Gefitinib (ZD1839)

目录号:S1025

Gefitinib (ZD1839) Chemical Structure

Molecular Weight(MW): 446.90

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。

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RMB 2205.98 现货
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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 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。
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 NXLxWI9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK4TWM2OD1yLkC1OEDPxE1? M2fk[lE3PTF4NEez
NIH3T3 MWHGeY5kfGmxbjDBd5NigQ>? Moe4NE4zKM7:TR?= NXizZm13OiCq MofESG1UVw>? NVq0Uot4UW6qaXLpeIlwdiCxZjDFS2Yhe3SrbYXsZZRm\CCqdX3hckBmemKEMTDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxOFQh|ryP M1[yXVE3PDhyMki0
COS7 MkLoSpVv[3Srb36gRZN{[Xl? MXS5OkDPxE1? NGrhTmxKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? NGfLVWIyPzF5OEeyNi=>
A549 M1LFW2N6fG:2b4jpZ{BCe3OjeR?= Mly2PVYhcA>? NFL3cnBFVVOR M3Lid2lEPTB;MUOuOVkh|ryP M4K2[|E5OzF|OEC3
K562 NHPSUmtEgXSxdH;4bYMhSXO|YYm= MXG5OkBp MUnEUXNQ MULJR|UxRTlwM{[g{txO MkHpNVg{OTN6MEe=
MDA-MB-231 MYLDfZRwfG:6aXOgRZN{[Xl? MUG5OkBp MlfBSG1UVw>? MlHZTWM2OD1|Nj62NUDPxE1? NG\STGUyQDNzM{iwOy=>
MOLT4 NUi3cZF[S3m2b4TvfIlkKEG|c3H5 MoDYPVYhcA>? NEfqdHpFVVOR MUXJR|UxRTF3LkCyJO69VQ>? NIL4XmIyQDNzM{iwOy=>
MCF7 MWrDfZRwfG:6aXOgRZN{[Xl? NEL1Tmk2OCEQvF2= NVzqc4pGPzJiaB?= MmHFTWM2OD1zMj6wOUDPxE1? NXfKUmhXOTh5N{G4NVk>
BT474 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;xZ|Y4OiCq NIqyVmRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXSRoIzKHerdHigSWM2OCCxZjCwMlMh|ryP MWexPVAzQDR{NB?=
HN5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnvO|IhcA>? NYqwUFhjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUlUh[2WubIOgc5ZmemW6cILld5NqdmdiRVfGVkB4cXSqIFXDOVAhd2ZiMD6wNUDPxE1? NVnMcFR6OTlyMki0NlQ>
BA/F3 NYTLR2RNS3m2b4TvfIlkKEG|c3H5 MUO3NkBp NEn6cVlEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO MkjZNVkzOzl{Mkm=
NIH3T3 NFT2PI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHNUYMxPzJiaB?= MkLRS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgUmlJNzOWMzDj[YxteyCneIDy[ZN{cW6pIHXyRlIh\2WwZTD3bZRpKEmFNUCgc4YhOC53NDFOwG0> NHrhXXkyQTZ4NUO3Oy=>
MCF7 MX MkjPSpVv[3Srb36gRZN{[Xl? NFTyUFk{OCCvaX6= MnXNTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMT6xJO69VQ>? M3XKWlE6QTN{OU[w
A431 NULFSoZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xNEDPxE1? Mlj2O|IhcA>? NXTqWmR3T0l3ME2wMlUyPCEQvF2= NUfjXpFMOTl7Nkm0OlU>
A431 NHnkfmJMcW6jc3WgRZN{[Xl? MYmwMlEh|ryP MYKxJIg> NVHmWHpFUW6qaXLpeIlwdiCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? M{PMO|E6QTZ7NE[1
A431 MYjLbY5ie2ViQYPzZZk> NI\GOpEyODBizszN NYHZb2NwOTBibXnu M2SwVHBzd2yxbnfl[EBqdmirYnn0c5J6KGGldHn2bZR6KG:oIFXHSk1qdmS3Y3XkJGVITlJicHjvd5Bpd3K7bHH0bY9v MU[xPVk3QTR4NR?=
Sf9 NWXqflJUU2mwYYPlJGF{e2G7 MkTBNVAhdWmw MmS5SG1UVw>? NHfyN4tKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN MWKyNFA2PjR{NR?=
NCI-H1975 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT1[HI2KM7:TR?= NYezdpFCPzJiaB?= NFnEUIVKSzVyPUiuNlYh|ryP NVLLXFBOOjBzNUG2O|A>
NCI-H1975 MmLyT4lv[XOnIFHzd4F6 MXuxNEDPxE1? NUXhXnpzUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25? NHLDe3EzODF3MU[3NC=>
NCI-H1975 MU\GeY5kfGmxbjDBd5NigQ>? NUi1O2pjOTBizszN MofyTY5pcWKrdHnvckBw\iCHUlLCNkBifXSxcHjvd5Bpd3K7bHH0bY9v MWCyNFE2OTZ5MB?=
NCI-H1975 Mlr4SpVv[3Srb36gRZN{[Xl? NWfC[HpjPSEQvF2= NFLRfpE1QCCq M1TjNGlv\HWldHnvckBw\iCjcH;weI9{cXNiYYPz[ZN{\WRiYYOgZYN1cX[jdHnvckBw\iClYYPwZZNmNTN? NYf5WZp2OjBzNUG2O|A>
A375 NIrCb45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPSOFghcA>? MkDITWM2OD1{MD61OUDPxE1? NF\xU5QzODNyNEWzOy=>
SMMC7721 MlSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLkOFghcA>? NIHQc2tKSzVyPUOzMlEzKM7:TR?= NWTTWppLOjB|MES1N|c>
DU145 NUnRTZd7S3m2b4TvfIlkKEG|c3H5 MoHyOUBl MVPEUXNQ NWe2TGhMUUN3ME20Nk4yPyEQvF2= Mn23NlA1PjZ3NUW=
MIAPaCa2 M2fEe2N6fG:2b4jpZ{BCe3OjeR?= MYe1JIQ> NFrFR5VFVVOR M1fDVmlEPTB;NUCuOlIh|ryP M3PhTlIxPDZ4NUW1
PANC1 MnXUR5l1d3SxeHnjJGF{e2G7 M1PsdlUh\A>? NY\K[2Z6TE2VTx?= MUTJR|UxRTRyLkSyJO69VQ>? NVv6T5hoOjB2Nk[1OVU>
PC9 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFS2ZTNWSnZnnjbYVvfCCqdX3hckBRSzliY3XscJMhf2m2aDDFR|UxKG:oIECuNFE4KM7:TR?= NW\FO|BEOjF{MEi4NFI>
PC9 Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDndo94fGhvcnXzbZN1[W62IHj1cYFvKFCFOTDj[YxteyCneIDy[ZN{cW6pIFXHSnIhTTd2Nm;BO|UxN1R5OUDNJI12fGGwdDD3bZRpKEWFNUCgc4YhPyEQvF2= M{\ybFIyOjB6OECy
PC3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\lNVAh|ryP NH\wPJY4OiCq MUHEUXNQ NV3NW4VNUUN3ME23MlQh|ryP MWKyNVM2OzV2Nh?=
MDA-MB-468 NUHJUGYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUSxdGhHOTByIN88US=> M4O0UFQ5KGh? NVLDNZh5TE2VTx?= MmXPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdIm= NVnUXXBiOjF2Mkm2N|I>
Plasmodium falciparum MWjxTHRUKHC{b3\pcIlv\yCob4KgbY5pcWKrdH;yd{Bw\iCSbHHzcY9lcXWvIH\hcINqeGG{dX2gdJJwdGmoZYLheIlwdg>? M{PaVFIyQDF5MES1
NCI-H1993 NFzJboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pa[|czKGh? MULEUXNQ M{iw[WlEPTB;MD6xJO69VQ>? M3ruTFIyQTF4NEOz
NCI-H292 Ml7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[3blczKGh? NWXXbIZoTE2VTx?= M3nwS2lEPTB;MD6wNkDPxE1? MomwNlE6OTZ2M{O=
A431 NFjm[YhMcW6jc3WgRZN{[Xl? M2W5SlIhcA>? NVzTbYl2TE2VTx?= NUjYPIxQUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCHR1[td5RqdXWuYYTl[EBpfW2jbjDBOFMyKHerdHigTWM2OCCxZjCwMlAxOSEQvF2= NHfYNo8zOjFyMUGzNi=>
MCF7 M2jkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWyPFZ5OTBywrFOwIcwdUx? MWS0PEBp MVfEUXNQ MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDn[Y5mKHerdHigTWM2OCCxZjCxNk4xPSEQvF2= NEC0cpUzOjFzOUGzNC=>
BT474 MVXDfZRwfG:6aXOgRZN{[Xl? MX6xNEDPxE1? M2HQR|Q5KGh? NGXHNXVEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIFLUOFc1KGOnbHzz MY[yNlE{QDNyOB?=
MCF7 M{SxdWN6fG:2b4jpZ{BCe3OjeR?= M2nOWlExKM7:TR?= Mmf1OFghcA>? M37XXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHOncoXtMZN1[XK4ZXSgbJVu[W5iTVPGO{Bk\WyuczDveoVzNWW6cILld5NqdmdiRYLiRlIh[2WubIO= NWDxemt5OjJzM{izNFg>
HCC827 NV63NmlPU2mwYYPlJGF{e2G7 Mn:wNE4yOjVizszN M3vmXlI1KGh? M3qzN2ROW09? MXzJcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQhYTFyNkigZZV1d3Cqb4PwbI9zgWyjdHnvci=> MoT2NlI{Ozl|NEK=
HCC827 M3\mSGtqdmG|ZTDBd5NigQ>? NInUTJoxNjF{NTFOwG0> M{fEblI1KGh? NUCyd5hDTE2VTx?= MYDJcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQudWWmaXH0[YQhTXKtIIDoc5NxcG:{eXzheIlwdg>? NWLVT|F7OjJ|M{mzOFI>
HCC827 MXjLbY5ie2ViQYPzZZk> NVzOe3ZWOC5zMkWg{txO MoTYNlQhcA>? NIXzZWdFVVOR NH:xemZKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?= NV;BUXQ{OjJ|M{mzOFI>
A431 NX3lRVF6U2mwYYPlJGF{e2G7 NFfZ[IUyODBizszN M4mxU|MxKG2rbh?= MkXHTY5pcWKrdHnvckBw\iCHR1\SJIRmemm4ZXSg[pJwdSCqdX3hckBCPDNzIHPlcIwhdWWvYoLhcoUh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBxd2y7LVfseU1VgXJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxMlA5KM7:TR?= MV[yNlY6QDd6Mh?=
H460 NY\z[JBCS3m2b4TvfIlkKEG|c3H5 M3e5UlczKGh? NGPtXnZKSzVyPUWuOVkh|ryP MYGyNlczPzR2OR?=
HT-29 MV;DfZRwfG:6aXOgRZN{[Xl? MmfRO|IhcA>? NVjORnJUUUN3ME2zMlM3KM7:TR?= MkTLNlI4Ojd2NEm=
SGC7901 NELxVmtEgXSxdH;4bYMhSXO|YYm= MX[3NkBp MlXkTWM2OD1zMD6yOkDPxE1? M3vOeVIzPzJ5NES5
A498 MkDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNEm4JINmdGy|IHX4dJJme3OrbnegSWdHWiCjbnSgV3JEKHerdHigTWM2OCCxZjC4MlYh|ryP NG[3ZVczOjhzOEi0PC=>
Calu3 MVLDfZRwfG:6aXOgRZN{[Xl? MVWxNEDPxGdxbVy= NGTwflg4OiCq MYDJR|UxRTFwNjFOwG0> MVqyN|EyPjF4OB?=
FADU Mn75R5l1d3SxeHnjJGF{e2G7 M4DoTFExKM7:Zz;tUC=> MmHVO|IhcA>? MW\JR|UxRTBwMEWg{txO NXfLUYlpOjNzMU[xOlg>
HCC827 NUHPWmViS3m2b4TvfIlkKEG|c3H5 NHnacpgyOCEQvHevcWw> MUC3NkBp MlPQTWM2OD1yLkCwNVUh|ryP NI\6W|gzOzFzNkG2PC=>
PC9 NYe5d|RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxNEDPxGdxbVy= NEfseWo4OiCq MYfJR|UxRTBwMEG0JO69VQ>? M{XKPVI{OTF4MU[4
Sf9 NFvEbFRMcW6jc3WgRZN{[Xl? NWr4XWpOOSCq Mn65SG1UVw>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGdUXC22YXfn[YQhTUeIUjDMPFM1WiCvdYThcpQh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlAyPSEQvF2= MY[yN|YyOTZ7MR?=
16HBE14o- NF:zRmtEgXSxdH;4bYMhSXO|YYm= MnfsNVAh|ryP NEK2ZWE4OiCq NH7LW3RFVVOR MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxOmhDTTF2bz2gZ4VtdHNiaHHyZo9zcW6pIIfpcIQhfHmyZTDFS2ZTKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAyOi55MTFOwG0> NYLhRY9iOjN4Nki0OFE>
NCI-H1975 NEjkR5ZEgXSxdH;4bYMhSXO|YYm= NIHxN4cyOCEQvF2= M1LkZ|czKGh? M4jqVWROW09? NIrOR3REgXSxdH;4bYNqfHliYXfhbY5{fCCpZX\peIlvcWJvcnXzbZN1[W62IHj1cYFvKE6FST3INVk4PSClZXzsd{Bp[XKkb4LpcochTUeIUjDMPFU5Wi:WN{mwUUBld3WkbHWgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJdqfGhiSVO1NEBw\iB4LkmxO{DPxE1? MkXBNlM3Pjh2NEG=
16HBE NFPXOXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPpO|IhcA>? NUfnR|VwTE2VTx?= NG\mT2NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEG2TGJGKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWJRmKge4l1cCCLQ{WwJI9nKDFwNkCxJO69VQ>? M2XHVFI{Pzl{M{G4
16HBE M37uNmZ2dmO2aX;uJGF{e2G7 MWmxNFAh|ryP NH7ZTFUyPTBibXnu NHHlVI1FVVOR NVvkWWw{UW6mdXP0bY9vKG:oIH7peJJq[yCxeHnk[UBxem:mdXP0bY9vKGmwIHj1cYFvKDF4SFLFJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGVITlJ? NVP0SG5HOjN5OUKzNVg>
A549 NXz5cFUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1mxVFczKGh? M{DoWGROW09? MmHmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDD3bYxlKHS7cHWgSWdHWi:tLWLhd{Bl\XCnbnTlcpQhcHWvYX6gRVU1QSClZXzsd{B4cXSqIFnDOVAhd2ZiND62NlYh|ryP MlnhNlM4QTJ|MUi=
SH-SY5Y MmXtR5l1d3SxeHnjJGF{e2G7 NGLhSW44OiCq M3zEemlEPTB;MUiuNlEh|ryP NXHXc4xGOjN6N{G5NFk>
LoVo Mk\0T4lv[XOnIFHzd4F6 MUSyJEBp NYrTbmk5TE2VTx?= M{XvZmlvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwME[yJO69VQ>? Ml[5NlM6OzB7OUS=
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HCC827 Ml3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\CUJp{PzJiaB?= MVnJR|UxRTBwMEGyJO69VQ>? MVSyN|k4OzF4OB?=
A549 MXPLbY5ie2ViQYPzZZk> NHLqWGwyKM7:TR?= M4jW[lEhcA>? NEXYTpRFVVOR NHPofnJKdmirYnn0bY9vKG:oIFXHSnIh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzl7IN88US=> MnPHNlM6QDh|NUS=
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NCI-H358 NWTSTFA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzUTWM2OD13MkeuOlYhdk1? NEL2eHdUSU6JRWK=
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NCI-H82 M4GxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTV2MD61JI5O MVjTRW5ITVJ?
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RS4-11 NYjIdoFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTV4OD61PUBvVQ>? MV3TRW5ITVJ?
CAN Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG1XllbUUN3ME21PFAvPzZibl2= M{LK[3NCVkeHUh?=
Ca9-22 NVGyVWtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLvcY0{UUN3ME21PFgvPjRibl2= NFTxRVdUSU6JRWK=
CAL-39 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\Le4ZKSzVyPUW5Ok4{KG6P NFrpXIpUSU6JRWK=
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NB69 M{HuW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq4OWtKSzVyPU[xOE4{PSCwTR?= M2PwSnNCVkeHUh?=
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MV-4-11 M1mxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz1TWM2OD14MkeuO{BvVQ>? MlXlV2FPT0WU
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ME-180 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTZ|Mj65JI5O MUPTRW5ITVJ?
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COR-L105 MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXPTWM2OD14NkKuOVMhdk1? M2XQT3NCVkeHUh?=
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NCI-H1770 MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDiTWM2OD15MkKuOEBvVQ>? MUjTRW5ITVJ?
HAL-01 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTd|ND63NUBvVQ>? M1TSTXNCVkeHUh?=
COLO-684 M{jKdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHGUWdKSzVyPUe1N{4xOSCwTR?= NYe2[pd{W0GQR1XS
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NCI-H1304 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYOyOZdvUUN3ME2xMlAyPjR|IN88US=> NULnTXNqW0GQR1XS
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C32 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrFNHJKSzVyPUmuOlM{PCEQvF2= M1nrRXNCVkeHUh?=
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NCI-H1581 NFvje3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknyTWM2OD1zNz60OFEyKM7:TR?= NVXmbo9oW0GQR1XS
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SW1783 NET5XGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\4RXhDUUN3ME2xO{43PDF3IN88US=> NHvXRYdUSU6JRWK=
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D-502MG NE\U[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXDTWM2OD1zNz65PFA5KM7:TR?= MV7TRW5ITVJ?
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NCI-H1437 MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3uxOGlEPTB;MUmuNFQ3PyEQvF2= MVzTRW5ITVJ?
NCI-H1048 NXTN[JpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF7LkKzNlYh|ryP M3O4THNCVkeHUh?=
NCI-H446 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPrTWM2OD1zOT6zOVg6KM7:TR?= MnnDV2FPT0WU
NCI-N87 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF7LkW5PVIh|ryP NUjnR|RvW0GQR1XS
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NCI-H650 NU\XSIluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF7Lke1NFgh|ryP MWPTRW5ITVJ?
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H-EMC-SS MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P0c2lEPTB;NEWuO|Y6OyEQvF2= MUXTRW5ITVJ?
NCI-H2052 NUjuXnhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTuXm9KSzVyPUS1MlkxOjdizszN MXXTRW5ITVJ?
SW684 M3XqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR5LkCwPFEh|ryP NY\obYgzW0GQR1XS
HCC1569 MkPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV72XXoyUUN3ME20O{4yPjV6IN88US=> MYfTRW5ITVJ?
KGN NGq0VWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTRTWM2OD12Nz6zN|EyKM7:TR?= MXPTRW5ITVJ?
LCLC-103H MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\PN2lEPTB;NEeuOFQxPCEQvF2= M4j5fXNCVkeHUh?=
SW780 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTR5Lk[zOVEh|ryP M2PHPXNCVkeHUh?=
NCI-H1703 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiwdJNDUUN3ME20PE4{OzV{IN88US=> NHvYWGtUSU6JRWK=
HCC1395 M2LnUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR6Lke0N|Ih|ryP NGLZTpdUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT; 

PubMed: 22586683     


Effect of overexpressing CRKL on phosphorylation levels of EGFR, ERK, AKT and SRC in response to gefitinib. HCC827 cells expressing a control vector or CRKL were exposed to gefitinib at indicated concentrations for 6 h and cell lysates were collected for immunoblotting with indicated specific antibodies.

Cyclin D1/ p16 / p27 / pRb; 

PubMed: 18559346     


levels of phosphorylated and total EGFR, IGF-1R, Akt, ERK1/2, and Rb and levels of cyclin D1, p27, p16, and actin following 6- or 16-h treatment of A431 cells with combinations of 1 or 3 μm gefitinib and 3 μm NVP-ADW742. Data are representative of two independent experiments.

uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP; 

PubMed: 23102728     


Apoptosis resulting from combined treatment with gefitinib and an MEK inhibitor. (A) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/wt and PC‐9/gef B4 cells. (B) Apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/wt and PC‐9/gef B4 cells. (C) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/gefE3 and PC‐9/gefE7 cells. (D) apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/gefE3 and PC‐9/gefE7 cells.

PPAR-γ; 

PubMed: 23409107     


Fold increase relative to control was determined after normalization with β-actin as external loading control. 

22586683 18559346 23102728 23409107
Immunofluorescence
EGFR / LC3; 

PubMed: 31196210     


H157 and H1299 cells were treated with gefitinib, or curcumin alone, or gefitinib plus curcumin at indicated concentration for 48 h and then were fixed with methanol, immunostained with anti-EGFR (green), anti-LC3 (red), and DAPI (blue), and analyzed by confocal microscopy to determine the intracellular locations of EGFR and LC3.

PPAR-γ; 

PubMed: 23409107     


Upregulation and nuclear accumulation of PPARγ following treatment with gefitinib (24 hs).

p-EGFR / β-catenin; 

PubMed: 23461856     


In untreated CNE2 cells, β-catenin was located in cytoplasmic membranes and cytoplasm. Treatment with EGF (50 ng/mL) resulted in increased β-catenin nuclear staining, which was reversed by either gefitinib (1 μM) or LY294002 (15 μM). 

31196210 23409107 23461856
Growth inhibition assay
GI50; 

PubMed: 23409107     


Dose-response of bladder cancer cell lines to EGFR inhibitor (gefitinib). The GI50 value was defined as the mean concentration of drug that generates 50% of growth inhibition as compared to controls.

23409107
体内研究 Gefitinib 作用于无胸腺裸鼠,抑制SKOV3 或MDA-MB-231 肿瘤生长。Gefitinib高效作用于两种类型肿瘤。处理14天后,MDA-MB-231肿瘤和SKOV3肿瘤生长抑制分别为71%和32%。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
+ 展开
  • Cell lines: NR6, NR6M 和 NR6W 细胞
  • Concentrations: 0 μM -2 μM
  • Incubation Time: 72 小时
  • Method: 呈指数生长的细胞,包括 NR6, NR6M, NR6M和NR6W细胞按6倍接种在96孔板上,每孔为2000个细胞, 粘附,随后在PBS 中清洗,然后在含0.5% FCS的培养基上温育过夜。使用不同浓度(0-2 μM) Gefitinib或溶质对照DMSO 和EGF 处理细胞。诱导NR6wtEGFR和NR6W 细胞增殖的EGF最佳浓度已经测定,因此NR6wtEGFR和 NR6W 细胞中分别加入10 nM和 0.1 nM EGF。NR6 和NR6M细胞中不加入EGF。72 小时后,通过MTT 增殖检测测量细胞数。
    (Only for Reference)
动物实验:[3]
+ 展开
  • Animal Models: 携带 SKOV3或MDA-MB-231肿瘤的无胸腺裸鼠
  • Formulation: 0.2% DMSO
  • Dosages: 75 mg/kg
  • Administration: 饲喂处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 89 mg/mL (199.14 mM)
Ethanol 4 mg/mL (8.95 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% CMC Na
30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 446.90
化学式

C22H24ClFN4O3

CAS号 184475-35-2
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03866499 Not yet recruiting NSCLC Beta Pharma Inc. May 2019 Phase 3
NCT03866499 Not yet recruiting NSCLC Beta Pharma Inc. May 2019 Phase 3
NCT03787992 Not yet recruiting Locally Advanced or Metastatic EGFR Sensitising Mutation Positive Non-small Cell Lung Cancer Allist Pharmaceuticals Inc. April 1 2019 Phase 3
NCT03787992 Not yet recruiting Locally Advanced or Metastatic EGFR Sensitising Mutation Positive Non-small Cell Lung Cancer Allist Pharmaceuticals Inc. April 1 2019 Phase 3
NCT03766490 Not yet recruiting Non-Small-Cell Lung The First Affiliated Hospital of Soochow University|The First People''s Hospital of Changzhou|Second Affiliated Hospital of Soochow University|Nantong University|Affiliated Hospital of Jiangnan University|Jiangyin People''s Hospital|Changzhou No.2 People''s Hospital|Chia Tai Tianqing Pharmaceutical Group Co. Ltd. March 30 2019 Not Applicable
NCT03856697 Not yet recruiting Advanced Non-small Cell Lung Cancer Hangzhou ACEA Pharmaceutical Research Co. Ltd.|Guangdong Provincial People''s Hospital March 2019 Phase 3

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?

  • 回答:

    S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID