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。

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RMB 2205.98 现货
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客户使用Selleck生产的Gefitinib (ZD1839)发表文献443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
KB NVTG[XV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PNZWlEPTB;MD6wOVQh|ryP M1vydlE3PTF4NEez
NIH3T3 MY\GeY5kfGmxbjDBd5NigQ>? NXvxfnJUOC5{IN88US=> NHvo[3IzKGh? NIG3XpdFVVOR MnWzTY5pcWKrdHnvckBw\iCHR1[gd5RqdXWuYYTl[EBpfW2jbjDldoJDOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNESg{txO MlWwNVY1QDB{OES=
COS7 MlPYSpVv[3Srb36gRZN{[Xl? NWfkNJh6QTZizszN NH;xV4FKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? NHqwPHAyPzF5OEeyNi=>
A549 NVTlXIxPS3m2b4TvfIlkKEG|c3H5 NVPV[mFCQTZiaB?= NUm2cWFnTE2VTx?= MWfJR|UxRTF|LkW5JO69VQ>? M3GwT|E5OzF|OEC3
K562 MX\DfZRwfG:6aXOgRZN{[Xl? MV[5OkBp NH3BOoNFVVOR NV3GNZdTUUN3ME25MlM3KM7:TR?= NVLsVFA1OTh|MUO4NFc>
MDA-MB-231 MknRR5l1d3SxeHnjJGF{e2G7 MW[5OkBp NU\yfJN6TE2VTx?= NH7oUXZKSzVyPUO2MlYyKM7:TR?= MYCxPFMyOzhyNx?=
MOLT4 NXPCVWhkS3m2b4TvfIlkKEG|c3H5 M3;XbVk3KGh? NGL1Z4ZFVVOR NGjjRZhKSzVyPUG1MlAzKM7:TR?= NWLzZmNlOTh|MUO4NFc>
MCF7 NVn2VGRNS3m2b4TvfIlkKEG|c3H5 MV[1NEDPxE1? MXu3NkBp NEfofYRKSzVyPUGyMlA2KM7:TR?= M1rTS|E5PzdzOEG5
BT474 M1\zWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XJPFczKGh? NHPvdZBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXSRoIzKHerdHigSWM2OCCxZjCwMlMh|ryP MXyxPVAzQDR{NB?=
HN5 NVPIVo9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3SwXlczKGh? M4DmWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKge4l1cCCHQ{WwJI9nKDBwMEGg{txO MUixPVAzQDR{NB?=
BA/F3 NHXPb2REgXSxdH;4bYMhSXO|YYm= NUew[VJ6PzJiaB?= M3Gx[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBNQDV6UjDteZRidnRid3n0bEBKSzVyIH;mJFAvODFyODFOwG0> MWixPVI{QTJ{OR?=
NIH3T3 NUnDWHZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPjOW04OiCq MnPUS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgUmlJNzOWMzDj[YxteyCneIDy[ZN{cW6pIHXyRlIh\2WwZTD3bZRpKEmFNUCgc4YhOC53NDFOwG0> M2nxVlE6PjZ3M{e3
MCF7 MX NFnzeFRHfW6ldHnvckBCe3OjeR?= MYmzNEBucW5? MWnJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzLkGg{txO NEf2SVMyQTl|Mkm2NC=>
A431 NVPJUVVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zUVFExKM7:TR?= NE\BfZQ4OiCq MWjHTVUxRTBwNUG0JO69VQ>? M2rVc|E6QTZ7NE[1
A431 M1y0fWtqdmG|ZTDBd5NigQ>? M2flUlAvOSEQvF2= M4npXVEhcA>? NXnRdpFJUW6qaXLpeIlwdiCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? MYexPVk3QTR4NR?=
A431 MoDoT4lv[XOnIFHzd4F6 NXSyOlkyOTByIN88US=> MnK4NVAhdWmw MVXQdo9td26pZXSgbY5pcWKrdH;yfUBi[3Srdnn0fUBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvci=> NHfi[nQyQTl4OUS2OS=>
Sf9 M1[4emtqdmG|ZTDBd5NigQ>? MmK4NVAhdWmw MnnhSG1UVw>? NGPVS3lKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN M1j3bVIxODV4NEK1
NCI-H1975 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq1JO69VQ>? M3\UOVczKGh? M4DyfWlEPTB;OD6yOkDPxE1? M4W2RVIxOTVzNkew
NCI-H1975 NEX3OYNMcW6jc3WgRZN{[Xl? MX[xNEDPxE1? NW\0WHdEUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25? M3XrdFIxOTVzNkew
NCI-H1975 M4XhZmZ2dmO2aX;uJGF{e2G7 NFjTd5gyOCEQvF2= MXLJcohq[mm2aX;uJI9nKEWUQlKyJIF2fG:yaH;zdIhwenmuYYTpc44> NGO0UG4zODF3MU[3NC=>
NCI-H1975 M3zqS2Z2dmO2aX;uJGF{e2G7 NHL1PHU2KM7:TR?= MYW0PEBp NH\xO29KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiY3HzdIF{\S1| Mk\mNlAyPTF4N{C=
A375 Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TWT|Q5KGh? MXvJR|UxRTJyLkW1JO69VQ>? MnXzNlA{ODR3M{e=
SMMC7721 MnyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnyOFghcA>? NXLYbXI6UUN3ME2zN{4yOiEQvF2= MVGyNFMxPDV|Nx?=
DU145 M1mySmN6fG:2b4jpZ{BCe3OjeR?= NFnnZno2KGR? M{DkeGROW09? MYnJR|UxRTR{LkG3JO69VQ>? M{i5UFIxPDZ4NUW1
MIAPaCa2 MmXmR5l1d3SxeHnjJGF{e2G7 MU[1JIQ> MXLEUXNQ MV3JR|UxRTVyLk[yJO69VQ>? M370T|IxPDZ4NUW1
PANC1 M4C1UGN6fG:2b4jpZ{BCe3OjeR?= MUm1JIQ> Mk\zSG1UVw>? NWPDRnl6UUN3ME20NE41OiEQvF2= M1;IcVIxPDZ4NUW1
PC9 M4fUbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zv[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSWdHWi2mZX\pZ4lmdnRiaIXtZY4hWEN7IHPlcIx{KHerdHigSWM2OCCxZjCwMlAyPyEQvF2= M2HyPVIyOjB6OECy
PC9 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXKbXlWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEB4cXSqIFXDOVAhd2ZiNzFOwG0> Mo[5NlEzODh6MEK=
PC3 NWi2b4JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;zNVAh|ryP MUG3NkBp M2T1WGROW09? NGT0PZRKSzVyPUeuOEDPxE1? NVXQboZLOjF|NUO1OFY>
MDA-MB-468 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[zS|ExOCEQvF2= M132SFQ5KGh? NYnaPWNDTE2VTx?= M1zUb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5 M3zIS|IyPDJ7NkOy
Plasmodium falciparum MYHxTHRUKHC{b3\pcIlv\yCob4KgbY5pcWKrdH;yd{Bw\iCSbHHzcY9lcXWvIH\hcINqeGG{dX2gdJJwdGmoZYLheIlwdg>? NIPJO3czOThzN{C0OS=>
NCI-H1993 NWnkdI9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vGblczKGh? NFzvZ2ZFVVOR MX7JR|UxRTBwMTFOwG0> M{HUd|IyQTF4NEOz
NCI-H292 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T2c|czKGh? M4HWUWROW09? MlXLTWM2OD1yLkCyJO69VQ>? M3TwXVIyQTF4NEOz
A431 NWL5cFR3U2mwYYPlJGF{e2G7 NWfmXWRkOiCq Mm\kSG1UVw>? Mn\MTY5pcWKrdHnvckBw\iCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBGT0Zvc4TpcZVt[XSnZDDoeY1idiCDNEOxJJdqfGhiSVO1NEBw\iByLkCwNUDPxE1? NYXISm86OjJzMEGxN|I>
MCF7 NWD6THVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfQUIlwOTBywrFOwIcwdUx? NXHzSmxZPDhiaB?= Ml3lSG1UVw>? NWDJOlFlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXHSnIh\2WwZTD3bZRpKEmFNUCgc4YhOTJwMEWg{txO MUGyNlEyQTF|MB?=
BT474 NXvs[2tiS3m2b4TvfIlkKEG|c3H5 M3TyO|ExKM7:TR?= NFHOeXY1QCCq NEjxOlVEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIFLUOFc1KGOnbHzz NF\FTnczOjF|OEOwPC=>
MCF7 MVPDfZRwfG:6aXOgRZN{[Xl? NEKwbmwyOCEQvF2= M3fERlQ5KGh? M2jyfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHOncoXtMZN1[XK4ZXSgbJVu[W5iTVPGO{Bk\WyuczDveoVzNWW6cILld5NqdmdiRYLiRlIh[2WubIO= MkjvNlIyOzh|MEi=
HCC827 MV3LbY5ie2ViQYPzZZk> MV2wMlEzPSEQvF2= MXqyOEBp MUnEUXNQ NH7ZdJJKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRiWUGwOlgh[XW2b4Doc5NxcG:{eXzheIlwdg>? M2DJdlIzOzN7M{Sy
HCC827 MYDLbY5ie2ViQYPzZZk> NXrjfnRzOC5zMkWg{txO M{LTclI1KGh? NH[4SWtFVVOR NXvZO2FCUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36= M4rXelIzOzN7M{Sy
HCC827 MYfLbY5ie2ViQYPzZZk> M4nhXFAvOTJ3IN88US=> NV\I[odqOjRiaB?= MXfEUXNQ NUGyZYJpUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62LX3l[IlifGWmIFHreEBxcG:|cHjvdplt[XSrb36= MkfnNlI{Ozl|NEK=
A431 M{TVbWtqdmG|ZTDBd5NigQ>? NXfNW|hWOTByIN88US=> NVnNcJdDOzBibXnu NH\mbJJKdmirYnn0bY9vKG:oIFXHSnIh\GW{aY\l[EBnem:vIHj1cYFvKEF2M{GgZ4VtdCCvZX3idoFv\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHCxbImtS4x2NVS7cjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEvODhizszN Mk\6NlI3QTh5OEK=
H460 MXnDfZRwfG:6aXOgRZN{[Xl? NEXRN3o4OiCq MYTJR|UxRTVwNUmg{txO MVKyNlczPzR2OR?=
HT-29 MVPDfZRwfG:6aXOgRZN{[Xl? MV[3NkBp MlryTWM2OD1|LkO2JO69VQ>? M2nBVVIzPzJ5NES5
SGC7901 NYrRTlF[S3m2b4TvfIlkKEG|c3H5 MUW3NkBp MmH1TWM2OD1zMD6yOkDPxE1? NHfuXlkzOjd{N{S0PS=>
A498 NUTqd4tNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKGGwZDDTVmMhf2m2aDDJR|UxKG:oIEiuOkDPxE1? NGSyVY0zOjhzOEi0PC=>
Calu3 NIm3SlNEgXSxdH;4bYMhSXO|YYm= M2fkblExKM7:Zz;tUC=> MXK3NkBp NGK0NYdKSzVyPUGuOkDPxE1? NXnqbXY3OjNzMU[xOlg>
FADU M1PCT2N6fG:2b4jpZ{BCe3OjeR?= MYexNEDPxGdxbVy= NVLKdplbPzJiaB?= M1jnWmlEPTB;MD6wOUDPxE1? MoPkNlMyOTZzNki=
HCC827 Mk\iR5l1d3SxeHnjJGF{e2G7 NEHGOW0yOCEQvHevcWw> Mn64O|IhcA>? MWnJR|UxRTBwMECxOUDPxE1? NHXo[JQzOzFzNkG2PC=>
PC9 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXqbVNDOTBizsznM41N M3vMOFczKGh? MXTJR|UxRTBwMEG0JO69VQ>? MU[yN|EyPjF4OB?=
Sf9 NFr4TppMcW6jc3WgRZN{[Xl? NFLoZVgyKGh? M1zyS2ROW09? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGdUXC22YXfn[YQhTUeIUjDMPFM1WiCvdYThcpQh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlAyPSEQvF2= MkTENlM3OTF4OUG=
16HBE14o- MVPDfZRwfG:6aXOgRZN{[Xl? NW\XT2M{OTBizszN NFu5RpM4OiCq M3ThOGROW09? MkTqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNVZJSkVzNH:tJINmdGy|IHjhdoJwemmwZzD3bYxlKHS7cHWgSWdHWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOTJwN{Gg{txO M17UUlI{PjZ6NESx
NCI-H1975 NVvZTXMyS3m2b4TvfIlkKEG|c3H5 NE[2XnQyOCEQvF2= Mo\EO|IhcA>? NUjTdZI6TE2VTx?= NHTRPVlEgXSxdH;4bYNqfHliYXfhbY5{fCCpZX\peIlvcWJvcnXzbZN1[W62IHj1cYFvKE6FST3INVk4PSClZXzsd{Bp[XKkb4LpcochTUeIUjDMPFU5Wi:WN{mwUUBld3WkbHWgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJdqfGhiSVO1NEBw\iB4LkmxO{DPxE1? M3;YelI{PjZ6NESx
16HBE M4\5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fJRVczKGh? NYeyfox4TE2VTx?= NGjGWYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEG2TGJGKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWJRmKge4l1cCCLQ{WwJI9nKDFwNkCxJO69VQ>? NFnPfZgzOzd7MkOxPC=>
16HBE NYfNdml{TnWwY4Tpc44hSXO|YYm= NInTZWoyODBizszN Ml\ONVUxKG2rbh?= NFzaOZJFVVOR NYqwO4VEUW6mdXP0bY9vKG:oIH7peJJq[yCxeHnk[UBxem:mdXP0bY9vKGmwIHj1cYFvKDF4SFLFJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGVITlJ? NVTlTVVOOjN5OUKzNVg>
A549 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS3NkBp MnHTSG1UVw>? M{PLOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGVITlJxaz3SZZMh\GWyZX7k[Y51KGi3bXHuJGE2PDliY3XscJMhf2m2aDDJR|UxKG:oIESuOlI3KM7:TR?= M2H1VlI{Pzl{M{G4
SH-SY5Y NUPlV2NwS3m2b4TvfIlkKEG|c3H5 MoPJO|IhcA>? MljBTWM2OD1zOD6yNUDPxE1? NGjaeJIzOzh5MUmwPS=>
LoVo NV24PGFHU2mwYYPlJGF{e2G7 M17FUFIhKGh? MUTEUXNQ NXLuPWhnUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wOlIh|ryP NGe5WZgzOzl|MEm5OC=>
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HCC827 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvhO|IhcA>? M{fnNWlEPTB;MD6wNVIh|ryP M4PsPFI{QTd|MU[4
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