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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HN MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Gw[2lEPTB;NUG3MlM5KG6P NGDVV4FUSU6JRWK=
SCC-15 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\UVpFKSzVyPUWyOU43QCCwTR?= MU\TRW5ITVJ?
NCI-H358 NF;ibWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTV{Nz62OkBvVQ>? Mn\mV2FPT0WU
KYSE-180 NFPOZ2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPwfVBKSzVyPUWzNE43OiCwTR?= MX3TRW5ITVJ?
NCI-H82 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKweXhTUUN3ME21OFAvPSCwTR?= MUHTRW5ITVJ?
NB7 NGj6WnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHxTWM2OD13NE[uN|Ihdk1? NF7Lb4hUSU6JRWK=
DSH1 MoL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXtTWM2OD13Nk[uPFghdk1? MXvTRW5ITVJ?
RS4-11 M3HSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;hTWM2OD13NkiuOVkhdk1? MkPCV2FPT0WU
CAN Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnrfotKSzVyPUW4NE44PiCwTR?= MWfTRW5ITVJ?
Ca9-22 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG0dYZKSzVyPUW4PE43PCCwTR?= MYjTRW5ITVJ?
CAL-39 NGHyeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPaeI9KSzVyPUW5Ok4{KG6P NVG5bmVoW0GQR1XS
NCI-H1623 NV2zSJE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P3XWlEPTB;NUm5MlM3KG6P M1zGVHNCVkeHUh?=
FADU Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTKTWM2OD14MESuOlkhdk1? MoLWV2FPT0WU
NB69 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTZzND6zOUBvVQ>? Mn7pV2FPT0WU
Ramos-2G6-4C10 NHvtXGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvzUGkzUUN3ME22NlEvPDZibl2= Mn3lV2FPT0WU
LB1047-RCC M1\jbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLZdoxKSzVyPU[yOU4zQSCwTR?= NWrxR5ROW0GQR1XS
MV-4-11 NWntOoVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjOenVKSzVyPU[yO{44KG6P NUTwVlRXW0GQR1XS
DBTRG-05MG NHXMOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnVOlI6UUN3ME22N|IvOjhibl2= NFjJc25USU6JRWK=
ME-180 NE\1fFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvQTWM2OD14M{KuPUBvVQ>? M1fRdnNCVkeHUh?=
NBsusSR MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG2O|BkUUN3ME22OFYvPTJibl2= NWL4T3lIW0GQR1XS
COR-L105 NEDYXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvDVI9KSzVyPU[2Nk42OyCwTR?= M3PY[HNCVkeHUh?=
ETK-1 Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle4TWM2OD14NkKuOVkhdk1? MmDiV2FPT0WU
L-363 NH3oT5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF71TZpKSzVyPU[3NU46PCCwTR?= M4DpNnNCVkeHUh?=
LU-134-A NHnpZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTdzOT6wPUBvVQ>? MmLvV2FPT0WU
NCI-H1770 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jU[GlEPTB;N{KyMlQhdk1? NW\3Vld1W0GQR1XS
HAL-01 MonvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPQZWdKSzVyPUezOE44OSCwTR?= NGC0U|RUSU6JRWK=
COLO-684 NGjQR3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTd3Mz6wNUBvVQ>? NGL6NGtUSU6JRWK=
TE-6 M{\OUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr3WoVEUUN3ME23OlQvOzFibl2= M4m5N3NCVkeHUh?=
A431 NFXFbVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTd6MD6wOEBvVQ>? Mm\MV2FPT0WU
LU-135 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTjTWM2OD15OEOuNFMhdk1? Mo\kV2FPT0WU
EC-GI-10 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH0XZRwUUN3ME23PFgvPTJibl2= MYPTRW5ITVJ?
TE-12 NGj5NWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHThTW9KSzVyPUiyNU4yOSCwTR?= M1nT[3NCVkeHUh?=
LoVo NIq2cYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPtPXpVUUN3ME24OVkvODZibl2= MnHYV2FPT0WU
23132-87 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTh4ND6yPEBvVQ>? MnLyV2FPT0WU
AU565 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnj0TWM2OD16NkmuOkBvVQ>? Mnf0V2FPT0WU
DEL M13MWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fObGlEPTB;OEe3MlY2KG6P MWPTRW5ITVJ?
COR-L88 M1yyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;FbppHUUN3ME24PFIvOjZibl2= NGXzO|FUSU6JRWK=
NCI-H2126 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13hWWlEPTB;OEiyMlg{KG6P MVXTRW5ITVJ?
CAPAN-1 NWLsfop1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTh6Mz6yPUBvVQ>? NYjMW|YyW0GQR1XS
BT-474 NIXGV4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK1OGVWUUN3ME25N|gvOTRibl2= MXXTRW5ITVJ?
BHY NX7q[XRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnTe|RVUUN3ME25O|UvPDhibl2= MYPTRW5ITVJ?
HT-3 NVnLeI9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7CPGQ3UUN3ME25PFIvPDFibl2= NXjPT3RVW0GQR1XS
SK-NEP-1 NUDxSpJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnvbG9KUUN3ME25PFkvPDRibl2= MXTTRW5ITVJ?
MS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq4RW5KSzVyPUm5OE43QSCwTR?= NFHWfmVUSU6JRWK=
DOHH-2 NHHFNWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXEOZViUUN3ME2xMlAxODJzIN88US=> MW\TRW5ITVJ?
NCI-H1304 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPI[IZnUUN3ME2xMlAyPjR|IN88US=> NH;UN2hUSU6JRWK=
EM-2 M2j2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonPTWM2OD1zLkCzNFE3KM7:TR?= NEHpW4hUSU6JRWK=
MHH-PREB-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe1VFJ2UUN3ME2xMlA5PDVzIN88US=> NY[1XGZ{W0GQR1XS
KU-19-19 NEnaTIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPQTWM2OD1zLkC4OVQyKM7:TR?= M3PrT3NCVkeHUh?=
NCI-H1648 NVPXUWNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzlTWM2OD1zLkGwOlE3KM7:TR?= M4f0TnNCVkeHUh?=
MKN1 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwMkG5PFch|ryP MWXTRW5ITVJ?
SNU-449 NIXGUWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzETWM2OD1zLkKyNlA5KM7:TR?= M{jGPHNCVkeHUh?=
OAW-42 Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzBSm1KSzVyPUGuNlc5OjVizszN NGnuR3RUSU6JRWK=
769-P NXrNWWlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3yUoZoUUN3ME2xMlI4QTF6IN88US=> MnjhV2FPT0WU
SW1088 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\hZo5vUUN3ME2xMlI6PjB5IN88US=> MoTyV2FPT0WU
GCIY Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KyW2lEPTB;MT6zNFE{OiEQvF2= MVXTRW5ITVJ?
CTV-1 NGT5SHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfjTWM2OD1zLkOwPEDPxE1? NIH2dXRUSU6JRWK=
NCI-H1092 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HjNWlEPTB;MT6zNFg2KM7:TR?= MoPLV2FPT0WU
NKM-1 M1HKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPRTWM2OD1zLkOyOVk4KM7:TR?= NX\XcJduW0GQR1XS
NCI-H1650 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljxTWM2OD1zLkOzOFgzKM7:TR?= M2f5dXNCVkeHUh?=
SW954 NVft[FlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X6eGlEPTB;MT6zOFA1QCEQvF2= NFrMO5lUSU6JRWK=
SW48 NVP4dHNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlX5TWM2OD1zLkO2OlE5KM7:TR?= MoLWV2FPT0WU
SK-N-DZ NF7mcohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TLUGlEPTB;MT6zOlk1PyEQvF2= MXPTRW5ITVJ?
KMOE-2 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvuTpYxUUN3ME2xMlM6QDF3IN88US=> M2\nc3NCVkeHUh?=
NB5 MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC5bJpxUUN3ME2xMlQxQDl2IN88US=> M3nhS3NCVkeHUh?=
CCRF-CEM NWnkRYtFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PERmlEPTB;MT60NVEyKM7:TR?= MVHTRW5ITVJ?
RH-1 M4LReWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vlcGlEPTB;MT60NVE{PiEQvF2= NWPjc2FPW0GQR1XS
NCI-H526 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3qZ45RUUN3ME2xMlQ{QDJ4IN88US=> NHy2[5VUSU6JRWK=
697 MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWThPIx5UUN3ME2xMlQ1OTB2IN88US=> M{XqbHNCVkeHUh?=
J82 NX;BRXhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFwNEW3OlYh|ryP NUWxXoxjW0GQR1XS
BE-13 M{j5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD4blhKSzVyPUGuOVA3PzFizszN MXXTRW5ITVJ?
SAS M1;WUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1qzVGlEPTB;MT61NVYzOiEQvF2= MUfTRW5ITVJ?
SCC-25 NWj5[phDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DqOmlEPTB;MT61NlMzOiEQvF2= M4LuVXNCVkeHUh?=
LAMA-84 MnfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwNUO4NVUh|ryP NGG4[I5USU6JRWK=
HSC-3 NFTiOYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTnTWM2OD1zLkW0N|gh|ryP MYTTRW5ITVJ?
BT-549 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFwNUi3OFch|ryP MWDTRW5ITVJ?
ML-2 M1\PVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3HWphKSzVyPUGuOlQxOjlizszN MXfTRW5ITVJ?
BB30-HNC NXrRR|B{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSwc|hKSzVyPUGuOlg6PzJizszN M1;mUHNCVkeHUh?=
PANC-03-27 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLaTWM2OD1zLkewNVM6KM7:TR?= MUfTRW5ITVJ?
COLO-678 NWD3[otKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;JTWM2OD1zLkezOFQ1KM7:TR?= M4H2UnNCVkeHUh?=
NCI-H1666 MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn5TWM2OD1zLke0O|A1KM7:TR?= NYjk[JNEW0GQR1XS
NCI-H209 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwN{eyOlkh|ryP M1m1NHNCVkeHUh?=
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OMC-1 NHH1NVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTFwOUm4PFgh|ryP M3:2OnNCVkeHUh?=
HCC70 NHrLcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjuU5ZKSzVyPUKuNFA5OTVizszN MojHV2FPT0WU
CAL-12T NIHDWmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJwMEG4OlEh|ryP NYHvbZdvW0GQR1XS
TGBC24TKB M3fXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LTZ2lEPTB;Mj6wNlk3OSEQvF2= M1rkfnNCVkeHUh?=
EKVX MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz2fVl{UUN3ME2yMlA1QTN7IN88US=> MmfyV2FPT0WU
SW1116 NXvtVItsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3m5TGlEPTB;Mj6wOlAxQSEQvF2= NUDvdFFvW0GQR1XS
NCI-H2009 NVH6[YFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHkdIx7UUN3ME2yMlA3OjF2IN88US=> M2XwNHNCVkeHUh?=
RPMI-8866 NFLmXIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{GxUGlEPTB;Mj6wPFQ5OSEQvF2= MkOyV2FPT0WU
KARPAS-45 Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJwMUK0O|kh|ryP M2C1OnNCVkeHUh?=
RXF393 NG\rUmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ofIFKSzVyPUKuNVMxOzZizszN MoC0V2FPT0WU
786-0 Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJwMUi0NFYh|ryP NHO1NWNUSU6JRWK=
SCC-4 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTPOFkxUUN3ME2yMlIyPzd4IN88US=> MXPTRW5ITVJ?
BT-20 NH;md5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJwMk[3OFQh|ryP NV\hV3BSW0GQR1XS
A498 M2DjOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\ON4hKSzVyPUKuNlk1OTVizszN MXjTRW5ITVJ?
IGROV-1 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzEV2hKSzVyPUKuN|EzOzdizszN MkTwV2FPT0WU
JVM-3 NVP2[4JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwM{S2OFMh|ryP NXzTZ3dRW0GQR1XS
NCI-H2170 NV;NSodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;HcnVKSzVyPUKuN|Q4QDNizszN MlzWV2FPT0WU
EW-18 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJwM{W0O|Eh|ryP NVPrfZJHW0GQR1XS
KU812 NWDQXVF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnnbGM1UUN3ME2yMlM3Pzd7IN88US=> MnXvV2FPT0WU
NY NIDkdnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvmTWM2OD1{LkO3Nlch|ryP NGjjbW1USU6JRWK=
HTC-C3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJwNEKyOlch|ryP NGfwRmpUSU6JRWK=
CFPAC-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DYfGlEPTB;Mj60N|g3PCEQvF2= MmfzV2FPT0WU
HH MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJwNEm4OVQh|ryP M4n5d3NCVkeHUh?=
MKN7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi0WFd5UUN3ME2yMlYzPzR6IN88US=> NGfzepVUSU6JRWK=
TE-8 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX75T|lsUUN3ME2yMlY{PjV|IN88US=> MXjTRW5ITVJ?
MC-IXC NIXGbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljXTWM2OD1{Lk[0OFU{KM7:TR?= MnG2V2FPT0WU
DMS-79 M2rlTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO2TWM2OD1{Lk[5Nlg1KM7:TR?= NG[0WWJUSU6JRWK=
Detroit562 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjZfGNVUUN3ME2yMlY6QDR3IN88US=> MYHTRW5ITVJ?
HuP-T4 NInVXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLhe5dNUUN3ME2yMlczQDF6IN88US=> M1nhbnNCVkeHUh?=
QIMR-WIL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn0d4Z2UUN3ME2yMlc2QTV{IN88US=> MXHTRW5ITVJ?
BB65-RCC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJwOEC3NVMh|ryP NEC5bZZUSU6JRWK=
PC-3 NF\FSY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WzNGlEPTB;Mj64N|MyPyEQvF2= MVjTRW5ITVJ?
OVCAR-3 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPxOY1UUUN3ME2yMlg2PTl2IN88US=> NVq5RYE6W0GQR1XS
KYSE-510 NIj6W4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7MbWxFUUN3ME2yMlg3Pzh4IN88US=> NULycZB{W0GQR1XS
HC-1 M3H0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJwOUSwNVIh|ryP M{W5ZXNCVkeHUh?=
NCI-H1693 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz6bYFkUUN3ME2yMlk2QDl5IN88US=> MYPTRW5ITVJ?
DU-4475 NWPa[nJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnu5TWM2OD1{Lkm5NFUzKM7:TR?= MknxV2FPT0WU
COLO-680N M3zqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C4VWlEPTB;Mz6wNFQ6PSEQvF2= MnzZV2FPT0WU
MN-60 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m3e2lEPTB;Mz6wOFk4PCEQvF2= M4rOS3NCVkeHUh?=
BCPAP NE[0V2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XRNGlEPTB;Mz6wPFI6PSEQvF2= MonJV2FPT0WU
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CAL-62 M3nYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jLVmlEPTB;Nz6zPVg3PiEQvF2= M{\SZnNCVkeHUh?=
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KGN NHXUV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTR5LkOzNVEh|ryP MoXxV2FPT0WU
LCLC-103H MnPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV31eJJYUUN3ME20O{41PDB2IN88US=> NHP6O49USU6JRWK=
SW780 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjWXW1KSzVyPUS3MlY{PTFizszN NITNWoVUSU6JRWK=
NCI-H1703 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTYTWM2OD12OD6zN|UzKM7:TR?= NF7SeIFUSU6JRWK=
HCC1395 MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XpPWlEPTB;NEiuO|Q{OiEQvF2= NYG2WHNTW0GQR1XS

... 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

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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