Gefitinib (ZD1839)

For research use only. Not for use in humans.

製品コードS1025 別名:Iressa

Gefitinib (ZD1839)化学構造

CAS No. 184475-35-2

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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 33700 あり
JPY 26400 あり
JPY 46800 あり
最寄りの販売代理店を探す

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バルク問合せ

文献中Selleckの製品使用例(464)

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
特性 A potent EGFR tyrosine kinase inhibitor.
ターゲット
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES3e4lKSzVyPUKxMlQ3OSEQvF2= NIfETJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJzLkSzN|Eh|ryP Mnv5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HUTU-80 NFXKcWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XOTWlEPTB;MkGuOFM{PiEQvF2= M{TydFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
PA-1 NInWcotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LZTGlEPTB;MkGuNlc5PyEQvF2= NV\zWHc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HOP-62 M3\ZXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTCTWM2OD1{MT6yO|g1KM7:TR?= M1z6blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
GI-1 NFjYfmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf6e2pKSzVyPUKxMlE4KM7:TR?= M2rNSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MC116 M16xZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLqPFQ{UUN3ME2yNU4xPzJ|IN88US=> NYDMW5pORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
A375 M1;sbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX5TWM2OD1{MT6wOVY4KM7:TR?= NFjuflY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
IST-SL1 NIq5W2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\OTWM2OD1{MD63PFc6KM7:TR?= NGnlfFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
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TYK-nu NGLOU2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF7LkizO|gh|ryP NUPDT5lbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H650 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;IPGlEPTB;MUmuO|UxQCEQvF2= M1zaVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
WM-115 NX7TcJRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF7Lk[3O|Qh|ryP MkWzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HuH-7 NUG0W25HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX33VVlkUUN3ME2xPU44PDJzIN88US=> M{Tnd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-N87 NHLJWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\0TWM2OD1zOT61PVkzKM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1048 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF7LkKzNlYh|ryP NUPyRXRDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H446 M3nUUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF7LkO1PFkh|ryP NV74bVdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H1437 NUXTOWdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHKx[YlKSzVyPUG5MlA1PjdizszN NHTPdYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
D-263MG NF:5ephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfnTWM2OD1zOT6wNVczKM7:TR?= NW[5cnlMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
MFH-ino MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrM[nZDUUN3ME2xPE46PjZ7IN88US=> Ml7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
U-266 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF6Lki2OFkh|ryP NHroNWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
OVCAR-8 NX3vR44xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TXZmlEPTB;MUiuPVI4PiEQvF2= NXP4THJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
KNS-42 NEHpdZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTscGtyUUN3ME2xPE45ODF3IN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
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MFE-280 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOz[4xOUUN3ME2xPE44Ojl|IN88US=> NILhfJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H1563 M1jSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\POmlEPTB;MUiuO|EzPCEQvF2= NIDURmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
MDA-MB-361 NF\NWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV62dXNsUUN3ME2xPE42PTh6IN88US=> NILFeWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HLE Ml7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF6LkOxOFgh|ryP M{C2TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
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NCI-H1573 MknXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor1TWM2OD1zNz6yPFI3KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
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