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。

规格

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库存

购买数量

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501篇：

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Cancer Sci, 2012, 103(1):7-16

PubMed: 21951556 ( click the link to review the publication )

Biochem Pharmacol, 2012, 84(4):425-31

PubMed: 22634404 ( click the link to review the publication )

Int J Mol Sci, 2012, 13(9):12000-16

PubMed: 23109896 ( click the link to review the publication )

Int J Oncol, 2012, 41(3):869-75

PubMed: 22752005 ( click the link to review the publication )

Cancer Res Treat, 2012, 44(3):202-9

PubMed: 23091447 ( click the link to review the publication )

PLoS One, 2012, 7(9):e42441

PubMed: 22957020 ( click the link to review the publication )

PLoS One, 2012, 7(12):e51549

PubMed: 23272116 ( click the link to review the publication )

Oncotarget, 2012, 2(12):1134-44

PubMed: 22193779 ( click the link to review the publication )

Mol Syst Biol, 2011, 7:486

PubMed: 21525872 ( click the link to review the publication )

Oncogene, 2011, 30(6):737-50

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Antivir Res, 2011, 89(1):64-70

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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	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-
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