Gefitinib (ZD1839) 化学構造
分子量: 446.90

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Quality Control & MSDS

製品説明

  • Compare EGFR Inhibitors
    EGFR製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Gefitinib (ZD1839) は、NR6wtEGFRとNR6W細胞のTyr1173、Tyr992、Tyr1173とTyr992のためのEGFR阻害剤で、IC50 がそれぞれ 37 nM、 37nM、 26 nM 、57 nMです。
ターゲット Tyr1173 (NR6wtEGFR cells) Tyr992 (NR6wtEGFR cells) Tyr1173 (NR6W cells) Tyr992 (NR6W cells)
IC50 37 nM 37nM 26 nM 57 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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A549 Ml3aR5l1d3SxeHnjJGF{e2G7 MlLpPVYhcA>? NF24dpJFVVOR MnfhTWM2OD1zMz61PUDPxE1? MXuxPFMyOzhyNx?=
K562 M4PxOWN6fG:2b4jpZ{BCe3OjeR?= NIDPRnk6PiCq NELwPXpFVVOR MkfkTWM2OD17LkO2JO69VQ>? NFnVc4kyQDNzM{iwOy=>
MDA-MB-231 NHrJVWJEgXSxdH;4bYMhSXO|YYm= MXq5OkBp MWLEUXNQ NXy2T2QyUUN3ME2zOk43OSEQvF2= NHLxVZAyQDNzM{iwOy=>
MOLT4 M3PQ[2N6fG:2b4jpZ{BCe3OjeR?= M3:0clk3KGh? MljvSG1UVw>? MVfJR|UxRTF3LkCyJO69VQ>? MWixPFMyOzhyNx?=
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NCI-H1975 NWTDOZpyTnWwY4Tpc44hSXO|YYm= NUHBRWhYOTBizszN M1\4b2lvcGmkaYTpc44hd2ZiRWLCRlIh[XW2b4Doc5NxcG:{eXzheIlwdg>? NYfmTpJNOjBzNUG2O|A>
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Plasmodium falciparum NXPVTng{eUiWUzDwdo9ncWyrbneg[o9zKGmwaHnibZRwenNib3[gVIxie22xZHn1cUBn[WylaYDhdpVuKHC{b3zp[oVz[XSrb36= NV\2dlcxOjF6MUewOFU>
NCI-H1993 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnSO|IhcA>? MXzEUXNQ M4rsN2lEPTB;MD6xJO69VQ>? MnH2NlE6OTZ2M{O=
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A431 NULDNZVUU2mwYYPlJGF{e2G7 M2HjXVIhcA>? M2G1N2ROW09? M323Z2lvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36gbY4hTUeILYP0bY12dGG2ZXSgbJVu[W5iQUSzNUB4cXSqIFnDOVAhd2ZiMD6wNFEh|ryP NV\QUI1GOjJzMEGxN|I>
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BT474 M2PJfGN6fG:2b4jpZ{BCe3OjeR?= NVTmXXNNOTBizszN MYC0PEBp NUDwSYFDS3m2b4TvfIlkcXS7IHHnZYlve3Ric3XyeY0ue3Sjco\l[EBpfW2jbjDCWFQ4PCClZXzsdy=> NWrYTWtzOjJzM{izNFg>
MCF7 MWTDfZRwfG:6aXOgRZN{[Xl? MUSxNEDPxE1? NU[5bHY5PDhiaB?= NWTT[2Y5S3m2b4TvfIlkcXS7IHHnZYlve3Ric3XyeY0ue3Sjco\l[EBpfW2jbjDNR2Y4KGOnbHzzJI93\XJvZYjwdoV{e2mwZzDFdoJDOiClZXzsdy=> MYOyNlE{QDNyOB?=
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SGC7901 Mk\0R5l1d3SxeHnjJGF{e2G7 MkXVO|IhcA>? MonSTWM2OD1zMD6yOkDPxE1? NHPG[VAzOjd{N{S0PS=>
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SCC-15 NV7uc4c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHQVIRKSzVyPUWyOU43QCCwTR?= MXrTRW5ITVJ?
NCI-H358 NIT2fpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTV{Nz62OkBvVQ>? MU\TRW5ITVJ?
KYSE-180 M3PyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfRSmxUUUN3ME21N|AvPjJibl2= M2SwfXNCVkeHUh?=
NCI-H82 MnLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G4[GlEPTB;NUSwMlUhdk1? Mn\OV2FPT0WU
NB7 M33sVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXpTWM2OD13NE[uN|Ihdk1? MUTTRW5ITVJ?
DSH1 NEXUfGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT3bm9vUUN3ME21OlYvQDhibl2= MUDTRW5ITVJ?
RS4-11 NI\GSZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzBfmRGUUN3ME21OlgvPTlibl2= MULTRW5ITVJ?
CAN NHLvTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonBTWM2OD13OECuO|Yhdk1? M3PzWHNCVkeHUh?=
Ca9-22 NGW1WJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\iTWM2OD13OEiuOlQhdk1? M2nVbnNCVkeHUh?=
CAL-39 NFrx[|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTV7Nj6zJI5O M1vrRnNCVkeHUh?=
NCI-H1623 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:zeG53UUN3ME21PVkvOzZibl2= MXnTRW5ITVJ?
FADU M33RW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC0TWM2OD14MESuOlkhdk1? MVLTRW5ITVJ?
NB69 NVHwdYlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTZzND6zOUBvVQ>? NFP2PYRUSU6JRWK=
Ramos-2G6-4C10 NGrvXJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1GwOGlEPTB;NkKxMlQ3KG6P Ml3TV2FPT0WU
LB1047-RCC NYD6WmVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\Hb|FKSzVyPU[yOU4zQSCwTR?= NXXtVpFbW0GQR1XS
MV-4-11 NXvSSHdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjFVodKSzVyPU[yO{44KG6P NF[4XnVUSU6JRWK=
DBTRG-05MG MnPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTxTWM2OD14M{KuNlghdk1? Mlu0V2FPT0WU
ME-180 NXjUepJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jBemlEPTB;NkOyMlkhdk1? MkHtV2FPT0WU
NBsusSR NV\HPY9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DsOGlEPTB;NkS2MlUzKG6P MWDTRW5ITVJ?
COR-L105 Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTZ4Mj61N{BvVQ>? MlrwV2FPT0WU
ETK-1 NEPZeIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nL[GlEPTB;Nk[yMlU6KG6P M4X1fHNCVkeHUh?=
L-363 MmKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rLOWlEPTB;NkexMlk1KG6P M1n0e3NCVkeHUh?=
LU-134-A MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjC[plKSzVyPUexPU4xQSCwTR?= NIfGcZZUSU6JRWK=
NCI-H1770 NYDJRos5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXwWGxLUUN3ME23NlIvPCCwTR?= NFWyO4xUSU6JRWK=
HAL-01 M1HBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPtTWM2OD15M{SuO|Ehdk1? MkLwV2FPT0WU
COLO-684 M3rPU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTd3Mz6wNUBvVQ>? NGTtVnRUSU6JRWK=
TE-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILNW5FKSzVyPUe2OE4{OSCwTR?= MVLTRW5ITVJ?
A431 NX;mXY1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q1O2lEPTB;N{iwMlA1KG6P M3P4VXNCVkeHUh?=
LU-135 NGTOeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;HTWM2OD15OEOuNFMhdk1? NEPSSZRUSU6JRWK=
EC-GI-10 NHPSUHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;ZTlRKSzVyPUe4PE42OiCwTR?= NEj1WG1USU6JRWK=
TE-12 NHLJPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofLTWM2OD16MkGuNVEhdk1? M1LRNHNCVkeHUh?=
LoVo Mnq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[3dmlEPTB;OEW5MlA3KG6P M1;NU3NCVkeHUh?=
23132-87 M16yWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTh4ND6yPEBvVQ>? Moq4V2FPT0WU
AU565 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPo[482UUN3ME24OlkvPiCwTR?= M3zCSnNCVkeHUh?=
DEL NFP0cGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;je2lEPTB;OEe3MlY2KG6P M33FZXNCVkeHUh?=
COR-L88 NXHtUIp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHsTWM2OD16OEKuNlYhdk1? MUHTRW5ITVJ?
NCI-H2126 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTh6Mj64N{BvVQ>? M2LRbXNCVkeHUh?=
CAPAN-1 M2HZ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTucHlmUUN3ME24PFMvOjlibl2= M2K4XXNCVkeHUh?=
BT-474 MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7yPHk5UUN3ME25N|gvOTRibl2= NELiRXpUSU6JRWK=
BHY M{D0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPuTWM2OD17N{WuOFghdk1? NXPJSmhkW0GQR1XS
HT-3 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny2TWM2OD17OEKuOFEhdk1? MV;TRW5ITVJ?
SK-NEP-1 NVric5ltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLITWM2OD17OEmuOFQhdk1? MnvXV2FPT0WU
MS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPUTWM2OD17OUSuOlkhdk1? M3ewbXNCVkeHUh?=
DOHH-2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXETWM2OD1zLkCwNFIyKM7:TR?= M4HyXnNCVkeHUh?=
NCI-H1304 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnUUXNUUUN3ME2xMlAyPjR|IN88US=> NFXp[41USU6JRWK=
EM-2 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX5coxKSzVyPUGuNFMxOTZizszN MlrOV2FPT0WU
MHH-PREB-1 NHvJb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XQW2lEPTB;MT6wPFQ2OSEQvF2= M2nTUHNCVkeHUh?=
KU-19-19 M3XEWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljUTWM2OD1zLkC4OVQyKM7:TR?= MXnTRW5ITVJ?
NCI-H1648 M{K1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXYTWM2OD1zLkGwOlE3KM7:TR?= M{L4RnNCVkeHUh?=
MKN1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\TU2lEPTB;MT6yNVk5PyEQvF2= Mkn6V2FPT0WU
SNU-449 NEfWdI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfxTWM2OD1zLkKyNlA5KM7:TR?= MVjTRW5ITVJ?
OAW-42 M4DDdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\UbmlEPTB;MT6yO|gzPSEQvF2= MUnTRW5ITVJ?
769-P NVvpeYV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTKWmFzUUN3ME2xMlI4QTF6IN88US=> NITWXpdUSU6JRWK=
SW1088 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFwMkm2NFch|ryP NW\BZXNSW0GQR1XS
GCIY MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fxSmlEPTB;MT6zNFE{OiEQvF2= M{\2ZXNCVkeHUh?=
CTV-1 NYjDNFh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfnTWM2OD1zLkOwPEDPxE1? MWXTRW5ITVJ?
NCI-H1092 MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDrTWM2OD1zLkOwPFUh|ryP MXHTRW5ITVJ?
NKM-1 MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzvdphKSzVyPUGuN|I2QTdizszN MnXPV2FPT0WU
NCI-H1650 M3XSTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFwM{O0PFIh|ryP M1\4WnNCVkeHUh?=
SW954 M1XUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwM{SwOFgh|ryP MUjTRW5ITVJ?
SW48 MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom2TWM2OD1zLkO2OlE5KM7:TR?= NYriS5FqW0GQR1XS
SK-N-DZ Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7OTZJIUUN3ME2xMlM3QTR5IN88US=> NWS4T2NCW0GQR1XS
KMOE-2 MkSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHUTWM2OD1zLkO5PFE2KM7:TR?= NFPOeYZUSU6JRWK=
NB5 NE\RTWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;F[mlEPTB;MT60NFg6PCEQvF2= MonCV2FPT0WU
CCRF-CEM MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zpcmlEPTB;MT60NVEyKM7:TR?= MWfTRW5ITVJ?
RH-1 M1PlTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzMTWM2OD1zLkSxNVM3KM7:TR?= MWDTRW5ITVJ?
NCI-H526 NYDFc3lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH6TWM2OD1zLkSzPFI3KM7:TR?= MV3TRW5ITVJ?
697 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkewTWM2OD1zLkS0NVA1KM7:TR?= MkLDV2FPT0WU
J82 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFwNEW3OlYh|ryP MWrTRW5ITVJ?
BE-13 NWr1ZZVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXSwfWVXUUN3ME2xMlUxPjdzIN88US=> NH6wd49USU6JRWK=
SAS MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HFUWlEPTB;MT61NVYzOiEQvF2= NGDVdYdUSU6JRWK=
SCC-25 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXM[5NKSzVyPUGuOVI{OjJizszN MWXTRW5ITVJ?
LAMA-84 NH7RU5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC5TJlKSzVyPUGuOVM5OTVizszN NHLkfHJUSU6JRWK=
HSC-3 NYPoWVVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwNUSzPEDPxE1? Ml3hV2FPT0WU
BT-549 NXHjUWZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC1ZYNsUUN3ME2xMlU5PzR5IN88US=> MXrTRW5ITVJ?
ML-2 NYrTOYF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XhfGlEPTB;MT62OFAzQSEQvF2= MV7TRW5ITVJ?
BB30-HNC NVrUOmpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFwNki5O|Ih|ryP NX\QXYd3W0GQR1XS
PANC-03-27 M{nFSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\KelJKSzVyPUGuO|AyOzlizszN NWPZdoQ3W0GQR1XS
COLO-678 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:2TWM2OD1zLkezOFQ1KM7:TR?= NEHYOG9USU6JRWK=
NCI-H1666 M4HjU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFwN{S3NFQh|ryP NWPmN2gzW0GQR1XS
NCI-H209 MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;hTWM2OD1zLke3NlY6KM7:TR?= NF\0U2tUSU6JRWK=
EPLC-272H NE\2XVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDmeZJmUUN3ME2xMlg2PTR7IN88US=> MYTTRW5ITVJ?
OMC-1 MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwOUm4PFgh|ryP NGLBfFlUSU6JRWK=
HCC70 M3LCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJwMEC4NVUh|ryP NVfQZZI{W0GQR1XS
CAL-12T NVnnelBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn3RYRJUUN3ME2yMlAyQDZzIN88US=> MoHYV2FPT0WU
TGBC24TKB NHHtcpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKwTWM2OD1{LkCyPVYyKM7:TR?= MUDTRW5ITVJ?
EKVX NYDlXGV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJwMES5N|kh|ryP MW\TRW5ITVJ?
SW1116 NGTpPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzJTWM2OD1{LkC2NFA6KM7:TR?= NGLkT2lUSU6JRWK=
NCI-H2009 MlnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3hTWM2OD1{LkC2NlE1KM7:TR?= M1PhbnNCVkeHUh?=
RPMI-8866 NFyycIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TTfmlEPTB;Mj6wPFQ5OSEQvF2= M2n6T3NCVkeHUh?=
KARPAS-45 Mlf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTHd5Z1UUN3ME2yMlEzPDd7IN88US=> NWnlNWd4W0GQR1XS
RXF393 Mn23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPCUHNKSzVyPUKuNVMxOzZizszN NHvQXpNUSU6JRWK=
786-0 M1fOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DkdWlEPTB;Mj6xPFQxPiEQvF2= MWXTRW5ITVJ?
SCC-4 MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXrVXVKSzVyPUKuNlE4PzZizszN MlLuV2FPT0WU
BT-20 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPCcG1KSzVyPUKuNlY4PDRizszN MkXaV2FPT0WU
A498 Ml3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fTNmlEPTB;Mj6yPVQyPSEQvF2= M4jmfnNCVkeHUh?=
IGROV-1 NGn5c|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O3OGlEPTB;Mj6zNVI{PyEQvF2= NV[ydWVSW0GQR1XS
JVM-3 M2TRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTJwM{S2OFMh|ryP NW[5TVk3W0GQR1XS
NCI-H2170 NVHybXJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJwM{S3PFMh|ryP NEfLOmRUSU6JRWK=
EW-18 NFyxNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHxTHlKSzVyPUKuN|U1PzFizszN MVXTRW5ITVJ?
KU812 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJwM{[3O|kh|ryP NIL1SINUSU6JRWK=
NY NYLZbY9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG1U4E3UUN3ME2yMlM4OjdizszN MnXpV2FPT0WU
HTC-C3 NWryenVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnGUItKSzVyPUKuOFIzPjdizszN M{DSNHNCVkeHUh?=
CFPAC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLzVG9RUUN3ME2yMlQ{QDZ2IN88US=> Mlu0V2FPT0WU
HH NVfKVmZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjOXmlKSzVyPUKuOFk5PTRizszN NXTJd5d2W0GQR1XS
MKN7 NI[xUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJwNkK3OFgh|ryP NUDLVW5xW0GQR1XS
TE-8 NEj6SpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HifmlEPTB;Mj62N|Y2OyEQvF2= NEDZSHFUSU6JRWK=
MC-IXC NVrnUXZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2G0e2lEPTB;Mj62OFQ2OyEQvF2= NVLsRnFCW0GQR1XS
DMS-79 NHTHWoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLGTWM2OD1{Lk[5Nlg1KM7:TR?= NYntbGZYW0GQR1XS
Detroit562 M1TVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0TWM2OD1{Lk[5PFQ2KM7:TR?= NILj[nRUSU6JRWK=
HuP-T4 M3jheGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJwN{K4NVgh|ryP M2nGdnNCVkeHUh?=
QIMR-WIL NFu0bmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXJN2g{UUN3ME2yMlc2QTV{IN88US=> NIPTblJUSU6JRWK=
BB65-RCC MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTlOGxwUUN3ME2yMlgxPzF|IN88US=> NY\DcpcyW0GQR1XS
PC-3 NYS1cI1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJwOEOzNVch|ryP M3flc3NCVkeHUh?=
OVCAR-3 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrERlU1UUN3ME2yMlg2PTl2IN88US=> NV;SZpVbW0GQR1XS
KYSE-510 NYXwcYJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm5TWM2OD1{Lki2O|g3KM7:TR?= MX\TRW5ITVJ?
HC-1 M3jOVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XXO2lEPTB;Mj65OFAyOiEQvF2= Mki0V2FPT0WU
NCI-H1693 M1PDc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TYRWlEPTB;Mj65OVg6PyEQvF2= NXHieG1tW0GQR1XS
DU-4475 Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rMe2lEPTB;Mj65PVA2OiEQvF2= NVnkb3lZW0GQR1XS
COLO-680N NY\sOpJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfXVWVKUUN3ME2zMlAxPDl3IN88US=> NVz6RocyW0GQR1XS
MN-60 M{HBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTNwMES5O|Qh|ryP NInDbplUSU6JRWK=
BCPAP NFzneYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOxTWM2OD1|LkC4Nlk2KM7:TR?= NHXNUVNUSU6JRWK=
647-V MmGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[2SlhlUUN3ME2zMlE3OjJizszN NWjGW3c3W0GQR1XS
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LCLC-103H NFHBbm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonvTWM2OD12Nz60OFA1KM7:TR?= MV7TRW5ITVJ?
SW780 MoGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M36zcGlEPTB;NEeuOlM2OSEQvF2= NV3GXndLW0GQR1XS
NCI-H1703 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn6TWM2OD12OD6zN|UzKM7:TR?= M{m0UHNCVkeHUh?=
HCC1395 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTR6Lke0N|Ih|ryP M2WwWHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Gefitinib has entered in a phase II clinical trial in the treatment of non small cell lung cancer.
特集 A potent EGFR tyrosine kinase inhibitor.

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 NR6, NR6M and NR6W cells
濃度 0-2 μM
反応時間 72 hours
実験の流れ 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.

動物実験: [3]

動物モデル Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
製剤 0.5% polysorbate
投薬量 100 mg/kg
投与方法 Once daily by oral administration (0.1 mL/10 g body weight) for 14 days

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Gefitinib (ZD1839) SDF
分子量 446.90
化学式

C22H24ClFN4O3

CAS No. 184475-35-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 89 mg/mL (199.14 mM)
エタノール 4 mg/mL (8.95 mM)
<1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80 12 mg/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.
化学名 N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

カスタマーフィードバック (11)


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Source Mol Syst Biol , 2011, 7, 486. Gefitinib (ZD1839) 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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Source Oncogene, 2010, 30, 737-750. Gefitinib (ZD1839) 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).

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Source Carcinogenesis, 2010, 31, 1948–1955 . Gefitinib (ZD1839) 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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Source Carcinogenesis, 2010, 31, 1948–1955. Gefitinib (ZD1839) 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 .

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Source J Immunother, 2011, 34(4), 372-81. Gefitinib (ZD1839) 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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Source Antiviral Res, 2010, 89, 64-70. Gefitinib (ZD1839) 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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Source Antiviral Res, 2010, 89, 64-70. Gefitinib (ZD1839) 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).

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Source Mol Biosyst, 2011, 7, 3223-33. Gefitinib (ZD1839) 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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Source Int J Proteomics , 2011, 215496. Gefitinib (ZD1839) 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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Source 2010, Dr. Zhang of Tianjin Medical University. Gefitinib (ZD1839) purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-5 nM
Incubation Time 24 h
Results

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Source 2010, Dr. Vicky Tin from University of Hong Kong. Gefitinib (ZD1839) 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

文献中の引用 (85)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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