Gefitinib (ZD1839)

Catalog No.S1025

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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Cited by 98 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 NWXOOpdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\1TWM2OD1yLkC1OEDPxE1? NYTGcFBoOTZ3MU[0O|M>
NIH3T3 NFu4[3VHfW6ldHnvckBCe3OjeR?= NI\kSVQxNjJizszN MUiyJIg> MX3EUXNQ MXfJcohq[mm2aX;uJI9nKEWJRjDzeIlufWyjdHXkJIh2dWGwIHXyZmIyKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODF2NDFOwG0> MYKxOlQ5ODJ6NB?=
COS7 NWfjXJFtTnWwY4Tpc44hSXO|YYm= Mk\XPVYh|ryP NEnSTG9KdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? MnLuNVcyPzh5MkK=
A549 NYK3S45PS3m2b4TvfIlkKEG|c3H5 M{SzNVk3KGh? M4LCfWROW09? NYXy[W9NUUN3ME2xN{42QSEQvF2= MYWxPFMyOzhyNx?=
K562 MVPDfZRwfG:6aXOgRZN{[Xl? NIrXZ3A6PiCq MoP5SG1UVw>? NWGxT|hRUUN3ME25MlM3KM7:TR?= NH[0bYwyQDNzM{iwOy=>
MDA-MB-231 M{HaemN6fG:2b4jpZ{BCe3OjeR?= NU\kbI84QTZiaB?= MmPtSG1UVw>? M4XKTGlEPTB;M{[uOlEh|ryP NHvPbmsyQDNzM{iwOy=>
MOLT4 M2qzfWN6fG:2b4jpZ{BCe3OjeR?= M2n4NVk3KGh? MWXEUXNQ MUDJR|UxRTF3LkCyJO69VQ>? MlrUNVg{OTN6MEe=
MCF7 M1fleGN6fG:2b4jpZ{BCe3OjeR?= MYK1NEDPxE1? M3L4VVczKGh? MXXJR|UxRTF{LkC1JO69VQ>? NImwXXYyQDd5MUixPS=>
BT474 Mn;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKz[HB7PzJiaB?= Mn25RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuczDveoVz\XiycnXzd4lv\yCHUlLiNkB4cXSqIFXDOVAhd2ZiMD6zJO69VQ>? NUjzcnQ4OTlyMki0NlQ>
HN5 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\IO|IhcA>? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIIfpeIghTUN3MDDv[kAxNjBzIN88US=> NG\r[IYyQTB{OESyOC=>
BA/F3 NEHEeXNEgXSxdH;4bYMhSXO|YYm= NHnwWlk4OiCq NF3LdmtEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO MmLjNVkzOzl{Mkm=
NIH3T3 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXGSVg4OiCq M1zrSmdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJG5KUC9|VEOgZ4VtdHNiZYjwdoV{e2mwZzDldmIzKGenbnWge4l1cCCLQ{WwJI9nKDBwNUSg{txO NVzXU|JOOTl4NkWzO|c>
MCF7 MX NUeyd45TTnWwY4Tpc44hSXO|YYm= MlflN|AhdWmw MXHJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzLkGg{txO M{XD[|E6QTN{OU[w
A431 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnHNVAh|ryP NV:3fG1GPzJiaB?= MXfHTVUxRTBwNUG0JO69VQ>? MXGxPVk3QTR4NR?=
A431 Mlu0T4lv[XOnIFHzd4F6 Ml3CNE4yKM7:TR?= NHrkT44yKGh? NVrRZWx2UW6qaXLpeIlwdiCxZjDFS2YucW6mdXPl[EBGT0[UIIDoc5NxcG:{eXzheIlwdg>? M2HPSVE6QTZ7NE[1
A431 NXLyVYNpU2mwYYPlJGF{e2G7 MlfqNVAxKM7:TR?= NFH0cVEyOCCvaX6= Mni4VJJwdG:wZ3XkJIlvcGmkaYTvdpkh[WO2aY\peJkhd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44> NI\hfXcyQTl4OUS2OS=>
Sf9 M1jEUGtqdmG|ZTDBd5NigQ>? MXGxNEBucW5? MkHkSG1UVw>? M2fWe2lvcGmkaYTpc44hd2ZiRVfGVkBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBz\WOncITvdkBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlA{OyEQvF2= MmTJNlAxPTZ2MkW=
NCI-H1975 NVP6dYZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\DUm42KM7:TR?= NHnTVos4OiCq MYXJR|UxRThwMk[g{txO MWCyNFE2OTZ5MB?=
NCI-H1975 Mnu2T4lv[XOnIFHzd4F6 MkXsNVAh|ryP MkDyTY5pcWKrdHnvckBw\iCHR1\SJIF2fG:yaH;zdIhwenmuYYTpc44> MYqyNFE2OTZ5MB?=
NCI-H1975 MnWwSpVv[3Srb36gRZN{[Xl? M2TBRlExKM7:TR?= NETEdpVKdmirYnn0bY9vKG:oIFXSRmIzKGG3dH;wbI9{eGixconsZZRqd25? Mny3NlAyPTF4N{C=
NCI-H1975 M2j6VWZ2dmO2aX;uJGF{e2G7 MXW1JO69VQ>? NYfPflg5PDhiaB?= NGXOT5lKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiY3HzdIF{\S1| NF3uOYszODF3MU[3NC=>
A375 Mn;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLROFghcA>? NF\abG5KSzVyPUKwMlU2KM7:TR?= MmfPNlA{ODR3M{e=
SMMC7721 M2K2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofnOFghcA>? MkDoTWM2OD1|Mz6xNkDPxE1? M4fXRVIxOzB2NUO3
DU145 NYW3dI1RS3m2b4TvfIlkKEG|c3H5 NV;MTpUxPSCm NWn0bIhrTE2VTx?= NHf3VWpKSzVyPUSyMlE4KM7:TR?= Mmn2NlA1PjZ3NUW=
MIAPaCa2 NIHlenBEgXSxdH;4bYMhSXO|YYm= NUftTYJGPSCm NGmwU45FVVOR M3X5ZWlEPTB;NUCuOlIh|ryP MoDBNlA1PjZ3NUW=
PANC1 NXPBW5dDS3m2b4TvfIlkKEG|c3H5 MXi1JIQ> NHzoWHFFVVOR NVv2UIw{UUN3ME20NE41OiEQvF2= M4Dv[VIxPDZ4NUW1
PC9 M1;LSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HmcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSWdHWi2mZX\pZ4lmdnRiaIXtZY4hWEN7IHPlcIx{KHerdHigSWM2OCCxZjCwMlAyPyEQvF2= M4WyTlIyOjB6OECy
PC9 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL0d|dwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEB4cXSqIFXDOVAhd2ZiNzFOwG0> M2PPbVIyOjB6OECy
PC3 NGC2NIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\1VW0yOCEQvF2= MVK3NkBp Mlz4SG1UVw>? M2rJ[WlEPTB;Nz60JO69VQ>? MWGyNVM2OzV2Nh?=
MDA-MB-468 M{DVc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPkVVYyODBizszN MmPmOFghcA>? MoTCSG1UVw>? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eR?= NGXoWIozOTR{OU[zNi=>
Plasmodium falciparum M4XYVpFJXFNicILv[oltcW6pIH\vdkBqdmirYnn0c5J{KG:oIGDsZZNud2SrdX2g[oFt[2myYYL1cUBxem:uaX\ldoF1cW:w NVrQV3RMOjF6MUewOFU>
NCI-H1993 M2K5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEixN3o4OiCq Mn31SG1UVw>? M1PuSGlEPTB;MD6xJO69VQ>? NEWxcXkzOTlzNkSzNy=>
NCI-H292 NXPSOHpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv2R3Q4OiCq NXLxN4VVTE2VTx?= NWSzfGp[UUN3ME2wMlAzKM7:TR?= MonINlE6OTZ2M{O=
A431 MWjLbY5ie2ViQYPzZZk> NVOySll6OiCq MkLGSG1UVw>? NH;UVHZKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIFG0N|Ehf2m2aDDJR|UxKG:oIECuNFAyKM7:TR?= NXn2WZBsOjJzMEGxN|I>
MCF7 NInpbXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOxNFDDqM7:Zz;tUC=> M{DaTlQ5KGh? MVTEUXNQ NHrFXItCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgc5ZmemW6cILld5NqdmdiRVfGVkBo\W6nIIfpeIghUUN3MDDv[kAyOi5yNTFOwG0> M2[1SFIzOTF7MUOw
BT474 MVTDfZRwfG:6aXOgRZN{[Xl? MWKxNEDPxE1? Ml7GOFghcA>? MVfDfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKEKWNEe0JINmdGy| MYiyNlE{QDNyOB?=
MCF7 MWLDfZRwfG:6aXOgRZN{[Xl? NILBVHcyOCEQvF2= MUK0PEBp NYKwdnU2S3m2b4TvfIlkcXS7IHHnZYlve3Ric3XyeY0ue3Sjco\l[EBpfW2jbjDNR2Y4KGOnbHzzJI93\XJvZYjwdoV{e2mwZzDFdoJDOiClZXzsdy=> M3ToPFIzOTN6M{C4
HCC827 M3XQSGtqdmG|ZTDBd5NigQ>? MoqzNE4yOjVizszN M1nyTVI1KGh? MmLPSG1UVw>? M2\sOGlvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfCC\MUC2PEBifXSxcHjvd5Bpd3K7bHH0bY9v NGLSVXozOjN|OUO0Ni=>
HCC827 M3GyfmtqdmG|ZTDBd5NigQ>? NWH5bGEyOC5zMkWg{txO NXTNVXBmOjRiaB?= M4S1TmROW09? NFH6TYxKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbh?= NHTWWHgzOjN|OUO0Ni=>
HCC827 NVfC[2J6U2mwYYPlJGF{e2G7 M{DnflAvOTJ3IN88US=> MWqyOEBp MVzEUXNQ MoTrTY5pcWKrdHnvckBw\iCHR1\SJIRmdCCHN{S2MWE4PTBibYX0ZY51NW2nZHnheIVlKEGtdDDwbI9{eGixconsZZRqd25? M2P6c|IzOzN7M{Sy
A431 NGqzWYhMcW6jc3WgRZN{[Xl? NGC5cZAyODBizszN NXzwUHJqOzBibXnu MoO0TY5pcWKrdHnvckBw\iCHR1\SJIRmemm4ZXSg[pJwdSCqdX3hckBCPDNzIHPlcIwhdWWvYoLhcoUh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBxd2y7LVfseU1VgXJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCxMlA5KM7:TR?= MoHNNlI3QTh5OEK=
H460 NW\mZ3pXS3m2b4TvfIlkKEG|c3H5 MYK3NkBp NHrwPJFKSzVyPUWuOVkh|ryP NXu5[5c3OjJ5Mke0OFk>
HT-29 NHHYNJZEgXSxdH;4bYMhSXO|YYm= M4e4Z|czKGh? NGfZV45KSzVyPUOuN|Yh|ryP NV7sOoRzOjJ5Mke0OFk>
SGC7901 NYjmTHBpS3m2b4TvfIlkKEG|c3H5 NEO2T404OiCq MkD0TWM2OD1zMD6yOkDPxE1? NXS4PG5MOjJ5Mke0OFk>
A498 MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrpRlJlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIV5eHKnc4PpcochTUeIUjDhcoQhW1KFIIfpeIghUUN3MDDv[kA5NjZizszN NWTiOHh3OjJ6MUi4OFg>
Calu3 MkTiR5l1d3SxeHnjJGF{e2G7 M2\yeVExKM7:Zz;tUC=> MX[3NkBp MUXJR|UxRTFwNjFOwG0> M2L2XFI{OTF4MU[4
FADU MkDIR5l1d3SxeHnjJGF{e2G7 M1XXfFExKM7:Zz;tUC=> MU[3NkBp NWfpZpVqUUN3ME2wMlA2KM7:TR?= M2TWUVI{OTF4MU[4
HCC827 MV;DfZRwfG:6aXOgRZN{[Xl? Mly5NVAh|rypL33M Mn\4O|IhcA>? NX;lSXpMUUN3ME2wMlAxOTVizszN NUf2V|ZrOjNzMU[xOlg>
PC9 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmThNVAh|rypL33M NHf6R4c4OiCq NVXkNotEUUN3ME2wMlAyPCEQvF2= MnLINlMyOTZzNki=
Sf9 MV;LbY5ie2ViQYPzZZk> NWnUZYpTOSCq MXHEUXNQ NI[yVFhKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD30ZYdo\WRiRVfGVkBNQDN2UjDteZRidnRiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> M3S2PFI{PjFzNkmx
16HBE14o- NIG4O2FEgXSxdH;4bYMhSXO|YYm= MkTENVAh|ryP NH7CTXg4OiCq MnLYSG1UVw>? M2K5fGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFE3UEKHMUTvMUBk\WyuczDoZZJjd3Krbnege4lt\CC2eYDlJGVITlJiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDF{LkexJO69VQ>? MVmyN|Y3QDR2MR?=
NCI-H1975 MWLDfZRwfG:6aXOgRZN{[Xl? NHOzT20yOCEQvF2= M13wXVczKGh? NWPvOotWTE2VTx?= MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBo\W[rdHnubYIuemW|aYP0ZY51KGi3bXHuJG5EUS2KMUm3OUBk\WyuczDoZZJjd3KrbnegSWdHWiCOOEW4Vk9VPzlyTTDkc5VjdGVibYX0ZY51KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kA3NjlzNzFOwG0> MnPONlM3Pjh2NEG=
16HBE NYi2NGk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXTNpU4OiCq MlrGSG1UVw>? MmXCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiBzNljCSUBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIIfpeIghUUN3MDDv[kAyNjZyMTFOwG0> NHuyfXQzOzd7MkOxPC=>
16HBE NHziT5pHfW6ldHnvckBCe3OjeR?= NG\6N2IyODBizszN NX7ITVE5OTVyIH3pci=> MV3EUXNQ NYLJV3EzUW6mdXP0bY9vKG:oIH7peJJq[yCxeHnk[UBxem:mdXP0bY9vKGmwIHj1cYFvKDF4SFLFJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGVITlJ? M4X2VFI{Pzl{M{G4
A549 NXm4U5N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\XSFBbPzJiaB?= Mn[ySG1UVw>? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIfpcIQhfHmyZTDFS2ZTN2tvUnHzJIRmeGWwZHXueEBpfW2jbjDBOVQ6KGOnbHzzJJdqfGhiSVO1NEBw\iB2Lk[yOkDPxE1? MUKyN|c6OjNzOB?=
SH-SY5Y MXLDfZRwfG:6aXOgRZN{[Xl? M1n4PFczKGh? Mk\ZTWM2OD1zOD6yNUDPxE1? MlzTNlM5PzF7MEm=
LoVo M17DRmtqdmG|ZTDBd5NigQ>? M2jB[VIhKGh? Mk\QSG1UVw>? NXrlZmNvUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wOlIh|ryP MnTTNlM6OzB7OUS=
PC9 M2ToZ2tqdmG|ZTDBd5NigQ>? MoXBNkBp MUPEUXNQ MlfRTY5pcWKrdHnvckBw\iCHR1\SJIV5d25iMUmg[IVt\XSrb36gZYN1cX[jdHnu[{BufXSjboSgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGDDPUBk\WyuczD3bZRpKEmFNUCgc4YhOC5yMEi3JO69VQ>? MWKyN|k{ODl7NB?=
HCC827 NVXwWZVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:0O|IhcA>? NInDcFFKSzVyPUCuNFEzKM7:TR?= MYmyN|k4OzF4OB?=
A549 M4XVfGtqdmG|ZTDBd5NigQ>? NIr4PJgyKM7:TR?= Mnz0NUBp MnjlSG1UVw>? MmTvTY5pcWKrdHnvckBw\iCHR1\SJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFM6QSEQvF2= NV\rS2NiOjN7OEizOVQ>
A549 MXnGeY5kfGmxbjDBd5NigQ>? NITCUooyKM7:TR?= NFTqTXQyKGh? NITxTYhFVVOR MkHFR4VtdHWuYYKgeZB1[Wun NEjufm8zOzl6OEO1OC=>
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NCI-H810 NXrUZpRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDTTWM2OD1zMD6xOVk4KM7:TR?= NVrLcm51W0GQR1XS
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H-EMC-SS NXe1THE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW4OoVKSzVyPUS1Mlc3QTNizszN NGLQXIlUSU6JRWK=
NCI-H2052 M2nudmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTR3LkmwNlch|ryP MlLYV2FPT0WU
SW684 NWrnN3pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFi5VIdKSzVyPUS3MlAxQDFizszN M2LUNnNCVkeHUh?=
HCC1569 NVvoR3RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HWfWlEPTB;NEeuNVY2QCEQvF2= NWTreohYW0GQR1XS
KGN NGTFdIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TLNGlEPTB;NEeuN|MyOSEQvF2= NUP4SFE6W0GQR1XS
LCLC-103H NYe1OohrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYGyeItLUUN3ME20O{41PDB2IN88US=> NFL1ZXlUSU6JRWK=
SW780 NHPHVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zZVWlEPTB;NEeuOlM2OSEQvF2= MkLIV2FPT0WU
NCI-H1703 NX;ofGwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;IRnhKSzVyPUS4MlM{PTJizszN NHXwXWFUSU6JRWK=
HCC1395 M{PENGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rqU2lEPTB;NEiuO|Q{OiEQvF2= MYXTRW5ITVJ?

... 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]
+ Expand
  • 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]
+ Expand
  • 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

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 (g) = Concentration (mol/L) × Volume (L) × 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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The Serial Dilution Calculator Equation

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

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