Gefitinib (ZD1839)

For research use only. Not for use in humans.

製品コードS1025

Gefitinib (ZD1839)化学構造

分子量(MW):446.90

Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 33700 あり
JPY 26400 あり
JPY 46800 あり
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バルク問合せ

文献中Selleckの製品使用例(287)

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.
特性 A potent EGFR tyrosine kinase inhibitor.
ターゲット
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
体外試験

Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. [1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. [2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfDPWxPUUN3ME2wMlA2PCEQvF2= NHjxNYsyPjVzNkS3Ny=>
NIH3T3 MYfGeY5kfGmxbjDBd5NigQ>? M4XSclAvOiEQvF2= MXuyJIg> NVS3PXVjTE2VTx?= MUfJcohq[mm2aX;uJI9nKEWJRjDzeIlufWyjdHXkJIh2dWGwIHXyZmIyKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODF2NDFOwG0> M{njVVE3PDhyMki0
COS7 MYnGeY5kfGmxbjDBd5NigQ>? M2LDRVk3KM7:TR?= MWXJcohq[mm2aX;uJI9nKGi3bXHuJGpCUzJiVk[xO2YhdXW2YX70JIV5eHKnc4Pl[C=> MU[xO|E4QDd{Mh?=
A549 NW\NZpdSS3m2b4TvfIlkKEG|c3H5 MlXXPVYhcA>? MkmxSG1UVw>? M2DpW2lEPTB;MUOuOVkh|ryP M{XBblE5OzF|OEC3
K562 MX7DfZRwfG:6aXOgRZN{[Xl? NVnPW|hEQTZiaB?= NEDhfGZFVVOR NWT2NpdtUUN3ME25MlM3KM7:TR?= MWCxPFMyOzhyNx?=
MDA-MB-231 MoLoR5l1d3SxeHnjJGF{e2G7 NXnLNnlVQTZiaB?= MYLEUXNQ NVrJN4FvUUN3ME2zOk43OSEQvF2= M4DvZlE5OzF|OEC3
MOLT4 MWDDfZRwfG:6aXOgRZN{[Xl? NYH4coZJQTZiaB?= NVPUOIxNTE2VTx?= NWTaZXVuUUN3ME2xOU4xOiEQvF2= NH7qTIEyQDNzM{iwOy=>
MCF7 NHjETVFEgXSxdH;4bYMhSXO|YYm= MXq1NEDPxE1? M{H5[FczKGh? M37ERmlEPTB;MUKuNFUh|ryP MV2xPFc4OThzOR?=
BT474 NX61SVJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTpO|IhcA>? NUH0foh2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFVmJjOiC5aYToJGVEPTBib3[gNE4{KM7:TR?= M3vJRVE6ODJ6NEK0
HN5 NV\qSmI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHiyR5U4OiCq MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIIfpeIghTUN3MDDv[kAxNjBzIN88US=> MkjYNVkxOjh2MkS=
BA/F3 MojKR5l1d3SxeHnjJGF{e2G7 M4jtd|czKGh? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJibYX0ZY51KHerdHigTWM2OCCxZjCwMlAyODhizszN MVixPVI{QTJ{OR?=
NIH3T3 NVHlboZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\NNFhIPzJiaB?= M1i0bWdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUC9|VEOgZ4VtdHNiZYjwdoV{e2mwZzDldmIzKGenbnWge4l1cCCLQ{WwJI9nKDBwNUSg{txO M{LNfFE6PjZ3M{e3
MCF7 MX M3PWdWZ2dmO2aX;uJGF{e2G7 NInTZY8{OCCvaX6= NEToS2JKdmirYnn0bY9vKG:oIFLDVnAh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxMlEh|ryP NVTmSFI4OTl7M{K5OlA>
A431 NVnmSVdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInETHAyOCEQvF2= NYPaPYs{PzJiaB?= NUn4R4FYT0l3ME2wMlUyPCEQvF2= NEG4dlcyQTl4OUS2OS=>
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A431 NIHZblRMcW6jc3WgRZN{[Xl? NFXMR5MyODBizszN MYKxNEBucW5? NIDScGhRem:ub37n[YQhcW6qaXLpeI9zgSCjY4Tpeol1gSCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? MX2xPVk3QTR4NR?=
Sf9 M3TM[GtqdmG|ZTDBd5NigQ>? MmH2NVAhdWmw MnezSG1UVw>? Mli0TY5pcWKrdHnvckBw\iCHR1\SJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJJm[2WydH;yJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFM{KM7:TR?= NWLUZ|RROjByNU[0NlU>
NCI-H1975 NYrH[HkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL1V3B{PSEQvF2= NWrNZ4tuPzJiaB?= MVPJR|UxRThwMk[g{txO MUeyNFE2OTZ5MB?=
NCI-H1975 MUTLbY5ie2ViQYPzZZk> MXmxNEDPxE1? M1H3UWlvcGmkaYTpc44hd2ZiRVfGVkBifXSxcHjvd5Bpd3K7bHH0bY9v M3\aflIxOTVzNkew
NCI-H1975 M4\LfWZ2dmO2aX;uJGF{e2G7 NUjzRphrOTBizszN NHrxeHZKdmirYnn0bY9vKG:oIFXSRmIzKGG3dH;wbI9{eGixconsZZRqd25? MWSyNFE2OTZ5MB?=
NCI-H1975 MlzwSpVv[3Srb36gRZN{[Xl? Ml7WOUDPxE1? Mn\0OFghcA>? NEDqe5hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiY3HzdIF{\S1| NVy4PXh3OjBzNUG2O|A>
A375 NH;2XWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrCVlZvPDhiaB?= MV7JR|UxRTJyLkW1JO69VQ>? NHrlT5EzODNyNEWzOy=>
SMMC7721 M3jOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1iwO|Q5KGh? M3\mPGlEPTB;M{OuNVIh|ryP NX\HU3BDOjB|MES1N|c>
DU145 NHu0UmNEgXSxdH;4bYMhSXO|YYm= MWS1JIQ> Mly1SG1UVw>? NVf3VoxnUUN3ME20Nk4yPyEQvF2= NFj1foMzODR4NkW1OS=>
MIAPaCa2 NInQT4lEgXSxdH;4bYMhSXO|YYm= MnXJOUBl NY\xNVJMTE2VTx?= NUS3cFZzUUN3ME21NE43OiEQvF2= NIPWcYkzODR4NkW1OS=>
PANC1 Mm\ZR5l1d3SxeHnjJGF{e2G7 MnnoOUBl NIPnNmZFVVOR Ml\VTWM2OD12MD60NkDPxE1? NH3NcIUzODR4NkW1OS=>
PC9 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLuW3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVITlJvZHXmbYNq\W62IHj1cYFvKFCFOTDj[YxteyC5aYToJGVEPTBib3[gNE4xOTdizszN M2W1WVIyOjB6OECy
PC9 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfyc5d1cC2{ZYPpd5RidnRiaIXtZY4hWEN7IHPlcIx{KGW6cILld5NqdmdiRVfGVkBGPzR4X1G3OVAwXDd7MF2gcZV1[W62IIfpeIghTUN3MDDv[kA4KM7:TR?= Mnm3NlEzODh6MEK=
PC3 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LnNFExKM7:TR?= NFLnN5U4OiCq NWmye4NVTE2VTx?= Ml;FTWM2OD15LkSg{txO Mn;1NlE{PTN3NE[=
MDA-MB-468 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7afIRLOTByIN88US=> M{mxflQ5KGh? NFn6XG5FVVOR M1LPUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5 M{\aZVIyPDJ7NkOy
Plasmodium falciparum MnnKdWhVWyCycn;mbYxqdmdiZn;yJIlvcGmkaYTvdpMhd2ZiUHzhd41w\Gm3bTDmZYxkcXCjcoXtJJBzd2yrZnXyZZRqd25? MYqyNVgyPzB2NR?=
NCI-H1993 NWfXdJVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy4UGg4OiCq M2KxeGROW09? MUfJR|UxRTBwMTFOwG0> MV6yNVkyPjR|Mx?=
NCI-H292 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXqO|IhcA>? MmrZSG1UVw>? MVHJR|UxRTBwMEKg{txO NIXabY0zOTlzNkSzNy=>
A431 M4jzT2tqdmG|ZTDBd5NigQ>? MmnMNkBp MUTEUXNQ NXnwcI44UW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCHR1[td5RqdXWuYYTl[EBpfW2jbjDBOFMyKHerdHigTWM2OCCxZjCwMlAxOSEQvF2= M1i0dFIzOTBzMUOy
MCF7 NUTjXHJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrTPFZNOTBywrFOwIcwdUx? MorWOFghcA>? NI[1blRFVVOR M{OzUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDveoVz\XiycnXzd4lv\yCHR1\SJIdmdmVid3n0bEBKSzVyIH;mJFEzNjB3IN88US=> NEGy[2wzOjFzOUGzNC=>
BT474 NF[4c5JEgXSxdH;4bYMhSXO|YYm= MoDhNVAh|ryP Mny3OFghcA>? NHnOUJREgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIFLUOFc1KGOnbHzz NUXGVnFwOjJzM{izNFg>
MCF7 MXfDfZRwfG:6aXOgRZN{[Xl? MWGxNEDPxE1? MlzEOFghcA>? MY\DfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKE2FRkegZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEW{YlKyJINmdGy| MUWyNlE{QDNyOB?=
HCC827 NIfpe3RMcW6jc3WgRZN{[Xl? NXPzOGNiOC5zMkWg{txO NVW2fHlQOjRiaB?= M136OGROW09? NVPXXlZuUW6qaXLpeIlwdiCxZjDFS2ZTKGSnbDDFO|Q3NUF5NUCgcZV1[W62IGmxNFY5KGG3dH;wbI9{eGixconsZZRqd25? Ml3mNlI{Ozl|NEK=
HCC827 M3WxUmtqdmG|ZTDBd5NigQ>? MVqwMlEzPSEQvF2= MV:yOEBp NE\IXmlFVVOR M1y0T2lvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfC2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:w NVXOXJdEOjJ|M{mzOFI>
HCC827 MXLLbY5ie2ViQYPzZZk> M{G2OlAvOTJ3IN88US=> NFjmdlYzPCCq M4qzfmROW09? NEPyWVlKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?= MWSyNlM{QTN2Mh?=
A431 M{HnVGtqdmG|ZTDBd5NigQ>? M4rIRVExOCEQvF2= NUjHeYp7OzBibXnu M2G5Z2lvcGmkaYTpc44hd2ZiRVfGVkBl\XKrdnXkJIZzd21iaIXtZY4hSTR|MTDj[YxtKG2nbXLyZY5mKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheG:ueT3HcJUuXHm{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNU4xQCEQvF2= NHi5VVEzOjZ7OEe4Ni=>
H460 M2PtdGN6fG:2b4jpZ{BCe3OjeR?= NUW4T4hwPzJiaB?= NXX3Z|RrUUN3ME21MlU6KM7:TR?= M3v6TlIzPzJ5NES5
HT-29 M3j0dWN6fG:2b4jpZ{BCe3OjeR?= MWe3NkBp MVjJR|UxRTNwM{[g{txO MViyNlczPzR2OR?=
SGC7901 MmXHR5l1d3SxeHnjJGF{e2G7 M33QWFczKGh? MmTwTWM2OD1zMD6yOkDPxE1? NHvtO|UzOjd{N{S0PS=>
A498 M4LwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKGGwZDDTVmMhf2m2aDDJR|UxKG:oIEiuOkDPxE1? M1j6OlIzQDF6OES4
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HCC827 Mn7uR5l1d3SxeHnjJGF{e2G7 MXWxNEDPxGdxbVy= M1HnNFczKGh? MXTJR|UxRTBwMECxOUDPxE1? Mo\sNlMyOTZzNki=
PC9 MmPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37lflExKM7:Zz;tUC=> NETDRpY4OiCq NYj3NlcyUUN3ME2wMlAyPCEQvF2= MkHLNlMyOTZzNki=
Sf9 NEn6b3ZMcW6jc3WgRZN{[Xl? MkfxNUBp MkW2SG1UVw>? M1\G[2lvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLYTh[4dm\CCHR1\SJGw5OzSUIH31eIFvfCCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvODF3IN88US=> M{\2[FI{PjFzNkmx
16HBE14o- NVzqb3JjS3m2b4TvfIlkKEG|c3H5 NVTEWIZDOTBizszN M17IOFczKGh? NUTWdoVXTE2VTx?= NUi3N41WS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMUKuO|Eh|ryP Mo\5NlM3Pjh2NEG=
NCI-H1975 M1j4WWN6fG:2b4jpZ{BCe3OjeR?= M1zDUlExKM7:TR?= Mn:5O|IhcA>? NEPNSYdFVVOR NV71eYQ2S3m2b4TvfIlkcXS7IHHnZYlve3RiZ3XmbZRqdmmkLYLld4l{fGGwdDDoeY1idiCQQ1mtTFE6PzViY3XscJMhcGG{Yn;ybY5oKEWJRmKgUFg2QFJxVEe5NG0h\G:3YnzlJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiNj65NVch|ryP NX7YVVRvOjN4Nki0OFE>
16HBE NVfxcFFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPGO|IhcA>? NHrZUWNFVVOR MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDF4SFLFJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGVITlJid3n0bEBKSzVyIH;mJFEvPjBzIN88US=> NFLKOFAzOzd7MkOxPC=>
16HBE NEixe2FHfW6ldHnvckBCe3OjeR?= NYKwZ2hJOTByIN88US=> NFLEVmYyPTBibXnu NF;yVWNFVVOR MUfJcoR2[3Srb36gc4Yhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36gbY4hcHWvYX6gNVZJSkViY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViRVfGVi=> Ml7jNlM4QTJ|MUi=
A549 Mn;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XTeFczKGh? NWfUdWQ6TE2VTx?= M4nDUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGVITlJxaz3SZZMh\GWyZX7k[Y51KGi3bXHuJGE2PDliY3XscJMhf2m2aDDJR|UxKG:oIESuOlI3KM7:TR?= M1XH[lI{Pzl{M{G4
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LoVo M3;seWtqdmG|ZTDBd5NigQ>? NIfVWm4zKCCq NGHz[XJFVVOR MVrJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB4MjFOwG0> NFzJZWozOzl|MEm5OC=>
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HCC827 NYTYXHFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIKwUHE4OiCq NEK3NHVKSzVyPUCuNFEzKM7:TR?= MkHzNlM6PzNzNki=
A549 M363NGtqdmG|ZTDBd5NigQ>? MXSxJO69VQ>? M4nKe|EhcA>? M13VcGROW09? NHXGTpRKdmirYnn0bY9vKG:oIFXHSnIh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzl7IN88US=> NFLlNIwzOzl6OEO1OC=>
A549 MWTGeY5kfGmxbjDBd5NigQ>? NIPxSIYyKM7:TR?= MnrZNUBp MYjEUXNQ MXLD[YxtfWyjcjD1dJRic2V? NIj2cGMzOzl6OEO1OC=>
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NCI-H1770 MljRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3zTWM2OD15MkKuOEBvVQ>? MkDHV2FPT0WU
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NCI-H1648 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HnWWlEPTB;MT6xNFYyPiEQvF2= MWrTRW5ITVJ?
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NCI-H526 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPrXZRmUUN3ME2xMlQ{QDJ4IN88US=> NHL0OWtUSU6JRWK=
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SCC-25 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK4UZU2UUN3ME2xMlUzOzJ{IN88US=> M3PRS3NCVkeHUh?=
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NCI-H2052 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTvS3JKSzVyPUS1MlkxOjdizszN NEPqPY9USU6JRWK=
SW684 NWjTWHJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;p[2lEPTB;NEeuNFA5OSEQvF2= MW\TRW5ITVJ?
HCC1569 NV:2OXE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqzSFVKSzVyPUS3MlE3PThizszN M1n3U3NCVkeHUh?=
KGN MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR5LkOzNVEh|ryP NFLGU5NUSU6JRWK=
LCLC-103H M3PBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTR5LkS0NFQh|ryP MWrTRW5ITVJ?
SW780 NUTJT2x4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXETWM2OD12Nz62N|UyKM7:TR?= NFe1NIlUSU6JRWK=
NCI-H1703 M2Ha[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\YTWM2OD12OD6zN|UzKM7:TR?= MmTHV2FPT0WU
HCC1395 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H6cWlEPTB;NEiuO|Q{OiEQvF2= NFG4NopUSU6JRWK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
体内試験 Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. [3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. [4]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
- 合併
  • 細胞株: NR6, NR6M and NR6W cells
  • 濃度: 0-2 μM
  • 反応時間: 72 hours
  • 実験の流れ: Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.
    (参考用のみ)
動物試験:[3]
- 合併
  • 動物モデル: Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
  • 製剤: 0.5% polysorbate
  • 投薬量: 100 mg/kg
  • 投与方法: Once daily by oral administration (0.1 mL/10 g body weight) for 14 days
    (参考用のみ)

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 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
1% CMC Na
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 446.90
化学式

C22H24ClFN4O3

CAS No. 184475-35-2
保管
in solvent
別名 N/A
Smiles COC1=C(OCCCN2CCOCC2)C=C3C(=NC=NC3=C1)NC4=CC=C(F)C(=C4)Cl

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03292133 Recruiting Drug: EGF816|Drug: Gefitinib Lung Cancer Massachusetts General Hospital|Novartis October 31 2017 Phase 2
NCT03122717 Recruiting Drug: Gefitinib|Drug: Osimertinib Non-Small Cell Lung Cancer Dana-Farber Cancer Institute|AstraZeneca May 9 2017 Phase 1|Phase 2
NCT02932345 Completed -- EGFR Mutation Positive Advanced Non-small-cell Lung Cancer AstraZeneca October 31 2016 --
NCT02824458 Recruiting Drug: Apatinib|Drug: Gefitinib|Drug: Placebo EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors Sun Yat-sen University June 2016 Phase 3
NCT02804100 Unknown status -- Carcinoma Non-Small-Cell Lung|Bronchial Neoplasms|Carcinoma Bronchogenic|Lung Diseases|Lung Neoplasms Wenzhou Medical University May 2016 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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