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
KB M1jFWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:2NZNXUUN3ME2wMlA2PCEQvF2= M1;DdVE3PTF4NEez
NIH3T3 NUjtNVAzTnWwY4Tpc44hSXO|YYm= MoXONE4zKM7:TR?= MVSyJIg> NIm2dFhFVVOR NV;RZmU2UW6qaXLpeIlwdiCxZjDFS2Yhe3SrbYXsZZRm\CCqdX3hckBmemKEMTDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxOFQh|ryP MlvFNVY1QDB{OES=
COS7 M1HFN2Z2dmO2aX;uJGF{e2G7 NHLFU4c6PiEQvF2= NYLJTnZPUW6qaXLpeIlwdiCxZjDoeY1idiCMQVuyJHY3OTeIIH31eIFvfCCneIDy[ZN{\WR? M{jwfVE4OTd6N{Ky
A549 M4HYOGN6fG:2b4jpZ{BCe3OjeR?= NXjEcYV7QTZiaB?= MnP1SG1UVw>? NH\BSHdKSzVyPUGzMlU6KM7:TR?= NVPsXGpsOTh|MUO4NFc>
K562 NFzne|lEgXSxdH;4bYMhSXO|YYm= NEjWbYg6PiCq NETlNWZFVVOR MWTJR|UxRTlwM{[g{txO MV:xPFMyOzhyNx?=
MDA-MB-231 Mm[wR5l1d3SxeHnjJGF{e2G7 MVW5OkBp NXLMZoFXTE2VTx?= M2D2UGlEPTB;M{[uOlEh|ryP NX2zd4NoOTh|MUO4NFc>
MOLT4 NF\pdlJEgXSxdH;4bYMhSXO|YYm= NYO2UnBtQTZiaB?= MoDSSG1UVw>? NGL0WHdKSzVyPUG1MlAzKM7:TR?= MWexPFMyOzhyNx?=
MCF7 MVLDfZRwfG:6aXOgRZN{[Xl? M3f6PFUxKM7:TR?= M4HEW|czKGh? NWLoSoFrUUN3ME2xNk4xPSEQvF2= Mnf0NVg4PzF6MUm=
BT474 M13JNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLYUYI4OiCq MmmyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuczDveoVz\XiycnXzd4lv\yCHUlLiNkB4cXSqIFXDOVAhd2ZiMD6zJO69VQ>? M17kOVE6ODJ6NEK0
HN5 MlLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrMWHU4OiCq M1PYZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKge4l1cCCHQ{WwJI9nKDBwMEGg{txO MnfTNVkxOjh2MkS=
BA/F3 MmXLR5l1d3SxeHnjJGF{e2G7 M3;oTFczKGh? NIWweJpEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO MUKxPVI{QTJ{OR?=
NIH3T3 NH;BeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPIRWhlPzJiaB?= M1nHOGdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUC9|VEOgZ4VtdHNiZYjwdoV{e2mwZzDldmIzKGenbnWge4l1cCCLQ{WwJI9nKDBwNUSg{txO M2Wy[FE6PjZ3M{e3
MCF7 MX M2LidmZ2dmO2aX;uJGF{e2G7 M2XYVVMxKG2rbh?= M3H1dGlvcGmkaYTpc44hd2ZiQlPSVEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuNUDPxE1? NVLCXGNqOTl7M{K5OlA>
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MCF7 MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnFNVYyODEEoN88[{9uVA>? MUC0PEBp M1jjV2ROW09? NHXGTWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgc5ZmemW6cILld5NqdmdiRVfGVkBo\W6nIIfpeIghUUN3MDDv[kAyOi5yNTFOwG0> M4\o[FIzOTF7MUOw
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HCC827 MnTrT4lv[XOnIFHzd4F6 NVjobWJ3OC5zMkWg{txO MUGyOEBp M2DhbmROW09? NV\sfJQ3UW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36= MnXCNlI{Ozl|NEK=
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HCC827 MWDDfZRwfG:6aXOgRZN{[Xl? NF7zOpcyOCEQvHevcWw> MnewO|IhcA>? NFruWppKSzVyPUCuNFAyPSEQvF2= NEXVN3ozOzFzNkG2PC=>
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Sf9 NIHyc|hMcW6jc3WgRZN{[Xl? NVXSNWx1OSCq Mo\FSG1UVw>? NWHWUXA2UW6qaXLpeIlwdiCxZjDoeY1idiCJU2SteIFo\2WmIFXHSnIhVDh|NGKgcZV1[W62IHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5yMUWg{txO MYWyN|YyOTZ7MR?=
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HN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fmNGlEPTB;NUG3MlM5KG6P M3uwenNCVkeHUh?=
SCC-15 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTV{NT62PEBvVQ>? NUC4NHhrW0GQR1XS
NCI-H358 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\zb|FKSzVyPUWyO{43PiCwTR?= NVTKVW57W0GQR1XS
KYSE-180 M1HHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTV|MD62NkBvVQ>? NFztfGNUSU6JRWK=
NCI-H82 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrh[pQ4UUN3ME21OFAvPSCwTR?= Mk\SV2FPT0WU
NB7 MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTV2Nj6zNkBvVQ>? NIK1TFFUSU6JRWK=
DSH1 NFvZO2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjOeGs4UUN3ME21OlYvQDhibl2= M3\reXNCVkeHUh?=
RS4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\I[ohHUUN3ME21OlgvPTlibl2= M3jhVHNCVkeHUh?=
CAN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTMZm1qUUN3ME21PFAvPzZibl2= Mo\hV2FPT0WU
Ca9-22 NFn4dHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXjOHA5UUN3ME21PFgvPjRibl2= M{L2NXNCVkeHUh?=
CAL-39 NXKycnk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:wcINKSzVyPUW5Ok4{KG6P MmjqV2FPT0WU
NCI-H1623 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVeycWx2UUN3ME21PVkvOzZibl2= NWPDZYlVW0GQR1XS
FADU MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXmUW1KSzVyPU[wOE43QSCwTR?= NWPBWW93W0GQR1XS
NB69 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TKOGlEPTB;NkG0MlM2KG6P M4W1bHNCVkeHUh?=
Ramos-2G6-4C10 M4\wO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj0ZlhDUUN3ME22NlEvPDZibl2= MmDwV2FPT0WU
LB1047-RCC NHjBb2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXjTWM2OD14MkWuNlkhdk1? MVXTRW5ITVJ?
MV-4-11 Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS2XGRKSzVyPU[yO{44KG6P M2nucXNCVkeHUh?=
DBTRG-05MG M4HGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF2xRWxKSzVyPU[zNk4zQCCwTR?= NYS4OHo6W0GQR1XS
ME-180 NY\CXIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzUVJFKSzVyPU[zNk46KG6P MV\TRW5ITVJ?
NBsusSR M3POcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\DV3NkUUN3ME22OFYvPTJibl2= NVnGXWREW0GQR1XS
COR-L105 MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPNZo9KSzVyPU[2Nk42OyCwTR?= MmXiV2FPT0WU
ETK-1 NXHkU4FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnZZ4FHUUN3ME22OlIvPTlibl2= NUW3dXlkW0GQR1XS
L-363 NUjkSlZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWxdJlxUUN3ME22O|EvQTRibl2= NEO2XVJUSU6JRWK=
LU-134-A MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnMTWM2OD15MUmuNFkhdk1? NHfae|dUSU6JRWK=
NCI-H1770 NHLxTJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTNTWM2OD15MkKuOEBvVQ>? MYXTRW5ITVJ?
HAL-01 M{Hwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXsTJk2UUN3ME23N|QvPzFibl2= NYf3WohZW0GQR1XS
COLO-684 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHZdY9yUUN3ME23OVMvODFibl2= M2Xwb3NCVkeHUh?=
TE-6 NYnlcVhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISwfHlKSzVyPUe2OE4{OSCwTR?= Mn\4V2FPT0WU
A431 NFPlZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjHTWZKSzVyPUe4NE4xPCCwTR?= M{LJcnNCVkeHUh?=
LU-135 NYr2VWtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HadWlEPTB;N{izMlA{KG6P M{TJXXNCVkeHUh?=
EC-GI-10 NFnoRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzvdFZYUUN3ME23PFgvPTJibl2= NVrxXpJOW0GQR1XS
TE-12 NEjNRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG0TWM2OD16MkGuNVEhdk1? MWHTRW5ITVJ?
LoVo MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrSVFBKSzVyPUi1PU4xPiCwTR?= NYjqdYlpW0GQR1XS
23132-87 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TQZmlEPTB;OE[0MlI5KG6P MUPTRW5ITVJ?
AU565 M4fRPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HVXWlEPTB;OE[5MlYhdk1? MV7TRW5ITVJ?
DEL NX;DR5l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTh5Nz62OUBvVQ>? NInjT|FUSU6JRWK=
COR-L88 NYHzdJI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTh6Mj6yOkBvVQ>? Mn\SV2FPT0WU
NCI-H2126 NIGwWndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\TNGFEUUN3ME24PFIvQDNibl2= M4HobHNCVkeHUh?=
CAPAN-1 NHfYbIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\4OoVKSzVyPUi4N{4zQSCwTR?= NFLGTIZUSU6JRWK=
BT-474 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTl|OD6xOEBvVQ>? NGX1eVRUSU6JRWK=
BHY NVOzR3lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrsTWM2OD17N{WuOFghdk1? NXTZS2Y3W0GQR1XS
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SK-NEP-1 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDHZZhKSzVyPUm4PU41PCCwTR?= MYLTRW5ITVJ?
MS-1 MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvTcoh5UUN3ME25PVQvPjlibl2= NWDaepQ1W0GQR1XS
DOHH-2 M361eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFwMECwNlEh|ryP NHXWXIZUSU6JRWK=
NCI-H1304 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF25bYRKSzVyPUGuNFE3PDNizszN M{KyPHNCVkeHUh?=
EM-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDPOVhKSzVyPUGuNFMxOTZizszN MmLFV2FPT0WU
MHH-PREB-1 NFHybIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLPTWM2OD1zLkC4OFUyKM7:TR?= MoXmV2FPT0WU
KU-19-19 MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n5d2lEPTB;MT6wPFU1OSEQvF2= MYDTRW5ITVJ?
NCI-H1648 NVnZcZdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7hPYhTUUN3ME2xMlExPjF4IN88US=> NIPITIVUSU6JRWK=
MKN1 NHu0UXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHyTWM2OD1zLkKxPVg4KM7:TR?= NWn3OFJLW0GQR1XS
SNU-449 NIraS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnBOXRKSzVyPUGuNlIzODhizszN NXT4NFJIW0GQR1XS
OAW-42 M2jRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlftTWM2OD1zLkK3PFI2KM7:TR?= NF7GW29USU6JRWK=
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SW1088 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfETWM2OD1zLkK5OlA4KM7:TR?= NGnteYJUSU6JRWK=
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CTV-1 M2DqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7KTWM2OD1zLkOwPEDPxE1? NVH0R5A5W0GQR1XS
NCI-H1092 M1XRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFwM{C4OUDPxE1? M3LTcnNCVkeHUh?=
NKM-1 Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKwSGZKSzVyPUGuN|I2QTdizszN MoS0V2FPT0WU
NCI-H1650 MlP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DMVGlEPTB;MT6zN|Q5OiEQvF2= NGnxVJhUSU6JRWK=
SW954 NEfac25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPCTWM2OD1zLkO0NFQ5KM7:TR?= NGHNO2JUSU6JRWK=
SW48 M4P4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTFwM{[2NVgh|ryP M1z4U3NCVkeHUh?=
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KMOE-2 NGDzT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwM{m4NVUh|ryP MlizV2FPT0WU
NB5 M1zrXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjRTWM2OD1zLkSwPFk1KM7:TR?= NIjyUWNUSU6JRWK=
CCRF-CEM NXTlb4RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwNEGxNUDPxE1? MmjVV2FPT0WU
RH-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTFwNEGxN|Yh|ryP MWPTRW5ITVJ?
NCI-H526 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj2TWM2OD1zLkSzPFI3KM7:TR?= NF63VYxUSU6JRWK=
697 M{fsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13CNmlEPTB;MT60OFExPCEQvF2= MUXTRW5ITVJ?
J82 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrhTWM2OD1zLkS1O|Y3KM7:TR?= NYLvSZBiW0GQR1XS
BE-13 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC4ZlVmUUN3ME2xMlUxPjdzIN88US=> M4Xhd3NCVkeHUh?=
SAS Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFwNUG2NlIh|ryP MXXTRW5ITVJ?
SCC-25 M{HTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TJbWlEPTB;MT61NlMzOiEQvF2= M4T2eXNCVkeHUh?=
LAMA-84 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwNUO4NVUh|ryP MYnTRW5ITVJ?
HSC-3 NGrvZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFwNUSzPEDPxE1? M2KxSnNCVkeHUh?=
BT-549 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvMTWM2OD1zLkW4O|Q4KM7:TR?= MkW1V2FPT0WU
ML-2 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\oco5KSzVyPUGuOlQxOjlizszN M2PoZnNCVkeHUh?=
BB30-HNC Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL2WXFKSzVyPUGuOlg6PzJizszN NX\Kc45vW0GQR1XS
PANC-03-27 M4HyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DQOmlEPTB;MT63NFE{QSEQvF2= M1fR[XNCVkeHUh?=
COLO-678 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvLd2JKSzVyPUGuO|M1PDRizszN MkXYV2FPT0WU
NCI-H1666 NYf1cYlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jTTWlEPTB;MT63OFcxPCEQvF2= NGrYT|hUSU6JRWK=
NCI-H209 NITBR2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3kRVRKUUN3ME2xMlc4OjZ7IN88US=> M3HxPHNCVkeHUh?=
EPLC-272H MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFwOEW1OFkh|ryP MUnTRW5ITVJ?
OMC-1 MmHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnroTWM2OD1zLkm5PFg5KM7:TR?= NX;IVYt4W0GQR1XS
HCC70 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nTNWlEPTB;Mj6wNFgyPSEQvF2= MVrTRW5ITVJ?
CAL-12T MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rtNmlEPTB;Mj6wNVg3OSEQvF2= NHrGPZFUSU6JRWK=
TGBC24TKB MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJwMEK5OlEh|ryP M1TqOXNCVkeHUh?=
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SW1116 NXi3SIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJwME[wNFkh|ryP M3XzXXNCVkeHUh?=
NCI-H2009 NH\wPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnSzTWM2OD1{LkC2NlE1KM7:TR?= MlezV2FPT0WU
RPMI-8866 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL2PXRKSzVyPUKuNFg1QDFizszN M2XMZXNCVkeHUh?=
KARPAS-45 NIfUSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJwMUK0O|kh|ryP NWPJNm5[W0GQR1XS
RXF393 MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjYNnJuUUN3ME2yMlE{ODN4IN88US=> NFnyc4FUSU6JRWK=
786-0 NGnoWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzuT5hKSzVyPUKuNVg1ODZizszN MnftV2FPT0WU
SCC-4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\KUWVKSzVyPUKuNlE4PzZizszN MYrTRW5ITVJ?
BT-20 NHv3NHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nBNWlEPTB;Mj6yOlc1PCEQvF2= NWXXRoJ6W0GQR1XS
A498 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGyTWM2OD1{LkK5OFE2KM7:TR?= NWXCbJhPW0GQR1XS
IGROV-1 M1vI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTac2JKSzVyPUKuN|EzOzdizszN M3L5RXNCVkeHUh?=
JVM-3 NUHEU3ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTTTWM2OD1{LkO0OlQ{KM7:TR?= NHv4S4pUSU6JRWK=
NCI-H2170 NET2VVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;QXmlEPTB;Mj6zOFc5OyEQvF2= NFXjZ2JUSU6JRWK=
EW-18 NEX4boJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rvSmlEPTB;Mj6zOVQ4OSEQvF2= MojsV2FPT0WU
KU812 NGnmZ|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofiTWM2OD1{LkO2O|c6KM7:TR?= MUDTRW5ITVJ?
NY M3vKNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TPT2lEPTB;Mj6zO|I4KM7:TR?= MnTmV2FPT0WU
HTC-C3 M1vNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTiTWM2OD1{LkSyNlY4KM7:TR?= NEPuRnhUSU6JRWK=
CFPAC-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzxZZlKSzVyPUKuOFM5PjRizszN Moq3V2FPT0WU
HH Mm\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXwOXhvUUN3ME2yMlQ6QDV2IN88US=> MX;TRW5ITVJ?
MKN7 MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDqTWM2OD1{Lk[yO|Q5KM7:TR?= MYnTRW5ITVJ?
TE-8 NUn3U2M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L6XGlEPTB;Mj62N|Y2OyEQvF2= NIL3PW1USU6JRWK=
MC-IXC NEHDcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7QTWM2OD1{Lk[0OFU{KM7:TR?= M1r4eHNCVkeHUh?=
DMS-79 NUXlXYs2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfBTGMyUUN3ME2yMlY6Ojh2IN88US=> Mn:zV2FPT0WU
Detroit562 NUDvV2U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJwNkm4OFUh|ryP NFLlOHNUSU6JRWK=
HuP-T4 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TSfWlEPTB;Mj63NlgyQCEQvF2= NG\kbo5USU6JRWK=
QIMR-WIL MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJwN{W5OVIh|ryP NYrvXow2W0GQR1XS
BB65-RCC M1TYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jsWmlEPTB;Mj64NFcyOyEQvF2= M{fIWHNCVkeHUh?=
PC-3 Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzr[JZ{UUN3ME2yMlg{OzF5IN88US=> MXPTRW5ITVJ?
OVCAR-3 M4TkSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDUTWM2OD1{Lki1OVk1KM7:TR?= NEDWd|NUSU6JRWK=
KYSE-510 NFHXU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4njdGlEPTB;Mj64Olc5PiEQvF2= M1H1O3NCVkeHUh?=
HC-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;XdWJKSzVyPUKuPVQxOTJizszN NEe3PXlUSU6JRWK=
NCI-H1693 NEOwPVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW2TWM2OD1{Lkm1PFk4KM7:TR?= M4ridnNCVkeHUh?=
DU-4475 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HIZ2lEPTB;Mj65PVA2OiEQvF2= Mn\MV2FPT0WU
COLO-680N MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPLUJhEUUN3ME2zMlAxPDl3IN88US=> MojKV2FPT0WU
MN-60 NEHVWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\MPGlEPTB;Mz6wOFk4PCEQvF2= M3TqN3NCVkeHUh?=
BCPAP NEfOS|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG0b5pKSzVyPUOuNFgzQTVizszN MXLTRW5ITVJ?
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HCC1569 NGrTfmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLjcZFKSzVyPUS3MlE3PThizszN MUTTRW5ITVJ?
KGN M4j3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4e|ZjUUN3ME20O{4{OzFzIN88US=> MUXTRW5ITVJ?
LCLC-103H NHH4U3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfhUnhKSzVyPUS3MlQ1ODRizszN NG\YV4NUSU6JRWK=
SW780 M4XEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFezNYZKSzVyPUS3MlY{PTFizszN MYPTRW5ITVJ?
NCI-H1703 M4rVdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR6LkOzOVIh|ryP MXvTRW5ITVJ?
HCC1395 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR6Lke0N|Ih|ryP MWLTRW5ITVJ?

... 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 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.
化学名 N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

文献中の引用 (90)

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