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563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 NYPXe25JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\xcGlEPTB;MkGuOFYyKM7:TR?= M1X6eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HT NYfMWmRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJzLkSzN|Eh|ryP NFvs[GM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HUTU-80 NIjleINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDZe5VKSzVyPUKxMlQ{OzZizszN MnTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
PA-1 NYHJN5F3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmezTWM2OD1{MT6yO|g4KM7:TR?= NVjrUJk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HOP-62 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LPNmlEPTB;MkGuNlc5PCEQvF2= M{HZSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
GI-1 M2DzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjMVXVKSzVyPUKxMlE4KM7:TR?= M3vJflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MC116 M1jSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;lTWM2OD1{MT6wO|I{KM7:TR?= NHjYTGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
A375 MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\oeJZKSzVyPUKxMlA2PjdizszN MnzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
IST-SL1 NEThUmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HudWlEPTB;MkCuO|g4QSEQvF2= M{Tne|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
TE-5 M{\tPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTZboxKSzVyPUKwMlc1QDJizszN M{HHUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
SiHa NFnTfpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny5TWM2OD1{MD6zO|EzKM7:TR?= NX7qPGI3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
LB2518-MEL NVHWWVVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHXWWtQUUN3ME2yNE4{PzN7IN88US=> MkO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
BB49-HNC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF7LkmyJO69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HGC-27 NYLldZBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITDWZpKSzVyPUKwMlE{QTRizszN M2LrXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
Becker MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jabmlEPTB;MUmuPFU1PyEQvF2= NXu1clhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
TYK-nu NIjWdlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHmS45GUUN3ME2xPU45Ozd6IN88US=> M1GwS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H650 M3XSTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTF7Lke1NFgh|ryP NEPOTGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
WM-115 NUHQdWdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e5e2lEPTB;MUmuOlc4PCEQvF2= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
HuH-7 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFuzU|RKSzVyPUG5Mlc1OjFizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-N87 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;CTWM2OD1zOT61PVkzKM7:TR?= NFTHTng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H1048 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL3TWM2OD1zOT6yN|I3KM7:TR?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H446 Mki2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TVWWlEPTB;MUmuN|U5QSEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1437 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLsTWM2OD1zOT6wOFY4KM7:TR?= NIK3bIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
D-263MG MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIni[WFKSzVyPUG5MlAyPzJizszN NWfDfmozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
MFH-ino NUXPSGpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqxNGZKSzVyPUG4Mlk3PjlizszN MnjuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
U-266 NFL3foFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L4dGlEPTB;MUiuPFY1QSEQvF2= NXuzdpdURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
OVCAR-8 MlHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\UTWM2OD1zOD65Nlc3KM7:TR?= Mn33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
KNS-42 MoPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXpbGJYUUN3ME2xPE45ODF3IN88US=> NEHOU289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
U251 NYHoVZZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDse2VlUUN3ME2xPE44OzR5IN88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MFE-280 NEXa[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXaU2tKSzVyPUG4MlczQTNizszN MnWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H1563 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSyVppKSzVyPUG4MlcyOjRizszN MojQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
MDA-MB-361 NVThdZFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Ti[2lEPTB;MUiuOVU5QCEQvF2= NV3DNnZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HLE M3npVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjMTWM2OD1zOD6zNVQ5KM7:TR?= M1[3flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
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KM-H2 MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF5Lkm0NVEh|ryP MkDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
D-502MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrnVnBKSzVyPUG3Mlk5ODhizszN NHTmTlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
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SF268 NYfBdItsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnUSXFPUUN3ME2xO{43QTZ7IN88US=> NUDKeJRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
Calu-6 NXrN[WpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\q[XRKSzVyPUG3MlY4QDJizszN NXnm[HRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SW1783 NHrvUZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13oO2lEPTB;MUeuOlQyPSEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H747 NGnvZ25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ftfGlEPTB;MUeuOVI6PyEQvF2= NWnRUIsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
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