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 189 Publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

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 NFq2T3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfrTWM2OD1yLkC1OEDPxE1? NXr2[npEOTZ3MU[0O|M>
NIH3T3 M4f4e2Z2dmO2aX;uJGF{e2G7 MoP2NE4zKM7:TR?= M{jvdlIhcA>? NGXNW5RFVVOR MnHCTY5pcWKrdHnvckBw\iCHR1[gd5RqdXWuYYTl[EBpfW2jbjDldoJDOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNESg{txO MXWxOlQ5ODJ6NB?=
COS7 M4C0c2Z2dmO2aX;uJGF{e2G7 M3jr[|k3KM7:TR?= M4PEVWlvcGmkaYTpc44hd2ZiaIXtZY4hUkGNMjDWOlE4TiCvdYThcpQh\XiycnXzd4Vl M4Pze|E4OTd6N{Ky
A549 MVHDfZRwfG:6aXOgRZN{[Xl? MlHFPVYhcA>? NGfReGRFVVOR Mnf1TWM2OD1zMz61PUDPxE1? NIm1dGQyQDNzM{iwOy=>
K562 MnSwR5l1d3SxeHnjJGF{e2G7 MlTTPVYhcA>? M4XvUWROW09? MUHJR|UxRTlwM{[g{txO NUnyWVExOTh|MUO4NFc>
MDA-MB-231 NFrO[IZEgXSxdH;4bYMhSXO|YYm= NYHQd|NEQTZiaB?= NV21Z3V[TE2VTx?= M1X2RWlEPTB;M{[uOlEh|ryP MX[xPFMyOzhyNx?=
MOLT4 MnjQR5l1d3SxeHnjJGF{e2G7 M{Tq[Vk3KGh? MlrESG1UVw>? NXrpeYtKUUN3ME2xOU4xOiEQvF2= NITnPI0yQDNzM{iwOy=>
MCF7 NYH5T|hWS3m2b4TvfIlkKEG|c3H5 MWO1NEDPxE1? NVjmWpYxPzJiaB?= NHHHSZlKSzVyPUGyMlA2KM7:TR?= NGLhcHMyQDd5MUixPS=>
BT474 MnnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXpdXNEPzJiaB?= MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWUQnKyJJdqfGhiRVO1NEBw\iByLkOg{txO MojuNVkxOjh2MkS=
HN5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;aSo5[PzJiaB?= M37IemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKge4l1cCCHQ{WwJI9nKDBwMEGg{txO NHzEW5YyQTB{OESyOC=>
BA/F3 MVTDfZRwfG:6aXOgRZN{[Xl? NUDxTGVLPzJiaB?= NWnqeldCS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEx6NUjSJI12fGGwdDD3bZRpKEmFNUCgc4YhOC5yMUC4JO69VQ>? NWfaUIVjOTl{M{myNlk>
NIH3T3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj6c2I4OiCq M1vkPGdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUC9|VEOgZ4VtdHNiZYjwdoV{e2mwZzDldmIzKGenbnWge4l1cCCLQ{WwJI9nKDBwNUSg{txO NUXHV|lFOTl4NkWzO|c>
MCF7 MX NHvyRW1HfW6ldHnvckBCe3OjeR?= MlvDN|AhdWmw NHvkO5pKdmirYnn0bY9vKG:oIFLDVnAh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxMlEh|ryP NV;aWGdQOTl7M{K5OlA>
A431 M17pVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrWc4FsOTBizszN M1XqbFczKGh? NW\mV5l2T0l3ME2wMlUyPCEQvF2= M3TRTFE6QTZ7NE[1
A431 MkTnT4lv[XOnIFHzd4F6 MXuwMlEh|ryP NV\2R4RtOSCq M3fp[mlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44> NIHaOVMyQTl4OUS2OS=>
A431 NGLUcppMcW6jc3WgRZN{[Xl? NEPke2MyODBizszN NWf4TXRJOTBibXnu NFe1UHFRem:ub37n[YQhcW6qaXLpeI9zgSCjY4Tpeol1gSCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? NVT4R2xyOTl7Nkm0OlU>
Sf9 Mke5T4lv[XOnIFHzd4F6 NF;JR4syOCCvaX6= NEDB[WJFVVOR NEHrZXJKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN NYXaNFliOjByNU[0NlU>
NCI-H1975 NFXYOnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P4fFUh|ryP NXGzOVFjPzJiaB?= MXzJR|UxRThwMk[g{txO NFW3bpAzODF3MU[3NC=>
NCI-H1975 NGDCdZNMcW6jc3WgRZN{[Xl? MYWxNEDPxE1? NHvET|dKdmirYnn0bY9vKG:oIFXHSnIh[XW2b4Doc5NxcG:{eXzheIlwdg>? NHGzUmQzODF3MU[3NC=>
NCI-H1975 NWSyUVRXTnWwY4Tpc44hSXO|YYm= MYKxNEDPxE1? MmjmTY5pcWKrdHnvckBw\iCHUlLCNkBifXSxcHjvd5Bpd3K7bHH0bY9v M{LnUlIxOTVzNkew
NCI-H1975 M4j1WmZ2dmO2aX;uJGF{e2G7 MlLxOUDPxE1? M{jyUVQ5KGh? M3fr[Wlv\HWldHnvckBw\iCjcH;weI9{cXNiYYPz[ZN{\WRiYYOgZYN1cX[jdHnvckBw\iClYYPwZZNmNTN? MUiyNFE2OTZ5MB?=
A375 NYLUfIliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy0PEBp NVvvenVlUUN3ME2yNE42PSEQvF2= MWGyNFMxPDV|Nx?=
SMMC7721 NFTxb49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkOyOFghcA>? M3zR[mlEPTB;M{OuNVIh|ryP MXSyNFMxPDV|Nx?=
DU145 MVLDfZRwfG:6aXOgRZN{[Xl? NIH1boE2KGR? MmjZSG1UVw>? MVHJR|UxRTR{LkG3JO69VQ>? NYHJTGlYOjB2Nk[1OVU>
MIAPaCa2 NVTvXVFHS3m2b4TvfIlkKEG|c3H5 Mn\wOUBl Mk\CSG1UVw>? M4XkcGlEPTB;NUCuOlIh|ryP NUDzfWR2OjB2Nk[1OVU>
PANC1 MojCR5l1d3SxeHnjJGF{e2G7 NV\5XlQ3PSCm MXfEUXNQ MYTJR|UxRTRyLkSyJO69VQ>? M1LJSVIxPDZ4NUW1
PC9 NEXQNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnr5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFS2ZTNWSnZnnjbYVvfCCqdX3hckBRSzliY3XscJMhf2m2aDDFR|UxKG:oIECuNFE4KM7:TR?= MlLONlEzODh6MEK=
PC9 NHfiV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfyc5d1cC2{ZYPpd5RidnRiaIXtZY4hWEN7IHPlcIx{KGW6cILld5NqdmdiRVfGVkBGPzR4X1G3OVAwXDd7MF2gcZV1[W62IIfpeIghTUN3MDDv[kA4KM7:TR?= MorLNlEzODh6MEK=
PC3 MkX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnFWGU3OTBizszN NES1NIU4OiCq MYPEUXNQ MX3JR|UxRTdwNDFOwG0> M2r2PVIyOzV|NUS2
MDA-MB-468 M{\0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTkNVAxKM7:TR?= M3;NXlQ5KGh? NYfyd4hOTE2VTx?= NGPzTlFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fS=> MmHzNlE1Ojl4M{K=
Plasmodium falciparum MojHdWhVWyCycn;mbYxqdmdiZn;yJIlvcGmkaYTvdpMhd2ZiUHzhd41w\Gm3bTDmZYxkcXCjcoXtJJBzd2yrZnXyZZRqd25? NHqxdI0zOThzN{C0OS=>
NCI-H1993 NXzoRpAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[3NkBp Mn7WSG1UVw>? M4H3OWlEPTB;MD6xJO69VQ>? MVOyNVkyPjR|Mx?=
NCI-H292 NGHJOIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYq3NkBp MX7EUXNQ Mm\sTWM2OD1yLkCyJO69VQ>? MoT5NlE6OTZ2M{O=
A431 Ml\wT4lv[XOnIFHzd4F6 MV6yJIg> MYTEUXNQ M{LTUmlvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36gbY4hTUeILYP0bY12dGG2ZXSgbJVu[W5iQUSzNUB4cXSqIFnDOVAhd2ZiMD6wNFEh|ryP NXnHfY5wOjJzMEGxN|I>
MCF7 NEP2cJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxNFDDqM7:Zz;tUC=> NUTvfWhuPDhiaB?= M{Tnc2ROW09? NIPsOVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgc5ZmemW6cILld5NqdmdiRVfGVkBo\W6nIIfpeIghUUN3MDDv[kAyOi5yNTFOwG0> MnzxNlIyOTlzM{C=
BT474 NUHte2tsS3m2b4TvfIlkKEG|c3H5 MnLJNVAh|ryP MlPLOFghcA>? MY\DfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKEKWNEe0JINmdGy| MnL5NlIyOzh|MEi=
MCF7 NUHMRZlNS3m2b4TvfIlkKEG|c3H5 MVKxNEDPxE1? M3LlblQ5KGh? NEW2e4ZEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIF3DSlch[2WubIOgc5Zmei2neIDy[ZN{cW6pIFXyZmIzKGOnbHzz MVmyNlE{QDNyOB?=
HCC827 NHn2cFBMcW6jc3WgRZN{[Xl? MXGwMlEzPSEQvF2= NX\SbmtiOjRiaB?= NEDO[25FVVOR M3rBbmlvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfCC\MUC2PEBifXSxcHjvd5Bpd3K7bHH0bY9v MXeyNlM{QTN2Mh?=
HCC827 NYDqelRRU2mwYYPlJGF{e2G7 M{TrVlAvOTJ3IN88US=> MVmyOEBp NWDQVXlxTE2VTx?= NEHCVnlKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbh?= M2j5WFIzOzN7M{Sy
HCC827 MXnLbY5ie2ViQYPzZZk> MWqwMlEzPSEQvF2= MWKyOEBp NUjHVZFsTE2VTx?= NVPxSWdmUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFHreEBxcG:|cHjvdplt[XSrb36= NGPvTIYzOjN|OUO0Ni=>
A431 NGnFeoVMcW6jc3WgRZN{[Xl? MWKxNFAh|ryP Mk\UN|AhdWmw NFnaWnpKdmirYnn0bY9vKG:oIFXHSnIh\GW{aY\l[EBnem:vIHj1cYFvKEF2M{GgZ4VtdCCvZX3idoFv\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHCxbImtS4x2NVS7cjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEvODhizszN NUnkOVUyOjJ4OUi3PFI>
H460 MlT5R5l1d3SxeHnjJGF{e2G7 M4TYOlczKGh? M2TwN2lEPTB;NT61PUDPxE1? NWnJbIxFOjJ5Mke0OFk>
HT-29 M2TiXWN6fG:2b4jpZ{BCe3OjeR?= NWr5[5pYPzJiaB?= Mmf5TWM2OD1|LkO2JO69VQ>? NVrv[ZpiOjJ5Mke0OFk>
SGC7901 MW\DfZRwfG:6aXOgRZN{[Xl? NIHJO2U4OiCq NUPzVXRmUUN3ME2xNE4zPiEQvF2= MXeyNlczPzR2OR?=
A498 NFKzO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLNbmFVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIV5eHKnc4PpcochTUeIUjDhcoQhW1KFIIfpeIghUUN3MDDv[kA5NjZizszN Ml\vNlI5OTh6NEi=
Calu3 NWXSSpBsS3m2b4TvfIlkKEG|c3H5 NXfBR|h4OTBizsznM41N MVO3NkBp NIDBN4NKSzVyPUGuOkDPxE1? MmG1NlMyOTZzNki=
FADU MWnDfZRwfG:6aXOgRZN{[Xl? NVnpc3J4OTBizsznM41N MV[3NkBp MnfMTWM2OD1yLkC1JO69VQ>? NHzKWJgzOzFzNkG2PC=>
HCC827 NWGxSIg3S3m2b4TvfIlkKEG|c3H5 MX:xNEDPxGdxbVy= MYK3NkBp MkLTTWM2OD1yLkCwNVUh|ryP MWSyN|EyPjF4OB?=
PC9 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13YN|ExKM7:Zz;tUC=> MUi3NkBp MW\JR|UxRTBwMEG0JO69VQ>? MlqyNlMyOTZzNki=
Sf9 NX;FUVdkU2mwYYPlJGF{e2G7 NV;tZ5hzOSCq M1T5bWROW09? NGP4[|NKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD30ZYdo\WRiRVfGVkBNQDN2UjDteZRidnRiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> MXqyN|YyOTZ7MR?=
16HBE14o- MVTDfZRwfG:6aXOgRZN{[Xl? NEflWpMyOCEQvF2= MWe3NkBp M2rDOWROW09? NGn5[|hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyPkiERUG0c{0h[2WubIOgbIFz[m:{aX7nJJdqdGRidInw[UBGT0[UIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJdqfGhiSVO1NEBw\iBzMj63NUDPxE1? MlfFNlM3Pjh2NEG=
NCI-H1975 MYHDfZRwfG:6aXOgRZN{[Xl? NWf5dJBkOTBizszN MYe3NkBp Mo[ySG1UVw>? NWm4N2dIS3m2b4TvfIlkcXS7IHHnZYlve3RiZ3XmbZRqdmmkLYLld4l{fGGwdDDoeY1idiCQQ1mtTFE6PzViY3XscJMhcGG{Yn;ybY5oKEWJRmKgUFg2QFJxVEe5NG0h\G:3YnzlJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiNj65NVch|ryP NGW3T2UzOzZ4OES0NS=>
16HBE NVX3NZNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3NkBp MljzSG1UVw>? NYW1RnRpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjCxOmhDTSClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCHR1\SJJdqfGhiSVO1NEBw\iBzLk[wNUDPxE1? MY[yN|c6OjNzOB?=
16HBE M1SzVGZ2dmO2aX;uJGF{e2G7 MYmxNFAh|ryP MXSxOVAhdWmw M4\DcmROW09? M3OybGlv\HWldHnvckBw\iCwaYTybYMhd3irZHWgdJJw\HWldHnvckBqdiCqdX3hckAyPkiERTDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDFS2ZT M{fRe|I{Pzl{M{G4
A549 NWjVPWM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW3NkBp MX3EUXNQ NXnmb4hMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEB4cWymIIT5dIUhTUeIUj;rMXJieyCmZYDlcoRmdnRiaIXtZY4hSTV2OTDj[YxteyC5aYToJGlEPTBib3[gOE43OjZizszN M{LlfFI{Pzl{M{G4
SH-SY5Y NFjtV4FEgXSxdH;4bYMhSXO|YYm= NIXRfYY4OiCq MnG3TWM2OD1zOD6yNUDPxE1? M1f5PVI{QDdzOUC5
LoVo M{izd2tqdmG|ZTDBd5NigQ>? NUPuVpZtOiBiaB?= NHXOcFRFVVOR MkK3TY5pcWKrdHnvckBw\iCHR1\SJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yNkKg{txO NHvhS2czOzl|MEm5OC=>
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HCC827 NWq0O2p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjLXIE4OiCq MoPmTWM2OD1yLkCxNkDPxE1? M3i0PFI{QTd|MU[4
A549 M{fJXmtqdmG|ZTDBd5NigQ>? MVyxJO69VQ>? MUexJIg> M2LBTGROW09? NVrqd5NLUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN7OTFOwG0> MoSwNlM6QDh|NUS=
A549 M37rSGZ2dmO2aX;uJGF{e2G7 NGjL[IcyKM7:TR?= NUf0cpJDOSCq MWLEUXNQ MVTD[YxtfWyjcjD1dJRic2V? M3PjV|I{QTh6M{W0
HCC827 MlvrT4lv[XOnIFHzd4F6 NHTiWWQxNjVizszN NF76XpozKGh? M17o[mROW09? M4XvPGlvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36gbY4h\2WoaYTpcoljNXKnc3nzeIFvfCCqdX3hckBJS0N6MkegZ4VtdHN? M4\uTlI{QTl|M{K4
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NCI-H358 M1TUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHxR|RLUUN3ME21NlcvPjZibl2= M3;lUnNCVkeHUh?=
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CAN MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MomyTWM2OD13OECuO|Yhdk1? MY\TRW5ITVJ?
Ca9-22 NY\YbJZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jxfGlEPTB;NUi4MlY1KG6P MUjTRW5ITVJ?
CAL-39 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmyS|VKSzVyPUW5Ok4{KG6P MlT4V2FPT0WU
NCI-H1623 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnFOXlKSzVyPUW5PU4{PiCwTR?= NEK3XVhUSU6JRWK=
FADU MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37hXmlEPTB;NkC0MlY6KG6P M2nUTHNCVkeHUh?=
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LB1047-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTsTWM2OD14MkWuNlkhdk1? MojLV2FPT0WU
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ETK-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnPWIdKSzVyPU[2Nk42QSCwTR?= NYXKRXVRW0GQR1XS
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LU-134-A M2r5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPlTWM2OD15MUmuNFkhdk1? M2myTnNCVkeHUh?=
NCI-H1770 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HYRmlEPTB;N{KyMlQhdk1? M3HuVXNCVkeHUh?=
HAL-01 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjQT3lKSzVyPUezOE44OSCwTR?= MWrTRW5ITVJ?
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A431 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zyeWlEPTB;N{iwMlA1KG6P NGC5[XhUSU6JRWK=
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EC-GI-10 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTd6OD61NkBvVQ>? NFvkOVdUSU6JRWK=
TE-12 NGrQXZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q1XGlEPTB;OEKxMlEyKG6P NWTIOHJSW0GQR1XS
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NCI-H2126 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfUTWM2OD16OEKuPFMhdk1? MoHrV2FPT0WU
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HT-3 M322cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjObI1KSzVyPUm4Nk41OSCwTR?= MXHTRW5ITVJ?
SK-NEP-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfSTWM2OD17OEmuOFQhdk1? Mki0V2FPT0WU
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NCI-H1092 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ywNGlEPTB;MT6zNFg2KM7:TR?= NHnx[VVUSU6JRWK=
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NCI-H1666 NGrt[lFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\1fmlEPTB;MT63OFcxPCEQvF2= NX7DTG17W0GQR1XS
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EPLC-272H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPRSJByUUN3ME2xMlg2PTR7IN88US=> NIi0RWlUSU6JRWK=
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CAL-12T NEfnTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HRVGlEPTB;Mj6wNVg3OSEQvF2= MorTV2FPT0WU
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BT-20 NXTmc4VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJwMk[3OFQh|ryP MlPaV2FPT0WU
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NCI-H2170 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwM{S3PFMh|ryP NGjiO4NUSU6JRWK=
EW-18 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfleW9pUUN3ME2yMlM2PDdzIN88US=> MXrTRW5ITVJ?
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HGC-27 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJyLkGzPVQh|ryP MoPIV2FPT0WU
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LCLC-103H Ml35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTR5LkS0NFQh|ryP MmKyV2FPT0WU
SW780 M3:2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnlTWM2OD12Nz62N|UyKM7:TR?= M{X3d3NCVkeHUh?=
NCI-H1703 NH:2bmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Szb2lEPTB;NEiuN|M2OiEQvF2= M3HkVXNCVkeHUh?=
HCC1395 NW\Se|ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HvNGlEPTB;NEiuO|Q{OiEQvF2= Mom0V2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT; 

PubMed: 22586683     


Effect of overexpressing CRKL on phosphorylation levels of EGFR, ERK, AKT and SRC in response to gefitinib. HCC827 cells expressing a control vector or CRKL were exposed to gefitinib at indicated concentrations for 6 h and cell lysates were collected for immunoblotting with indicated specific antibodies.

Cyclin D1/ p16 / p27 / pRb; 

PubMed: 18559346     


levels of phosphorylated and total EGFR, IGF-1R, Akt, ERK1/2, and Rb and levels of cyclin D1, p27, p16, and actin following 6- or 16-h treatment of A431 cells with combinations of 1 or 3 μm gefitinib and 3 μm NVP-ADW742. Data are representative of two independent experiments.

uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP; 

PubMed: 23102728     


Apoptosis resulting from combined treatment with gefitinib and an MEK inhibitor. (A) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/wt and PC‐9/gef B4 cells. (B) Apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/wt and PC‐9/gef B4 cells. (C) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/gefE3 and PC‐9/gefE7 cells. (D) apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/gefE3 and PC‐9/gefE7 cells.

PPAR-γ; 

PubMed: 23409107     


Fold increase relative to control was determined after normalization with β-actin as external loading control. 

22586683 18559346 23102728 23409107
Immunofluorescence
EGFR / LC3; 

PubMed: 31196210     


H157 and H1299 cells were treated with gefitinib, or curcumin alone, or gefitinib plus curcumin at indicated concentration for 48 h and then were fixed with methanol, immunostained with anti-EGFR (green), anti-LC3 (red), and DAPI (blue), and analyzed by confocal microscopy to determine the intracellular locations of EGFR and LC3.

PPAR-γ; 

PubMed: 23409107     


Upregulation and nuclear accumulation of PPARγ following treatment with gefitinib (24 hs).

p-EGFR / β-catenin; 

PubMed: 23461856     


In untreated CNE2 cells, β-catenin was located in cytoplasmic membranes and cytoplasm. Treatment with EGF (50 ng/mL) resulted in increased β-catenin nuclear staining, which was reversed by either gefitinib (1 μM) or LY294002 (15 μM). 

31196210 23409107 23461856
Growth inhibition assay
GI50; 

PubMed: 23409107     


Dose-response of bladder cancer cell lines to EGFR inhibitor (gefitinib). The GI50 value was defined as the mean concentration of drug that generates 50% of growth inhibition as compared to controls.

23409107
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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* 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:

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Dilution Calculator

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

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03292133 Recruiting Drug: EGF816|Drug: Gefitinib Lung Cancer Massachusetts General Hospital|Novartis October 31 2017 Phase 2
NCT03122717 Recruiting Drug: Gefitinib|Drug: Osimertinib Non-Small Cell Lung Cancer Dana-Farber Cancer Institute|AstraZeneca May 9 2017 Phase 1|Phase 2
NCT02932345 Completed -- EGFR Mutation Positive Advanced Non-small-cell Lung Cancer AstraZeneca October 31 2016 --
NCT02824458 Recruiting Drug: Apatinib|Drug: Gefitinib|Drug: Placebo EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors Sun Yat-sen University June 2016 Phase 3
NCT02804100 Unknown status -- Carcinoma Non-Small-Cell Lung|Bronchial Neoplasms|Carcinoma Bronchogenic|Lung Diseases|Lung Neoplasms Wenzhou Medical University May 2016 --

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

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Frequently Asked Questions

  • Question 1:

    I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?

  • Answer:

    S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID