODVizszN NVHw[XBJOjJzMUmxN|A>
BT474 Ml3yR5l1d3SxeHnjJGF{e2G7 NH;aeYoyOCEQvF2= M4XlNVQ5KGh? NHTPR5VEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIFLUOFc1KGOnbHzz M{[yWVIzOTN6M{C4
MCF7 MoTxR5l1d3SxeHnjJGF{e2G7 MU[xNEDPxE1? MVO0PEBp NGTSbXhEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIF3DSlch[2WubIOgc5Zmei2neIDy[ZN{cW6pIFXyZmIzKGOnbHzz MmPxNlIyOzh|MEi=
HCC827 NILDUW9McW6jc3WgRZN{[Xl? M3\VN|AvOTJ3IN88US=> NFPMcYwzPCCq NEHQe5VFVVOR NH65PGFKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRiWUGwOlgh[XW2b4Doc5NxcG:{eXzheIlwdg>? M4j3O|IzOzN7M{Sy
HCC827 MX\LbY5ie2ViQYPzZZk> M{LyNVAvOTJ3IN88US=> MonzNlQhcA>? M3;VXWROW09? M1zRN2lvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfC2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:w MWSyNlM{QTN2Mh?=
HCC827 M{n2PGtqdmG|ZTDBd5NigQ>? MW[wMlEzPSEQvF2= NVnEUohkOjRiaB?= M163TmROW09? NUO2U3VCUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFHreEBxcG:|cHjvdplt[XSrb36= NGPxfHMzOjN|OUO0Ni=>
A431 MoG2T4lv[XOnIFHzd4F6 NW\KRZFMOTByIN88US=> MlXVN|AhdWmw NHPyeYVKdmirYnn0bY9vKG:oIFXHSnIh\GW{aY\l[EBnem:vIHj1cYFvKEF2M{GgZ4VtdCCvZX3idoFv\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHCxbImtS4x2NVS7cjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEvODhizszN Mk[4NlI3QTh5OEK=
H460 NGi0SnBEgXSxdH;4bYMhSXO|YYm= NGDiU484OiCq M36ybmlEPTB;NT61PUDPxE1? NGrI[G4zOjd{N{S0PS=>
HT-29 MlfLR5l1d3SxeHnjJGF{e2G7 MlfFO|IhcA>? MULJR|UxRTNwM{[g{txO MUeyNlczPzR2OR?=
SGC7901 NXTodWNVS3m2b4TvfIlkKEG|c3H5 MVy3NkBp M2[3ZmlEPTB;MUCuNlYh|ryP Mn24NlI4Ojd2NEm=
A498 MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKGGwZDDTVmMhf2m2aDDJR|UxKG:oIEiuOkDPxE1? NV;M[FhCOjJ6MUi4OFg>
Calu3 M2TNOGN6fG:2b4jpZ{BCe3OjeR?= MUSxNEDPxGdxbVy= NWHaV2gzPzJiaB?= M121[WlEPTB;MT62JO69VQ>? NHXMRW8zOzFzNkG2PC=>
FADU NHTYOZhEgXSxdH;4bYMhSXO|YYm= MnfkNVAh|rypL33M MUS3NkBp NHm1VHlKSzVyPUCuNFUh|ryP MVSyN|EyPjF4OB?=
HCC827 NIr1ZYNEgXSxdH;4bYMhSXO|YYm= M4DCWFExKM7:Zz;tUC=> NYXYSmd4PzJiaB?= MoL1TWM2OD1yLkCwNVUh|ryP M3\jSFI{OTF4MU[4
PC9 M1XBOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixNEDPxGdxbVy= NUH4PW9HPzJiaB?= MX;JR|UxRTBwMECxOEDPxE1? M1vXTlI{OTF4MU[4
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16HBE14o- MVXDfZRwfG:6aXOgRZN{[Xl? NIW1dlgyOCEQvF2= NWf0[|BEPzJiaB?= MXTEUXNQ NYjmZ|A1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMUKuO|Eh|ryP MUKyN|Y3QDR2MR?=
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CAL-72 M4nR[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTtd3BKSzVyPUK2PE44OyCwTR?= M{XwfXNCVkeHUh?=
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LU-139 NVrBN|ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y0VWlEPTB;ND6zO|I1PyEQvF2= M1XiWXNCVkeHUh?=
HCC1937 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\EOHJKSzVyPUSuN|c6QTNizszN NHTvTHNUSU6JRWK=
GR-ST Mkj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnPWpZCUUN3ME20MlQ{OThizszN NG\tdFVUSU6JRWK=
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BFTC-905 M4PYRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK5c4RKSzVyPUWuOlU5PzhizszN NH6zU2xUSU6JRWK=
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HD-MY-Z MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTVwNki1PFEh|ryP MUHTRW5ITVJ?
HCC1187 Ml64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTVwN{GwN|Ih|ryP NHj1PYJUSU6JRWK=
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RT-112 M3vmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPHTWM2OD13LkmwNlQ2KM7:TR?= MnXNV2FPT0WU
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TE-10 NHO0bFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTZwMES4N|Mh|ryP MljUV2FPT0WU
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SK-MEL-28 NID2UoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX2TWM2OD14LkKwPVY4KM7:TR?= MX\TRW5ITVJ?
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CAL-120 NH76cHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfUTWM2OD14LkS1NVYzKM7:TR?= M{jISHNCVkeHUh?=
GAMG M{TSS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\udGlEPTB;Nj61NFYzKM7:TR?= NH75TZpUSU6JRWK=
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GCT MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTZwNUOzPFch|ryP MlXvV2FPT0WU
SH-4 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PaTGlEPTB;Nj61PFg1PCEQvF2= M{DDUXNCVkeHUh?=
Calu-3 M4f5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jpV2lEPTB;Nj62OVU3QCEQvF2= NEC5VGNUSU6JRWK=
SK-HEP-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETHfG9KSzVyPU[uO|E4PTNizszN MkLIV2FPT0WU
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NB12 NF7RV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\5TWM2OD14Lke4OFA1KM7:TR?= M1\kUXNCVkeHUh?=
A388 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYWwS2YxUUN3ME22Mlg6PTJizszN MXvTRW5ITVJ?
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TE-11 NHHHOGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTvTWM2OD15LkC0PVY4KM7:TR?= NIniVHJUSU6JRWK=
NCI-H2405 NH;VXlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXzTWM2OD15LkC4N|k{KM7:TR?= NUTYWmQ2W0GQR1XS
OVCAR-4 NFfBPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTdwMUWzOUDPxE1? M{H5THNCVkeHUh?=
KP-N-YS M2Xxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdwMUixOEDPxE1? M4PFbnNCVkeHUh?=
NOS-1 NIPu[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLyTWM2OD15LkK1PFI5KM7:TR?= NIrjO|NUSU6JRWK=
DMS-114 NFLo[4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\VTWM2OD15LkK5OlMyKM7:TR?= NEHCfGNUSU6JRWK=
NCI-H2030 NFLweoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTlTWM2OD15LkOzOlk5KM7:TR?= M3XTUHNCVkeHUh?=
HEL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnwTWM2OD15LkO3OVIyKM7:TR?= NI\x[mJUSU6JRWK=
CAL-62 NEPuS5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTdwM{m4OlYh|ryP M1fRXHNCVkeHUh?=
COLO-668 M4\mb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrYdGlSUUN3ME23MlQ{QTZ5IN88US=> M4fNfHNCVkeHUh?=
SKG-IIIa MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXLTZhKSzVyPUeuOFU{QDFizszN Ml;qV2FPT0WU
HCC1419 NXPYUVBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTrN2pRUUN3ME23MlQ3QDN|IN88US=> MX;TRW5ITVJ?
OS-RC-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW2TW81UUN3ME23MlQ6QDl2IN88US=> MXXTRW5ITVJ?
COLO-829 NYrqS|lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXYTWM2OD15Lk[2OFY{KM7:TR?= NWLF[WJnW0GQR1XS
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NCI-H510A MkH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjjSWl1UUN3ME2zPE43PDVzIN88US=> NFnXS|JUSU6JRWK=
NMC-G1 NVvzR|FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTN6LkeyNlIh|ryP M4HTOHNCVkeHUh?=
SW948 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLzTWM2OD1|OD64PVQ6KM7:TR?= M{HDZnNCVkeHUh?=
MFM-223 NF32XXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrofIlKSzVyPUO4Mlk1OzFizszN NFLtOmVUSU6JRWK=
PAN1 NELaeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHROVdNUUN3ME2zPE46QTF7IN88US=> MV\TRW5ITVJ?
MZ7-mel M2jVO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe1O4dKSzVyPUO5MlEyQTlizszN NYrNV2s4W0GQR1XS
COLO-679 NUPnb3FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjYNGg6UUN3ME2zPU46PzB6IN88US=> MXvTRW5ITVJ?
SW872 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTRyLkKwN|Eh|ryP NIXucIRUSU6JRWK=
HT-1197 NHHZfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HJfGlEPTB;NECuNlg3QSEQvF2= NEjSOG9USU6JRWK=
ES6 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4O3cmlEPTB;NECuOFU2OiEQvF2= MV3TRW5ITVJ?
SNU-387 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K5emlEPTB;NECuPFI{QCEQvF2= MV;TRW5ITVJ?
T47D NEHBd3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGwc3NKSzVyPUSxMlAyQTJizszN M4nj[3NCVkeHUh?=
G-402 NHXaPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTRzLkC4NFkh|ryP MoK3V2FPT0WU
MZ1-PC MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\wTWM2OD12MT64NUDPxE1? NHu4Rm1USU6JRWK=
SW1417 M1HMN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTR{LkOwN{DPxE1? NX22[|ZEW0GQR1XS
RERF-LC-MS MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr2SI1KSzVyPUSyMlUxQDdizszN NYTPZWx2W0GQR1XS
SF539 NV3nfnBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DWV2lEPTB;NEKuOVUzQSEQvF2= NYnZ[3VZW0GQR1XS
ESS-1 M2XqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLLRm9KSzVyPUSzMlU2PThizszN NX;PeVllW0GQR1XS
RO82-W-1 MlfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjReXdKSzVyPUSzMlYyPTNizszN M2S2bnNCVkeHUh?=
S-117 M4\nSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37W[WlEPTB;NEOuOlk2QCEQvF2= NH7ENVZUSU6JRWK=
SW756 M2P4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEeyb2lKSzVyPUSzMlgzPDJizszN NVnnbpFVW0GQR1XS
CP66-MEL NV3ie5JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR3LkexOFMh|ryP NF;0Z3NUSU6JRWK=
H-EMC-SS NHTWe4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfIOIxKSzVyPUS1Mlc3QTNizszN MVXTRW5ITVJ?
NCI-H2052 MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyyXHpKSzVyPUS1MlkxOjdizszN MoTNV2FPT0WU
SW684 NHm5eIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr1PYpKSzVyPUS3MlAxQDFizszN NITaZmlUSU6JRWK=
HCC1569 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X1Z2lEPTB;NEeuNVY2QCEQvF2= MWfTRW5ITVJ?
KGN MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHBdW1KSzVyPUS3MlM{OTFizszN NV3rO2pzW0GQR1XS
LCLC-103H M{PZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjTdYp3UUN3ME20O{41PDB2IN88US=> NEfJSpdUSU6JRWK=
SW780 M{\YXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TGXmlEPTB;NEeuOlM2OSEQvF2= NUH6e4lRW0GQR1XS
NCI-H1703 NFnybWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7jZnpKSzVyPUS4MlM{PTJizszN MoTXV2FPT0WU
HCC1395 MnPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnIVIhRUUN3ME20PE44PDN{IN88US=> M3z5OXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (199.14 mM)
Ethanol 4 mg/mL (8.95 mM)
Water <1 mg/mL
In vivo 5% DMSO+corn oil 2.5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 446.90
Formula

C22H24ClFN4O3

CAS No. 184475-35-2
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03050164 Completed Bioequivalence Study Hunan Kelun Pharmaceutical Co., Ltd. September 8, 2016 Phase 1
NCT02856893 Not yet recruiting NSCLC European Organisation for Research and Treatment of Cancer - EORTC|AstraZeneca March 2017 Phase 2
NCT02976116 Recruiting NSCLC Hutchison Medipharma Limited December 2016 Phase 2
NCT02951637 Not yet recruiting Lung Adenocarcinoma Shanghai Chest Hospital|Ruijin Hospital|Changhai Hospital December 2016 Phase 2
NCT02930954 Not yet recruiting Non-small-cell Lung Cancer Caicun Zhou|Tongji University November 2016 Phase 2
NCT02929693 Enrolling by invitation Cancer Shanghai University of Traditional Chinese Medicine|Shanghai Chest Hospital|Shanghai Pulmonary Hospital, Shanghai, China October 2016 Phase 3

Tech Support

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:3

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID