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479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 NWHVTY9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHO[HJqUUN3ME2yNU41PjFizszN Mny1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HT Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorGTWM2OD1{MT60N|MyKM7:TR?= M2\ZOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HUTU-80 M2T6e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fofmlEPTB;MkGuOFM{PiEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
PA-1 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn6cWRWUUN3ME2yNU4zPzh5IN88US=> Mn;2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HOP-62 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJzLkK3PFQh|ryP NUPqcW1vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
GI-1 NF7FW4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJzLkG3JO69VQ>? Mm\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
MC116 NXrsfFdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm3NHhvUUN3ME2yNU4xPzJ|IN88US=> MojxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
A375 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOzUGxnUUN3ME2yNU4xPTZ5IN88US=> M1z4N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
IST-SL1 M1\LfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTJyLke4O|kh|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
TE-5 M{O3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJyLke0PFIh|ryP NYnuOIJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SiHa M4\zRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fyVGlEPTB;MkCuN|cyOiEQvF2= MkDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
LB2518-MEL MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvjOHVKSzVyPUKwMlM4OzlizszN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
BB49-HNC M{\BUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf3W2M{UUN3ME2xPU46OiEQvF2= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HGC-27 NFPRSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fmNGlEPTB;MkCuNVM6PCEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
Becker NF7ZXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX34SHhlUUN3ME2xPU45PTR5IN88US=> Mm\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
TYK-nu M{HP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PUemlEPTB;MUmuPFM4QCEQvF2= NELPV5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H650 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3uRY1SUUN3ME2xPU44PTB6IN88US=> MlG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
WM-115 NHfhZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF7Lk[3O|Qh|ryP MmfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HuH-7 NW\JUIJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjMTWM2OD1zOT63OFIyKM7:TR?= NFKwNnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-N87 M3vzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TqOmlEPTB;MUmuOVk6OiEQvF2= NYTsNI1oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H1048 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF7LkKzNlYh|ryP NVPBSWpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H446 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj5VGtKSzVyPUG5MlM2QDlizszN MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1437 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfjbFhZUUN3ME2xPU4xPDZ5IN88US=> NGqzOXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
D-263MG MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF7LkCxO|Ih|ryP M4KyUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MFH-ino MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XtTWlEPTB;MUiuPVY3QSEQvF2= NFHq[4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
U-266 M2r5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfT[pBKSzVyPUG4Mlg3PDlizszN MmTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
OVCAR-8 NYfDd4U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWL0SZhrUUN3ME2xPE46Ojd4IN88US=> M4HWcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
KNS-42 MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[xfXNKSzVyPUG4MlgxOTVizszN MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
U251 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLHTWM2OD1zOD63N|Q4KM7:TR?= NESyPHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
MFE-280 Ml3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\QXll{UUN3ME2xPE44Ojl|IN88US=> M3X3UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1563 NIPuPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF6LkexNlQh|ryP M{ixNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MDA-MB-361 MmrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF6LkW1PFgh|ryP Mm\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HLE MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF6LkOxOFgh|ryP MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
SW982 M3Xje2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;NNGlEPTB;MUiuOFA4PSEQvF2= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
KM-H2 MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrZd29mUUN3ME2xO{46PDFzIN88US=> M{myclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
D-502MG MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G5SWlEPTB;MUeuPVgxQCEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
ES8 NGnYOHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF5Lki1PVMh|ryP NEPJdZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
SF268 NHzVVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jHWWlEPTB;MUeuOlk3QSEQvF2= NYf6ToNDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
Calu-6 NH3BW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P5cmlEPTB;MUeuOlc5OiEQvF2= NGi1NlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
SW1783 M2jHXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDneWhrUUN3ME2xO{43PDF3IN88US=> NITXNow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H747 NEjMcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF5LkWyPVch|ryP MnK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H1573 NXfubIRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTF5LkK4NlYh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
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