Gefitinib (ZD1839)

For research use only. Not for use in humans.

目录号:S1025 别名: Iressa 中文名称:吉非替尼

Gefitinib (ZD1839) Chemical Structure

CAS No. 184475-35-2

Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1574.78 现货
RMB 1227.69 现货
RMB 2205.98 现货
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客户使用Selleck生产的Gefitinib (ZD1839)发表文献514篇:

产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述 Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。
特性 Gefitinib是有效的EGFR酪氨酸激酶抑制剂。
靶点
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
体外研究

Gefitinib 作用于高和低表达EGFR的细胞系,包括NR6, NR6M 和 NR6W 细胞系,有效抑制EGFR上全部酪氨酸磷酸化位点。磷酸化位点 Tyr1173和Tyr992敏感性较低,需要高浓度Gefitinib才能抑制。Gefitinib作用于NR6W细胞,高效阻断PLC-γ磷酸化, IC50为27nM。NR6wtEGFR 和NR6M细胞系具有低水平PLC-γ磷酸化, IC50 分别为 43 nM和 369 nM。Gefitinib抑制AKT磷酸化,作用于低EGFR和EGFRvIII表达的细胞系, IC50 分别为220 和263nM。Gefitinib按 0.1 到 0.5μM剂量处理,显著促进而不是废除 NR6M细胞形成集落。然而, 2μM Gefitinib 完全抑制 NR6M 集落形成。Gefitinib 作用于高和低EGFR表达的细胞系,EGF 刺激72小时后,快速抑制EGFR 和ERK 磷酸化,这种作用存在剂量依赖性。[1]Gefitinib抑制 EGF驱动的未转化MCF10A 细胞生长,IC50为 20 nM。[2] Gefitinib 作用于MDA-MB-231细胞,抑制EGF信号。Gefitinib严重抑制细胞数的增多,这种作用存在剂量依赖性。 [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 M3HoZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzzTXlWUUN3ME2yNU41PjFizszN NIDQfFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HT MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTJzLkSzN|Eh|ryP MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HUTU-80 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3izbmlEPTB;MkGuOFM{PiEQvF2= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
PA-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HDemlEPTB;MkGuNlc5PyEQvF2= NYiwb2JlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HOP-62 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ntUmlEPTB;MkGuNlc5PCEQvF2= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
GI-1 M1LnXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPO[lhsUUN3ME2yNU4yPyEQvF2= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MC116 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjsTWM2OD1{MT6wO|I{KM7:TR?= NYrxRpVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
A375 NHjPV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jpXGlEPTB;MkGuNFU3PyEQvF2= M2jJU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
IST-SL1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJyLke4O|kh|ryP Mmf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
TE-5 MmDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJyLke0PFIh|ryP M3;2W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
SiHa M4LLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rGdGlEPTB;MkCuN|cyOiEQvF2= NV:2PYlWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
LB2518-MEL MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\xdoE{UUN3ME2yNE4{PzN7IN88US=> M{D2OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
BB49-HNC Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vvZ2lEPTB;MUmuPVIh|ryP M{G4PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HGC-27 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vYN2lEPTB;MkCuNVM6PCEQvF2= MoG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
Becker NEHpSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF7Lki1OFch|ryP NVnzS3NyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
TYK-nu NYrRfWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TTPWlEPTB;MUmuPFM4QCEQvF2= MnjCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H650 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnQTWM2OD1zOT63OVA5KM7:TR?= MmX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
WM-115 NXXHbYxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXrd2pnUUN3ME2xPU43Pzd2IN88US=> NFrKcHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HuH-7 NEK3bpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX2PJNiUUN3ME2xPU44PDJzIN88US=> M4rENFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-N87 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP6UFJIUUN3ME2xPU42QTl{IN88US=> NXPGb4pFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H1048 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF7LkKzNlYh|ryP Mn;OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H446 NWXuUGVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XETmlEPTB;MUmuN|U5QSEQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1437 M4HHc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;QTWM2OD1zOT6wOFY4KM7:TR?= NULXVVI4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
D-263MG NF3jTXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7SOYFVUUN3ME2xPU4xOTd{IN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MFH-ino NYXXNopKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL6WFdzUUN3ME2xPE46PjZ7IN88US=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
U-266 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXxbVlKSzVyPUG4Mlg3PDlizszN NEnDVYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
OVCAR-8 NEjwZpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDBTWM2OD1zOD65Nlc3KM7:TR?= NY\LPGdpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
KNS-42 NXjiem5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\JSFV5UUN3ME2xPE45ODF3IN88US=> M17TUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
U251 M2DYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XPdGlEPTB;MUiuO|M1PyEQvF2= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MFE-280 NVLaSJdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTaRYJsUUN3ME2xPE44Ojl|IN88US=> NH64dGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H1563 M1jZSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi1S5JKSzVyPUG4MlcyOjRizszN Mm\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
MDA-MB-361 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLKTWM2OD1zOD61OVg5KM7:TR?= NUDsdI1NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HLE NFXYeJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\YeGZKSzVyPUG4MlMyPDhizszN NHj4dJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
SW982 NYnEeFdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF6LkSwO|Uh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
KM-H2 M{XHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknFTWM2OD1zNz65OFEyKM7:TR?= NVXHWGJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
D-502MG M1izbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHHTWM2OD1zNz65PFA5KM7:TR?= Mk\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
ES8 NWnUXpJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rqfmlEPTB;MUeuPFU6OyEQvF2= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
SF268 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfDdlFLUUN3ME2xO{43QTZ7IN88US=> NEfzWII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
Calu-6 MnHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\obIFCUUN3ME2xO{43Pzh{IN88US=> NV;oW45ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SW1783 MoXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWxWIRIUUN3ME2xO{43PDF3IN88US=> NH2wdpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H747 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7FTWM2OD1zNz61Nlk4KM7:TR?= NHfvUFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
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