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

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。

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10mM (1mL in DMSO)	RMB 1574.78	现货
100mg	RMB 1227.69	现货
250mg	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：

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J Cell Sci, 2014, 127(Pt 16):3555-67

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Int J Biol Sci, 2014,

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Colloids and Surfaces B: Biointerfaces, 2014, 123:61-7

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Drug Metab Dispos, 2014, 42(3):318-22

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Cancer Chemoth Pharm, 2014, 74(3):511-20

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Exp Mol Pathol, 2014, 97(1):154-165

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JBUON , 2014, 19(2): 466-473

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Ann Oncol, 2013, 24(2):362-9

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Neuro Oncol, 2013, 15(11):1469-78

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J Cell Biol, 2013, 201(2):279-92

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Sci Signal, 2013, 6(279):ra45

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Mol Oncol, 2013, 7(1):121-9

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Carcinogenesis, 2013, 34(9):1994-9

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产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述

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	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-
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