Gefitinib (ZD1839)

For research use only. Not for use in humans.

Catalog No.S1025

287 publications

Gefitinib (ZD1839) Chemical Structure

Molecular Weight(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.

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Selleck's Gefitinib (ZD1839) has been cited by 287 publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description 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.
Features A potent EGFR tyrosine kinase inhibitor.
Targets
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WzRWlEPTB;MD6wOVQh|ryP NXLSe|dDOTZ3MU[0O|M>
NIH3T3 M1\yXmZ2dmO2aX;uJGF{e2G7 NVHJUXVxOC5{IN88US=> M4H0[VIhcA>? MmHRSG1UVw>? Ml7GTY5pcWKrdHnvckBw\iCHR1[gd5RqdXWuYYTl[EBpfW2jbjDldoJDOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNESg{txO M4rYXlE3PDhyMki0
COS7 Ml7HSpVv[3Srb36gRZN{[Xl? NYnJZYhNQTZizszN NGK2WWVKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? M4PYcFE4OTd6N{Ky
A549 MoSwR5l1d3SxeHnjJGF{e2G7 NXuzeYt[QTZiaB?= NHTjVZBFVVOR M3viNWlEPTB;MUOuOVkh|ryP MUKxPFMyOzhyNx?=
K562 MXXDfZRwfG:6aXOgRZN{[Xl? NUnFeItTQTZiaB?= NUPadndWTE2VTx?= Mn74TWM2OD17LkO2JO69VQ>? M{Pic|E5OzF|OEC3
MDA-MB-231 M2rIOmN6fG:2b4jpZ{BCe3OjeR?= NF3XNos6PiCq M3Psd2ROW09? M3jRRWlEPTB;M{[uOlEh|ryP M4XjOFE5OzF|OEC3
MOLT4 M12wRWN6fG:2b4jpZ{BCe3OjeR?= NF;BS2Q6PiCq NWm2eVRuTE2VTx?= NUDhSYNlUUN3ME2xOU4xOiEQvF2= NEfSPHAyQDNzM{iwOy=>
MCF7 NFHLN3ZEgXSxdH;4bYMhSXO|YYm= NYPUWHhTPTBizszN NHnIeXU4OiCq NYDGflhQUUN3ME2xNk4xPSEQvF2= M3rQ[VE5PzdzOEG5
BT474 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzpO|IhcA>? M2fX[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS0O|Qh[2WubIOgc5ZmemW6cILld5NqdmdiRWLCZlIhf2m2aDDFR|UxKG:oIECuN{DPxE1? NVfO[ZV7OTlyMki0NlQ>
HN5 M2XyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTabFE4OiCq MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIIfpeIghTUN3MDDv[kAxNjBzIN88US=> M4fxV|E6ODJ6NEK0
BA/F3 NVHqSG9lS3m2b4TvfIlkKEG|c3H5 MYO3NkBp NGXOb4tEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO Mn23NVkzOzl{Mkm=
NIH3T3 M2O1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;2RlBuPzJiaB?= NYjhUpNVT3Kxd4ToJIlvcGmkaYTpc44hd2ZibX;1d4UhVkmKL{PUN{Bk\WyuczDlfJBz\XO|aX7nJIVzSjJiZ3Xu[UB4cXSqIFnDOVAhd2ZiMD61OEDPxE1? MofmNVk3PjV|N{e=
MCF7 MX MVLGeY5kfGmxbjDBd5NigQ>? NHToS|Q{OCCvaX6= MnXiTY5pcWKrdHnvckBw\iCEQ2LQJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMT6xJO69VQ>? MoHqNVk6OzJ7NkC=
A431 NELkU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq1NHMyOCEQvF2= M3HMSlczKGh? NX7aS45rT0l3ME2wMlUyPCEQvF2= M1\1clE6QTZ7NE[1
A431 MmjBT4lv[XOnIFHzd4F6 NID5OZAxNjFizszN NVjQ[pdSOSCq MVPJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;u NGf0V48yQTl4OUS2OS=>
A431 NIi0c4pMcW6jc3WgRZN{[Xl? NXjZWZlHOTByIN88US=> MXqxNEBucW5? MlXXVJJwdG:wZ3XkJIlvcGmkaYTvdpkh[WO2aY\peJkhd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44> MomyNVk6Pjl2NkW=
Sf9 MlHuT4lv[XOnIFHzd4F6 MWWxNEBucW5? NV65TGJ[TE2VTx?= NW\oemZ1UW6qaXLpeIlwdiCxZjDFS2ZTKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKnY3XweI9zKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN|IN88US=> M2HrWlIxODV4NEK1
NCI-H1975 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXBOUDPxE1? M3PwcFczKGh? Ml\RTWM2OD16LkK2JO69VQ>? M3TQ[lIxOTVzNkew
NCI-H1975 NWPKXlN7U2mwYYPlJGF{e2G7 NHLDNIwyOCEQvF2= NE\uNZJKdmirYnn0bY9vKG:oIFXHSnIh[XW2b4Doc5NxcG:{eXzheIlwdg>? NUTxcHZDOjBzNUG2O|A>
NCI-H1975 NIr6O3ZHfW6ldHnvckBCe3OjeR?= NFTZfVUyOCEQvF2= MkHTTY5pcWKrdHnvckBw\iCHUlLCNkBifXSxcHjvd5Bpd3K7bHH0bY9v NGHxengzODF3MU[3NC=>
NCI-H1975 M1PqN2Z2dmO2aX;uJGF{e2G7 MlnPOUDPxE1? M{PUVlQ5KGh? NHLBXGRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiY3HzdIF{\S1| NGTId|UzODF3MU[3NC=>
A375 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XreFQ5KGh? MXLJR|UxRTJyLkW1JO69VQ>? NV3KVIp{OjB|MES1N|c>
SMMC7721 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TPRVQ5KGh? MXzJR|UxRTN|LkGyJO69VQ>? M1zjWVIxOzB2NUO3
DU145 Ml7uR5l1d3SxeHnjJGF{e2G7 M3nXNFUh\A>? NXP4WIpvTE2VTx?= NH\hflBKSzVyPUSyMlE4KM7:TR?= M4O0VlIxPDZ4NUW1
MIAPaCa2 NYPzU4Z5S3m2b4TvfIlkKEG|c3H5 MW[1JIQ> NY\rXXA2TE2VTx?= MlHlTWM2OD13MD62NkDPxE1? MWKyNFQ3PjV3NR?=
PANC1 MnzSR5l1d3SxeHnjJGF{e2G7 NFeyUFE2KGR? M4LvXWROW09? MX3JR|UxRTRyLkSyJO69VQ>? MVeyNFQ3PjV3NR?=
PC9 NXvybWdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXHSnIu\GWoaXPp[Y51KGi3bXHuJHBEQSClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wNVch|ryP M13GVVIyOjB6OECy
PC9 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfyc5d1cC2{ZYPpd5RidnRiaIXtZY4hWEN7IHPlcIx{KGW6cILld5NqdmdiRVfGVkBGPzR4X1G3OVAwXDd7MF2gcZV1[W62IIfpeIghTUN3MDDv[kA4KM7:TR?= NIrGb4YzOTJyOEiwNi=>
PC3 MmnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSxNEDPxE1? MlfmO|IhcA>? MUTEUXNQ MkTrTWM2OD15LkSg{txO NFjUcYMzOTN3M{W0Oi=>
MDA-MB-468 M4m0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHmVZVKOTByIN88US=> MYm0PEBp NF20SoRFVVOR NUK3NnhZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJk> MlfhNlE1Ojl4M{K=
Plasmodium falciparum M1XmTpFJXFNicILv[oltcW6pIH\vdkBqdmirYnn0c5J{KG:oIGDsZZNud2SrdX2g[oFt[2myYYL1cUBxem:uaX\ldoF1cW:w M1i4elIyQDF5MES1
NCI-H1993 M4jlbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv2Z4c4OiCq Ml\aSG1UVw>? NXjoUGY2UUN3ME2wMlEh|ryP MljaNlE6OTZ2M{O=
NCI-H292 M4rOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC2O|IhcA>? NFPsN4RFVVOR NH7F[oFKSzVyPUCuNFIh|ryP M1jsUFIyQTF4NEOz
A431 MmfPT4lv[XOnIFHzd4F6 NInqWXczKGh? NUjqSVluTE2VTx?= MYjJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHnuJGVITi2|dHnteYxifGWmIHj1cYFvKEF2M{Gge4l1cCCLQ{WwJI9nKDBwMECxJO69VQ>? NF:xfJYzOjFyMUGzNi=>
MCF7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrVZ3IyODEEoN88[{9uVA>? NH7hVFY1QCCq M3WxTmROW09? NVm5epFMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXHSnIh\2WwZTD3bZRpKEmFNUCgc4YhOTJwMEWg{txO MX2yNlEyQTF|MB?=
BT474 NGjWdGpEgXSxdH;4bYMhSXO|YYm= M2\VTVExKM7:TR?= MmLPOFghcA>? NIDjOG1EgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIFLUOFc1KGOnbHzz MXGyNlE{QDNyOB?=
MCF7 MlfZR5l1d3SxeHnjJGF{e2G7 MmrFNVAh|ryP MojnOFghcA>? NFXZOGhEgXSxdH;4bYNqfHliYXfhbY5{fCC|ZYL1cU1{fGG{dnXkJIh2dWGwIF3DSlch[2WubIOgc5Zmei2neIDy[ZN{cW6pIFXyZmIzKGOnbHzz MUiyNlE{QDNyOB?=
HCC827 MVXLbY5ie2ViQYPzZZk> NFTEXXkxNjF{NTFOwG0> NHKwW4ozPCCq MVXEUXNQ MWjJcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQhYTFyNkigZZV1d3Cqb4PwbI9zgWyjdHnvci=> MWGyNlM{QTN2Mh?=
HCC827 MV\LbY5ie2ViQYPzZZk> M1jzeFAvOTJ3IN88US=> NF\jSZAzPCCq NX71[HA3TE2VTx?= NEj1fHhKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbh?= NVn6d4ZXOjJ|M{mzOFI>
HCC827 MVvLbY5ie2ViQYPzZZk> NHrqXIwxNjF{NTFOwG0> M1HPWFI1KGh? NGmybllFVVOR NHfSNm9KdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?= MkfBNlI{Ozl|NEK=
A431 MojZT4lv[XOnIFHzd4F6 MmPGNVAxKM7:TR?= NFfKRmQ{OCCvaX6= NHzYRVJKdmirYnn0bY9vKG:oIFXHSnIh\GW{aY\l[EBnem:vIHj1cYFvKEF2M{GgZ4VtdCCvZX3idoFv\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHCxbImtS4x2NVS7cjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEvODhizszN M3\vXFIzPjl6N{iy
H460 MXXDfZRwfG:6aXOgRZN{[Xl? NUDrbnl7PzJiaB?= NH;GUXJKSzVyPUWuOVkh|ryP M4HVe|IzPzJ5NES5
HT-29 M{T3OWN6fG:2b4jpZ{BCe3OjeR?= NXrRNpVHPzJiaB?= NXfhfpdkUUN3ME2zMlM3KM7:TR?= Mmf4NlI4Ojd2NEm=
SGC7901 MmjJR5l1d3SxeHnjJGF{e2G7 NIr4c|I4OiCq M1LpXGlEPTB;MUCuNlYh|ryP NF3vUFIzOjd{N{S0PS=>
A498 M3fNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\0WYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOg[ZhxemW|c3nu[{BGT0[UIHHu[EBUWkNid3n0bEBKSzVyIH;mJFgvPiEQvF2= NH\0T3QzOjhzOEi0PC=>
Calu3 M1rMNWN6fG:2b4jpZ{BCe3OjeR?= NYrWdFNTOTBizsznM41N M{XHVFczKGh? M2HL[GlEPTB;MT62JO69VQ>? M1\ydVI{OTF4MU[4
FADU M33hemN6fG:2b4jpZ{BCe3OjeR?= Ml3yNVAh|rypL33M M1n6OVczKGh? MmPSTWM2OD1yLkC1JO69VQ>? MnPtNlMyOTZzNki=
HCC827 NYjhPZlSS3m2b4TvfIlkKEG|c3H5 NGHiNGUyOCEQvHevcWw> MW[3NkBp M3TpW2lEPTB;MD6wNFE2KM7:TR?= M1PrOFI{OTF4MU[4
PC9 Mkm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT0VpAyOCEQvHevcWw> NWfYco5LPzJiaB?= M13Pe2lEPTB;MD6wNVQh|ryP MXmyN|EyPjF4OB?=
Sf9 MXvLbY5ie2ViQYPzZZk> MV[xJIg> MX7EUXNQ NGWwbWJKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD30ZYdo\WRiRVfGVkBNQDN2UjDteZRidnRiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> MnL5NlM3OTF4OUG=
16HBE14o- NVfq[5FkS3m2b4TvfIlkKEG|c3H5 NGO4N5QyOCEQvF2= MVu3NkBp MWfEUXNQ NYS0Z2JYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOT[KQlWxOI8uKGOnbHzzJIhiemKxcnnu[{B4cWymIIT5dIUhTUeIUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMUKuO|Eh|ryP Mn3RNlM3Pjh2NEG=
NCI-H1975 MUPDfZRwfG:6aXOgRZN{[Xl? NWHSTW86OTBizszN MVO3NkBp MXfEUXNQ NW[3PFA5S3m2b4TvfIlkcXS7IHHnZYlve3RiZ3XmbZRqdmmkLYLld4l{fGGwdDDoeY1idiCQQ1mtTFE6PzViY3XscJMhcGG{Yn;ybY5oKEWJRmKgUFg2QFJxVEe5NG0h\G:3YnzlJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiNj65NVch|ryP NIn6UHIzOzZ4OES0NS=>
16HBE NYfieIp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLBXpN4PzJiaB?= Mn;GSG1UVw>? NEHBcWVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEG2TGJGKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWJRmKge4l1cCCLQ{WwJI9nKDFwNkCxJO69VQ>? NVrzNZhIOjN5OUKzNVg>
16HBE M2LvdmZ2dmO2aX;uJGF{e2G7 NU\W[ZFKOTByIN88US=> MkjSNVUxKG2rbh?= MV7EUXNQ MoWzTY5lfWO2aX;uJI9nKG6rdILpZ{BwgGmmZTDwdo9lfWO2aX;uJIlvKGi3bXHuJFE3UEKHIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXHSnI> NIXmWXUzOzd7MkOxPC=>
A549 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHEVnJlPzJiaB?= MoW5SG1UVw>? MmH0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDD3bYxlKHS7cHWgSWdHWi:tLWLhd{Bl\XCnbnTlcpQhcHWvYX6gRVU1QSClZXzsd{B4cXSqIFnDOVAhd2ZiND62NlYh|ryP M2PoUVI{Pzl{M{G4
SH-SY5Y NEi1VXpEgXSxdH;4bYMhSXO|YYm= NXXwRlV{PzJiaB?= MYnJR|UxRTF6LkKxJO69VQ>? M1faclI{QDdzOUC5
LoVo NVn6VnpQU2mwYYPlJGF{e2G7 NVOyPYt3OiBiaB?= M{nHOWROW09? MXrJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB4MjFOwG0> NFraXnMzOzl|MEm5OC=>
PC9 M{XVcmtqdmG|ZTDBd5NigQ>? NXfySlJROiCq MXvEUXNQ M{mzTWlvcGmkaYTpc44hd2ZiRVfGVkBmgG:wIEG5JIRmdGW2aX;uJIFkfGm4YYTpcochdXW2YX70JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDQR|kh[2WubIOge4l1cCCLQ{WwJI9nKDBwMEC4O{DPxE1? NGG3VGIzOzl|MEm5OC=>
HCC827 NVH2cZY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED6OYs4OiCq M2nrXWlEPTB;MD6wNVIh|ryP MUOyN|k4OzF4OB?=
A549 MWDLbY5ie2ViQYPzZZk> M1XiPFEh|ryP Ml3ONUBp NGXBXIlFVVOR MUDJcohq[mm2aX;uJI9nKEWJRmKgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wN|k6KM7:TR?= Mn3HNlM6QDh|NUS=
A549 NY\DcHRXTnWwY4Tpc44hSXO|YYm= M3y1T|Eh|ryP NHG1eZcyKGh? NV3MeZNSTE2VTx?= M{jhR2NmdGy3bHHyJJVxfGGtZR?= MnjVNlM6QDh|NUS=
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NCI-H2052 NV7mbW57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrvNXMyUUN3ME20OU46ODJ5IN88US=> M3z2NXNCVkeHUh?=
SW684 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfuXXNlUUN3ME20O{4xODhzIN88US=> MXTTRW5ITVJ?
HCC1569 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfCVGpKSzVyPUS3MlE3PThizszN NHz4OFVUSU6JRWK=
KGN MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K3RWlEPTB;NEeuN|MyOSEQvF2= MWDTRW5ITVJ?
LCLC-103H MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u4e2lEPTB;NEeuOFQxPCEQvF2= NHHRbFJUSU6JRWK=
SW780 NWPNTHVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHvVZlXUUN3ME20O{43OzVzIN88US=> NFznOo9USU6JRWK=
NCI-H1703 NEnSemZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTR6LkOzOVIh|ryP M3vSdXNCVkeHUh?=
HCC1395 NX\zVFI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnkPVZKSzVyPUS4Mlc1OzJizszN NFeyNmpUSU6JRWK=

... 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
In vivo 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]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: NR6, NR6M and NR6W cells
  • Concentrations: 0-2 μM
  • Incubation Time: 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[3]
- Collapse
  • Animal Models: Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
  • Formulation: 0.5% polysorbate
  • Dosages: 100 mg/kg
  • Administration: Once daily by oral administration (0.1 mL/10 g body weight) for 14 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (199.14 mM)
Ethanol 4 mg/mL (8.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 446.90
Formula

C22H24ClFN4O3

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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 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?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID