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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MDA-MB-231 NHfwTmZEgXSxdH;4bYMhSXO|YYm= NEHucnc6PiCq M3;rPGROW09? NX7SWZVzUUN3ME2zOk43OSEQvF2= NFTmNI4yQDNzM{iwOy=>
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Plasmodium falciparum NGHyOWJyUFSVIIDyc4ZqdGmwZzDmc5IhcW6qaXLpeI9zeyCxZjDQcIF{dW:maYXtJIZidGOrcHHyeY0heHKxbHnm[ZJifGmxbh?= NFi2VGIzOThzN{C0OS=>
NCI-H1993 M1nQZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7He3p1PzJiaB?= M2rjfWROW09? MUPJR|UxRTBwMTFOwG0> M4TXRlIyQTF4NEOz
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A431 NF;CUFhMcW6jc3WgRZN{[Xl? NHHYc2gzKGh? NW\DNpd3TE2VTx?= NH\H[FBKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIFG0N|Ehf2m2aDDJR|UxKG:oIECuNFAyKM7:TR?= M1PyRVIzOTBzMUOy
MCF7 NVu2cWhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e0SlExOMLizsznM41N M4XvZVQ5KGh? NGLocppFVVOR M1qzXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDveoVz\XiycnXzd4lv\yCHR1\SJIdmdmVid3n0bEBKSzVyIH;mJFEzNjB3IN88US=> MmLGNlIyOTlzM{C=
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MCF7 M2PoN2N6fG:2b4jpZ{BCe3OjeR?= MlTRNVAh|ryP MUK0PEBp M2jSXmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHOncoXtMZN1[XK4ZXSgbJVu[W5iTVPGO{Bk\WyuczDveoVzNWW6cILld5NqdmdiRYLiRlIh[2WubIO= M4mxSVIzOTN6M{C4
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NCI-H358 NULRZnBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XPU2lEPTB;NUK3MlY3KG6P MXHTRW5ITVJ?
KYSE-180 NHnOZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X5eGlEPTB;NUOwMlYzKG6P Mme0V2FPT0WU
NCI-H82 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3NTWM2OD13NECuOUBvVQ>? NWm0XHhyW0GQR1XS
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RS4-11 NY\XT5RZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDzTWM2OD13NkiuOVkhdk1? MWPTRW5ITVJ?
CAN NEjxeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P0S2lEPTB;NUiwMlc3KG6P MlnNV2FPT0WU
Ca9-22 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P1TWlEPTB;NUi4MlY1KG6P MoTpV2FPT0WU
CAL-39 M3q5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnQTWM2OD13OU[uN{BvVQ>? NWXWOYxiW0GQR1XS
NCI-H1623 NHLOd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvXO2JJUUN3ME21PVkvOzZibl2= NVHoNolXW0GQR1XS
FADU NFj0NYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLZNINGUUN3ME22NFQvPjlibl2= M2C4c3NCVkeHUh?=
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Ramos-2G6-4C10 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTZ{MT60OkBvVQ>? MWHTRW5ITVJ?
LB1047-RCC NVL2cHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDWlRQUUN3ME22NlUvOjlibl2= NUPONmVEW0GQR1XS
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COR-L105 NV31PWRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\PUod1UUN3ME22OlIvPTNibl2= M4POOnNCVkeHUh?=
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L-363 Ml3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnYOGdPUUN3ME22O|EvQTRibl2= MkiwV2FPT0WU
LU-134-A NFLs[oRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfOTWM2OD15MUmuNFkhdk1? M4fPVnNCVkeHUh?=
NCI-H1770 M13xU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTd{Mj60JI5O MoDiV2FPT0WU
HAL-01 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj6VmhpUUN3ME23N|QvPzFibl2= M13zenNCVkeHUh?=
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TE-6 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e0SmlEPTB;N{[0MlMyKG6P NYLoPI8yW0GQR1XS
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LU-135 NFfDe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkewTWM2OD15OEOuNFMhdk1? NYHRT5IzW0GQR1XS
EC-GI-10 NIi5O2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjhTWM2OD15OEiuOVIhdk1? NGjze5RUSU6JRWK=
TE-12 NV76cXJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[3XmlEPTB;OEKxMlEyKG6P M1z2bHNCVkeHUh?=
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23132-87 NHiybVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHuVpBKSzVyPUi2OE4zQCCwTR?= MnT4V2FPT0WU
AU565 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjX[JBRUUN3ME24OlkvPiCwTR?= NF3aPVNUSU6JRWK=
DEL MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jjRmlEPTB;OEe3MlY2KG6P M4HubHNCVkeHUh?=
COR-L88 M1;5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvaTWM2OD16OEKuNlYhdk1? NVO5do13W0GQR1XS
NCI-H2126 NH;DfXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjjd5lKSzVyPUi4Nk45OyCwTR?= MojKV2FPT0WU
CAPAN-1 NWrxW5N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTh6Mz6yPUBvVQ>? NGi1[m9USU6JRWK=
BT-474 M1TPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe4NGxKSzVyPUmzPE4yPCCwTR?= NH[5d5lUSU6JRWK=
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HT-3 Ml[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTl6Mj60NUBvVQ>? MV\TRW5ITVJ?
SK-NEP-1 M4Pvemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG4TIt7UUN3ME25PFkvPDRibl2= NV\6[5ZEW0GQR1XS
MS-1 M4[zfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTl7ND62PUBvVQ>? M3fXR3NCVkeHUh?=
DOHH-2 NUOycWJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\hPZdKSzVyPUGuNFAxOjFizszN M4DIdXNCVkeHUh?=
NCI-H1304 NYHYRnB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnac4JRUUN3ME2xMlAyPjR|IN88US=> M4fXd3NCVkeHUh?=
EM-2 MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3f5UWlEPTB;MT6wN|AyPiEQvF2= MVTTRW5ITVJ?
MHH-PREB-1 NVjON41DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVruO2VGUUN3ME2xMlA5PDVzIN88US=> NUXWeY1JW0GQR1XS
KU-19-19 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHqz[4dKSzVyPUGuNFg2PDFizszN MX3TRW5ITVJ?
NCI-H1648 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwMUC2NVYh|ryP MXfTRW5ITVJ?
MKN1 M2f5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfO[XVKSzVyPUGuNlE6QDdizszN NHf5bXdUSU6JRWK=
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OAW-42 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rudGlEPTB;MT6yO|gzPSEQvF2= NUP0WVEyW0GQR1XS
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SW1088 MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTFwMkm2NFch|ryP MoTZV2FPT0WU
GCIY MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[1Z2lEPTB;MT6zNFE{OiEQvF2= NUHiVXRqW0GQR1XS
CTV-1 NEXCd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37RZmlEPTB;MT6zNFgh|ryP NVzmZlZ{W0GQR1XS
NCI-H1092 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPudYFNUUN3ME2xMlMxQDVizszN NFn5b4tUSU6JRWK=
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NCI-H1650 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX6emRYUUN3ME2xMlM{PDh{IN88US=> NYH2ZYluW0GQR1XS
SW954 NFjCTW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLmTWM2OD1zLkO0NFQ5KM7:TR?= MlfaV2FPT0WU
SW48 Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jWc2lEPTB;MT6zOlYyQCEQvF2= MYDTRW5ITVJ?
SK-N-DZ NF3Je4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwM{[5OFch|ryP NUm3fG42W0GQR1XS
KMOE-2 NHfnTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwM{m4NVUh|ryP MlLTV2FPT0WU
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NCI-H526 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPITWM2OD1zLkSzPFI3KM7:TR?= NFu3epVUSU6JRWK=
697 M2KwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7md3JKSzVyPUGuOFQyODRizszN M1jzVXNCVkeHUh?=
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BE-13 M2PuZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETEUoZKSzVyPUGuOVA3PzFizszN NV:zbpY2W0GQR1XS
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SCC-25 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvkTWM2OD1zLkWyN|IzKM7:TR?= NVjQW5drW0GQR1XS
LAMA-84 M1;KZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFwNUO4NVUh|ryP NI\pUJdUSU6JRWK=
HSC-3 MmO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwNUSzPEDPxE1? NIrBZoNUSU6JRWK=
BT-549 M{DaR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jPe2lEPTB;MT61PFc1PyEQvF2= MXLTRW5ITVJ?
ML-2 NX3vRZlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TuW2lEPTB;MT62OFAzQSEQvF2= NHnCUGhUSU6JRWK=
BB30-HNC NH:zT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[5TWM2OD1zLk[4PVczKM7:TR?= NUPUWHdEW0GQR1XS
PANC-03-27 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3vTI5KSzVyPUGuO|AyOzlizszN MXvTRW5ITVJ?
COLO-678 MkCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4e0WWlEPTB;MT63N|Q1PCEQvF2= M2jmOnNCVkeHUh?=
NCI-H1666 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fzTGlEPTB;MT63OFcxPCEQvF2= M{nzWHNCVkeHUh?=
NCI-H209 M2\4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzoeXVKSzVyPUGuO|czPjlizszN NYHVZ|BqW0GQR1XS
EPLC-272H MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnjV2NKSzVyPUGuPFU2PDlizszN M3vybHNCVkeHUh?=
OMC-1 NEf4VYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzrV3pKSzVyPUGuPVk5QDhizszN NF24NnFUSU6JRWK=
HCC70 Mlu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm1ZoVMUUN3ME2yMlAxQDF3IN88US=> M2G2WHNCVkeHUh?=
CAL-12T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfoV4NpUUN3ME2yMlAyQDZzIN88US=> Ml3QV2FPT0WU
TGBC24TKB M4mxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT5dFlKSzVyPUKuNFI6PjFizszN NV60NYpDW0GQR1XS
EKVX M3nQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXmzV2VXUUN3ME2yMlA1QTN7IN88US=> Mm\TV2FPT0WU
SW1116 M3;xeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPpV4RKSzVyPUKuNFYxODlizszN MlH5V2FPT0WU
NCI-H2009 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fucWlEPTB;Mj6wOlIyPCEQvF2= NY\pNIhWW0GQR1XS
RPMI-8866 NYXh[oNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrNc3g5UUN3ME2yMlA5PDhzIN88US=> MYnTRW5ITVJ?
KARPAS-45 M3fBc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXPXoJKSzVyPUKuNVI1PzlizszN NGfab5VUSU6JRWK=
RXF393 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjzTWM2OD1{LkGzNFM3KM7:TR?= M4Lp[XNCVkeHUh?=
786-0 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvyZmNKSzVyPUKuNVg1ODZizszN M{DN[nNCVkeHUh?=
SCC-4 NXzIbJc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HuWWlEPTB;Mj6yNVc4PiEQvF2= NXPaV4pUW0GQR1XS
BT-20 MoXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJwMk[3OFQh|ryP M4jSZXNCVkeHUh?=
A498 M4jzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rjS2lEPTB;Mj6yPVQyPSEQvF2= MXPTRW5ITVJ?
IGROV-1 M4m1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLZW252UUN3ME2yMlMyOjN5IN88US=> NGfE[|BUSU6JRWK=
JVM-3 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn4TmJYUUN3ME2yMlM1PjR|IN88US=> MnnDV2FPT0WU
NCI-H2170 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJwM{S3PFMh|ryP NW\jNolIW0GQR1XS
EW-18 NYfrUItCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHiU4o5UUN3ME2yMlM2PDdzIN88US=> MVjTRW5ITVJ?
KU812 MnXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zsN2lEPTB;Mj6zOlc4QSEQvF2= NFHqV|JUSU6JRWK=
NY MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;iPYY1UUN3ME2yMlM4OjdizszN MYPTRW5ITVJ?
HTC-C3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3nTWM2OD1{LkSyNlY4KM7:TR?= MV3TRW5ITVJ?
CFPAC-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfmTWM2OD1{LkSzPFY1KM7:TR?= NVPhN2hvW0GQR1XS
HH Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TT[GlEPTB;Mj60PVg2PCEQvF2= NUTTT45VW0GQR1XS
MKN7 NYiyVHpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJwNkK3OFgh|ryP NX3oO2dPW0GQR1XS
TE-8 MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfHTWM2OD1{Lk[zOlU{KM7:TR?= MYHTRW5ITVJ?
MC-IXC NWL4[4VPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Pm[mlEPTB;Mj62OFQ2OyEQvF2= NEDyfXZUSU6JRWK=
DMS-79 M1u1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PkS2lEPTB;Mj62PVI5PCEQvF2= M2O2N3NCVkeHUh?=
Detroit562 NEHSboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXCTWM2OD1{Lk[5PFQ2KM7:TR?= NHnlR|RUSU6JRWK=
HuP-T4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XyV2lEPTB;Mj63NlgyQCEQvF2= NXfRWVJ3W0GQR1XS
QIMR-WIL M{LF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJwN{W5OVIh|ryP NHvNWHNUSU6JRWK=
BB65-RCC M1XQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPISIg5UUN3ME2yMlgxPzF|IN88US=> MoDKV2FPT0WU
PC-3 NHvQe45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH3eI5KSzVyPUKuPFM{OTdizszN NEf1TWZUSU6JRWK=
OVCAR-3 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmzenRtUUN3ME2yMlg2PTl2IN88US=> M4rnVHNCVkeHUh?=
KYSE-510 NGrYeW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH0[2pKSzVyPUKuPFY4QDZizszN MV3TRW5ITVJ?
HC-1 NIDoSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\GTWM2OD1{Lkm0NFEzKM7:TR?= M2rPSHNCVkeHUh?=
NCI-H1693 NX7JV|JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\xO411UUN3ME2yMlk2QDl5IN88US=> MlPPV2FPT0WU
DU-4475 MmHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfiOVNnUUN3ME2yMlk6ODV{IN88US=> MoTZV2FPT0WU
COLO-680N M2rz[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNwMEC0PVUh|ryP MnzPV2FPT0WU
MN-60 NILlXGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfQTWM2OD1|LkC0PVc1KM7:TR?= MkS4V2FPT0WU
BCPAP MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrpTWM2OD1|LkC4Nlk2KM7:TR?= MoHLV2FPT0WU
647-V M3Tv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTNwMU[yNkDPxE1? NGTGSJdUSU6JRWK=
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HCC1569 NUWwTZcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OwNGlEPTB;NEeuNVY2QCEQvF2= MlO2V2FPT0WU
KGN MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTwW5RKSzVyPUS3MlM{OTFizszN NILTfYlUSU6JRWK=
LCLC-103H MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;GfWRKSzVyPUS3MlQ1ODRizszN NILsdGhUSU6JRWK=
SW780 M37xfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrFTWM2OD12Nz62N|UyKM7:TR?= M4nQR3NCVkeHUh?=
NCI-H1703 NHi2SXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETse3RKSzVyPUS4MlM{PTJizszN M1LJcHNCVkeHUh?=
HCC1395 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP6TWM2OD12OD63OFMzKM7:TR?= MUHTRW5ITVJ?

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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