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538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 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL0XZprUUN3ME2yNU41PjFizszN NVrxbppNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HT MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJzLkSzN|Eh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HUTU-80 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDyUIRKSzVyPUKxMlQ{OzZizszN M{\rUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
PA-1 M3[4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGKydJVKSzVyPUKxMlI4QDdizszN MnHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HOP-62 M{TxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJzLkK3PFQh|ryP NXPxN4dpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
GI-1 NEnrWGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7lU2VKSzVyPUKxMlE4KM7:TR?= M2rGUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MC116 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYji[XBmUUN3ME2yNU4xPzJ|IN88US=> NGjiN5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
A375 NEHn[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;oUmlEPTB;MkGuNFU3PyEQvF2= NFvTZW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
IST-SL1 NFPXcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLZTWM2OD1{MD63PFc6KM7:TR?= MlfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
TE-5 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;kNpdKSzVyPUKwMlc1QDJizszN MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
SiHa NEjUPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJyLkO3NVIh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
LB2518-MEL MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:1cW9KSzVyPUKwMlM4OzlizszN NWfkb3hZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
BB49-HNC M1vHSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XzeWlEPTB;MUmuPVIh|ryP MnL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HGC-27 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTJyLkGzPVQh|ryP NX3RbZh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
Becker NXTkPWFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF7Lki1OFch|ryP NGH5dnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
TYK-nu MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTF7LkizO|gh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H650 M1HE[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDnNmpKSzVyPUG5Mlc2ODhizszN NXPNfos{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
WM-115 M4nKPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3uwPGlEPTB;MUmuOlc4PCEQvF2= MnjPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HuH-7 NIP5OXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7sc4M4UUN3ME2xPU44PDJzIN88US=> MkL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-N87 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYntfGRHUUN3ME2xPU42QTl{IN88US=> M1jkbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1048 M2j0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLWTWM2OD1zOT6yN|I3KM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H446 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrCfZFKSzVyPUG5MlM2QDlizszN M4XiPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1437 MkHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTh[XJKSzVyPUG5MlA1PjdizszN M1O4eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
D-263MG NUL3e5BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDYbGdXUUN3ME2xPU4xOTd{IN88US=> M3LU[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MFH-ino MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLCTWM2OD1zOD65OlY6KM7:TR?= M1nZXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
U-266 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPQUnFpUUN3ME2xPE45PjR7IN88US=> NHzLe4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
OVCAR-8 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fxfGlEPTB;MUiuPVI4PiEQvF2= NH24[VU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
KNS-42 NWnVS3MzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF6LkiwNVUh|ryP NGrCXpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
U251 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33XVmlEPTB;MUiuO|M1PyEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MFE-280 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF6LkeyPVMh|ryP MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1563 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[yTWM2OD1zOD63NVI1KM7:TR?= MoXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
MDA-MB-361 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jaOGlEPTB;MUiuOVU5QCEQvF2= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HLE MmPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NECzTW9KSzVyPUG4MlMyPDhizszN NWPXblduRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SW982 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXPeGdYUUN3ME2xPE41ODd3IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
KM-H2 NVv5PZhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\Ed3dKSzVyPUG3Mlk1OTFizszN NX[3epczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
D-502MG NFvqdpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn0doJtUUN3ME2xO{46QDB6IN88US=> M4PZSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
ES8 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrVTWM2OD1zNz64OVk{KM7:TR?= M4XKOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
SF268 NHmwVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nKbWlEPTB;MUeuOlk3QSEQvF2= NUKxUGJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
Calu-6 M1XRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILJZVRKSzVyPUG3MlY4QDJizszN MorCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
SW1783 NFzTdoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfuTWM2OD1zNz62OFE2KM7:TR?= Mn3NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H747 Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF5LkWyPVch|ryP M{jrblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1573 NIfaSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF5LkK4NlYh|ryP NXnab20xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
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