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501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 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fJVGlEPTB;MkGuOFYyKM7:TR?= NGC4[ng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HT M3niZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzrfGE1UUN3ME2yNU41OzNzIN88US=> NHj3b4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HUTU-80 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfTTWM2OD1{MT60N|M3KM7:TR?= NYDI[olmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
PA-1 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy5NYZKSzVyPUKxMlI4QDdizszN NXy0WWJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HOP-62 NUPCcFEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi2R2VKSzVyPUKxMlI4QDRizszN MmfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
GI-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojFTWM2OD1{MT6xO{DPxE1? M1jTdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MC116 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjKTWM2OD1{MT6wO|I{KM7:TR?= M3jrbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
A375 MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJzLkC1Olch|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
IST-SL1 M2LXW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDmeINKSzVyPUKwMlc5PzlizszN NI\XV3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
TE-5 NGDRPYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULIO4toUUN3ME2yNE44PDh{IN88US=> MonIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
SiHa NV3n[JFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJyLkO3NVIh|ryP M1nyOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
LB2518-MEL M1SzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJyLkO3N|kh|ryP MnXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
BB49-HNC NGnrOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH0TWM2OD1zOT65NkDPxE1? M4W5UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HGC-27 MmrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e4ZWlEPTB;MkCuNVM6PCEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
Becker MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\jOGlEPTB;MUmuPFU1PyEQvF2= NYnFZW1URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
TYK-nu MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPkTWM2OD1zOT64N|c5KM7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H650 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zw[2lEPTB;MUmuO|UxQCEQvF2= NH25XW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
WM-115 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\NTWM2OD1zOT62O|c1KM7:TR?= M4ixSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HuH-7 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF7Lke0NlEh|ryP NYDsR4dTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-N87 NXrVZnE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLxTWM2OD1zOT61PVkzKM7:TR?= MoW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H1048 M{jDNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XDSWlEPTB;MUmuNlMzPiEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H446 NF[5PVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\rTmNKSzVyPUG5MlM2QDlizszN NU\hd4psRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H1437 M{HLe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF7LkC0Olch|ryP Mlr5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
D-263MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF7LkCxO|Ih|ryP NECzNZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
MFH-ino NVLrcWtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF6Lkm2Olkh|ryP Mlq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
U-266 NI\xV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\4TWM2OD1zOD64OlQ6KM7:TR?= M{G4O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
OVCAR-8 MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnR[lFxUUN3ME2xPE46Ojd4IN88US=> M2TwNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
KNS-42 NFvqZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGwUW16UUN3ME2xPE45ODF3IN88US=> M2nNRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
U251 M1zOT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEizeVlKSzVyPUG4Mlc{PDdizszN MnnkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
MFE-280 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG2WVFSUUN3ME2xPE44Ojl|IN88US=> M2TJdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1563 NUmyfWtRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPOXWtKSzVyPUG4MlcyOjRizszN NV\uPXhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
MDA-MB-361 NILsSnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLtZlV1UUN3ME2xPE42PTh6IN88US=> NYL3NXQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HLE NHzMbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTF6LkOxOFgh|ryP MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
SW982 NIHjZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPSTWM2OD1zOD60NFc2KM7:TR?= NHjGemQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
KM-H2 NWDiPJg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG1TWM2OD1zNz65OFEyKM7:TR?= NVzuWpRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
D-502MG NID0NnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT4TpJoUUN3ME2xO{46QDB6IN88US=> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
ES8 NFy0blhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33uVWlEPTB;MUeuPFU6OyEQvF2= NUXwWHIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SF268 NH3E[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETuOldKSzVyPUG3MlY6PjlizszN M37KUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
Calu-6 MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF60OGVKSzVyPUG3MlY4QDJizszN M4nEdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
SW1783 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj6bHRUUUN3ME2xO{43PDF3IN88US=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H747 NGXhNZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ufGlEPTB;MUeuOVI6PyEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1573 NVm4PXdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLmcmJ5UUN3ME2xO{4zQDJ4IN88US=> Ml3JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
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