Gefitinib (ZD1839)

For research use only.

Catalog No.S1025

360 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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

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Selleck's Gefitinib (ZD1839) has been cited by 360 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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
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 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm5TWM2OD1yLkC1OEDPxE1? MVOxOlUyPjR5Mx?=
NIH3T3 M1[we2Z2dmO2aX;uJGF{e2G7 NVPZ[4NXOC5{IN88US=> MYCyJIg> M1v2NGROW09? NXfCUYhsUW6qaXLpeIlwdiCxZjDFS2Yhe3SrbYXsZZRm\CCqdX3hckBmemKEMTDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxOFQh|ryP NXWzOoR[OTZ2OECyPFQ>
COS7 M2nLXmZ2dmO2aX;uJGF{e2G7 NYHJXlNQQTZizszN NHz3TZlKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\A>? MojUNVcyPzh5MkK=
A549 NYHRWHRLS3m2b4TvfIlkKEG|c3H5 NFn5Vm06PiCq NIroVFZFVVOR MmnBTWM2OD1zMz61PUDPxE1? NWr2bmdYOTh|MUO4NFc>
K562 NFvPWGZEgXSxdH;4bYMhSXO|YYm= NHj6XJk6PiCq NXTRT|BRTE2VTx?= M3;5[WlEPTB;OT6zOkDPxE1? MWSxPFMyOzhyNx?=
MDA-MB-231 NHmy[Y9EgXSxdH;4bYMhSXO|YYm= NXjyOIozQTZiaB?= NFTufGdFVVOR NYX3eIRoUUN3ME2zOk43OSEQvF2= Moe4NVg{OTN6MEe=
MOLT4 MUPDfZRwfG:6aXOgRZN{[Xl? M363Xlk3KGh? MlTDSG1UVw>? MlK5TWM2OD1zNT6wNkDPxE1? NFnrfG8yQDNzM{iwOy=>
MCF7 M2DqSGN6fG:2b4jpZ{BCe3OjeR?= MkHROVAh|ryP MVO3NkBp MX;JR|UxRTF{LkC1JO69VQ>? M4nFfVE5PzdzOEG5
BT474 M2q3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnzc3g4OiCq MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWUQnKyJJdqfGhiRVO1NEBw\iByLkOg{txO NFSxSVcyQTB{OESyOC=>
HN5 NWfrelF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrMZo93PzJiaB?= NFHwOFFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuczDveoVz\XiycnXzd4lv\yCHR1\SJJdqfGhiRVO1NEBw\iByLkCxJO69VQ>? M{HETlE6ODJ6NEK0
BA/F3 MonKR5l1d3SxeHnjJGF{e2G7 MX23NkBp NWO3TIhDS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEx6NUjSJI12fGGwdDD3bZRpKEmFNUCgc4YhOC5yMUC4JO69VQ>? MmrlNVkzOzl{Mkm=
NIH3T3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7vXlh7PzJiaB?= MUPHdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDOTWgwO1R|IHPlcIx{KGW6cILld5NqdmdiZYLCNkBo\W6nIIfpeIghUUN3MDDv[kAxNjV2IN88US=> MWWxPVY3PTN5Nx?=
MCF7 MX MWLGeY5kfGmxbjDBd5NigQ>? MU[zNEBucW5? NGTVUZVKdmirYnn0bY9vKG:oIFLDVnAh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxMlEh|ryP MkP4NVk6OzJ7NkC=
A431 NXnLcYh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC0cmlQOTBizszN M{\VT|czKGh? M1LkZmdKPTB;MD61NVQh|ryP NF:wOGoyQTl4OUS2OS=>
A431 NVH4em1tU2mwYYPlJGF{e2G7 MVewMlEh|ryP MV:xJIg> NEnyVXNKdmirYnn0bY9vKG:oIFXHSk1qdmS3Y3XkJGVITlJicHjvd5Bpd3K7bHH0bY9v M4nJeFE6QTZ7NE[1
A431 M2\0VmtqdmG|ZTDBd5NigQ>? Mkj6NVAxKM7:TR?= NFfncGwyOCCvaX6= MV;Qdo9td26pZXSgbY5pcWKrdH;yfUBi[3Srdnn0fUBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvci=> M2r0[lE6QTZ7NE[1
Sf9 Ml[yT4lv[XOnIFHzd4F6 MVSxNEBucW5? Ml7FSG1UVw>? NUHBTnFrUW6qaXLpeIlwdiCxZjDFS2ZTKGW6cILld5Nm\CCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKnY3XweI9zKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN|IN88US=> M1zyXVIxODV4NEK1
NCI-H1975 NVXIPW1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi1JO69VQ>? NYjzNoJzPzJiaB?= MV\JR|UxRThwMk[g{txO NHf3ZmkzODF3MU[3NC=>
NCI-H1975 MoPMT4lv[XOnIFHzd4F6 MW[xNEDPxE1? NVHGPVNEUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25? NEDMTWgzODF3MU[3NC=>
NCI-H1975 M2nmfGZ2dmO2aX;uJGF{e2G7 NInqNokyOCEQvF2= NGrEdXhKdmirYnn0bY9vKG:oIFXSRmIzKGG3dH;wbI9{eGixconsZZRqd25? NH;POZYzODF3MU[3NC=>
NCI-H1975 NH33T2ZHfW6ldHnvckBCe3OjeR?= MkfCOUDPxE1? M3\VdVQ5KGh? M1OyVGlv\HWldHnvckBw\iCjcH;weI9{cXNiYYPz[ZN{\WRiYYOgZYN1cX[jdHnvckBw\iClYYPwZZNmNTN? MWKyNFE2OTZ5MB?=
A375 NYrLblJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTieHc1QCCq NVvve4U{UUN3ME2yNE42PSEQvF2= NFrGSm0zODNyNEWzOy=>
SMMC7721 NHmwcJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLCflY1QCCq NHTqem1KSzVyPUOzMlEzKM7:TR?= M4nzVFIxOzB2NUO3
DU145 NH7mdpFEgXSxdH;4bYMhSXO|YYm= MlnKOUBl MmL5SG1UVw>? NEjnV2NKSzVyPUSyMlE4KM7:TR?= MYGyNFQ3PjV3NR?=
MIAPaCa2 NY\iXGpbS3m2b4TvfIlkKEG|c3H5 NInJWm02KGR? NYT2VlRPTE2VTx?= M3nze2lEPTB;NUCuOlIh|ryP M{HET|IxPDZ4NUW1
PANC1 M1;WT2N6fG:2b4jpZ{BCe3OjeR?= M{DIc|Uh\A>? NV\LSWVkTE2VTx?= NVjEeJlZUUN3ME20NE41OiEQvF2= MnGxNlA1PjZ3NUW=
PC9 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\DRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFS2ZTNWSnZnnjbYVvfCCqdX3hckBRSzliY3XscJMhf2m2aDDFR|UxKG:oIECuNFE4KM7:TR?= MU[yNVIxQDhyMh?=
PC9 NVT1W3d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTE[VFOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBoem:5dHitdoV{cXO2YX70JIh2dWGwIGDDPUBk\WyuczDlfJBz\XO|aX7nJGVITlJiRUe0On9CPzVyL2S3PVBOKG23dHHueEB4cXSqIFXDOVAhd2ZiNzFOwG0> MY[yNVIxQDhyMh?=
PC3 M3z1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxNEDPxE1? MX23NkBp NI\KXpFFVVOR MkDCTWM2OD15LkSg{txO MWOyNVM2OzV2Nh?=
MDA-MB-468 M3r6fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3HOJdmOTByIN88US=> NX7LRYVEPDhiaB?= M1nTeGROW09? MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eR?= NWP3N5czOjF2Mkm2N|I>
Plasmodium falciparum MnHJdWhVWyCycn;mbYxqdmdiZn;yJIlvcGmkaYTvdpMhd2ZiUHzhd41w\Gm3bTDmZYxkcXCjcoXtJJBzd2yrZnXyZZRqd25? NXPodm5iOjF6MUewOFU>
NCI-H1993 NEDK[2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DqUFczKGh? NHfz[YlFVVOR MUTJR|UxRTBwMTFOwG0> Ml;6NlE6OTZ2M{O=
NCI-H292 NF21RWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzHbo1sPzJiaB?= M1\sfmROW09? M2DoS2lEPTB;MD6wNkDPxE1? M4XPN|IyQTF4NEOz
A431 NXjXcVRNU2mwYYPlJGF{e2G7 M1XxXVIhcA>? M{S3d2ROW09? NGDERVdKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIFG0N|Ehf2m2aDDJR|UxKG:oIECuNFAyKM7:TR?= MX6yNlExOTF|Mh?=
MCF7 NYG4SGFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH0NVAxyqEQvHevcWw> NWq5[IhXPDhiaB?= M2KxT2ROW09? Mki0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKg[4Vv\SC5aYToJGlEPTBib3[gNVIvODVizszN M17WPFIzOTF7MUOw
BT474 M2XkdGN6fG:2b4jpZ{BCe3OjeR?= M3joTFExKM7:TR?= M4\4VlQ5KGh? MlO5R5l1d3SxeHnjbZR6KGGpYXnud5Qhe2W{dX2td5Rien[nZDDoeY1idiCEVES3OEBk\Wyucx?= NITKNWkzOjF|OEOwPC=>
MCF7 NGjQVolEgXSxdH;4bYMhSXO|YYm= Ml;BNVAh|ryP Mm\zOFghcA>? M{L6Z2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KHOncoXtMZN1[XK4ZXSgbJVu[W5iTVPGO{Bk\WyuczDveoVzNWW6cILld5NqdmdiRYLiRlIh[2WubIO= MVeyNlE{QDNyOB?=
HCC827 MYLLbY5ie2ViQYPzZZk> MUWwMlEzPSEQvF2= MonmNlQhcA>? NGLXO5NFVVOR MYTJcohq[mm2aX;uJI9nKEWJRmKg[IVtKEV5NE[tRVc2OCCvdYThcpQhYTFyNkigZZV1d3Cqb4PwbI9zgWyjdHnvci=> MVyyNlM{QTN2Mh?=
HCC827 MWXLbY5ie2ViQYPzZZk> MYGwMlEzPSEQvF2= MYGyOEBp MnnGSG1UVw>? Mlz5TY5pcWKrdHnvckBw\iCHR1\SJIRmdCCHN{S2MWE4PTBibYX0ZY51NW2nZHnheIVlKEW{azDwbI9{eGixconsZZRqd25? NVPRZpYyOjJ|M{mzOFI>
HCC827 MV3LbY5ie2ViQYPzZZk> MV:wMlEzPSEQvF2= MmniNlQhcA>? NGjCdW1FVVOR M1:2SGlvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfC2vZXTpZZRm\CCDa4SgdIhwe3Cqb4L5cIF1cW:w NWHiU5ZvOjJ|M{mzOFI>
A431 MkHoT4lv[XOnIFHzd4F6 M17iTVExOCEQvF2= NGHhNZg{OCCvaX6= NFPsbHRKdmirYnn0bY9vKG:oIFXHSnIh\GW{aY\l[EBnem:vIHj1cYFvKEF2M{GgZ4VtdCCvZX3idoFv\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHCxbImtS4x2NVS7cjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFEvODhizszN MmT6NlI3QTh5OEK=
H460 NI\iUoJEgXSxdH;4bYMhSXO|YYm= NH:w[WM4OiCq MXjJR|UxRTVwNUmg{txO Mn\uNlI4Ojd2NEm=
HT-29 NGTVd3hEgXSxdH;4bYMhSXO|YYm= MnHMO|IhcA>? NVHnSmRrUUN3ME2zMlM3KM7:TR?= NXzMTlBpOjJ5Mke0OFk>
SGC7901 MoW0R5l1d3SxeHnjJGF{e2G7 M3XvfVczKGh? MnnxTWM2OD1zMD6yOkDPxE1? NULKXFUxOjJ5Mke0OFk>
A498 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvBUVhySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIV5eHKnc4PpcochTUeIUjDhcoQhW1KFIIfpeIghUUN3MDDv[kA5NjZizszN M3vzOVIzQDF6OES4
Calu3 NVfy[W1US3m2b4TvfIlkKEG|c3H5 Mk\0NVAh|rypL33M NYXIe5o1PzJiaB?= M3PQVWlEPTB;MT62JO69VQ>? NEPVW4kzOzFzNkG2PC=>
FADU M4LwfGN6fG:2b4jpZ{BCe3OjeR?= M4PWTFExKM7:Zz;tUC=> M4TySlczKGh? MWfJR|UxRTBwMEWg{txO M37QXlI{OTF4MU[4
HCC827 NIn6[Y9EgXSxdH;4bYMhSXO|YYm= M2\hdVExKM7:Zz;tUC=> MoDtO|IhcA>? NVztfoxTUUN3ME2wMlAxOTVizszN MWiyN|EyPjF4OB?=
PC9 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTVNVAh|rypL33M Mn65O|IhcA>? MmjjTWM2OD1yLkCxOEDPxE1? NIrG[lMzOzFzNkG2PC=>
Sf9 MmX2T4lv[XOnIFHzd4F6 MXyxJIg> M{H4OWROW09? M4eweWlvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLYTh[4dm\CCHR1\SJGw5OzSUIH31eIFvfCCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFAvODF3IN88US=> MnSyNlM3OTF4OUG=
16HBE14o- M2PHcmN6fG:2b4jpZ{BCe3OjeR?= MUexNEDPxE1? MnzWO|IhcA>? NFTXV3dFVVOR MlHlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNVZJSkVzNH:tJINmdGy|IHjhdoJwemmwZzD3bYxlKHS7cHWgSWdHWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOTJwN{Gg{txO NGDLTJAzOzZ4OES0NS=>
NCI-H1975 MXPDfZRwfG:6aXOgRZN{[Xl? NWnG[4JCOTBizszN MnHRO|IhcA>? NWLZWYFLTE2VTx?= MlHuR5l1d3SxeHnjbZR6KGGpYXnud5Qh\2WoaYTpcoljNXKnc3nzeIFvfCCqdX3hckBPS0lvSEG5O|Uh[2WubIOgbIFz[m:{aX7nJGVITlJiTEi1PHIwXDd7MF2g[I92[mynIH31eIFvfCCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhPi57MUeg{txO MY[yN|Y3QDR2MR?=
16HBE NUDa[IZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXkNVY4OiCq MVHEUXNQ NG\T[JNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEG2TGJGKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWJRmKge4l1cCCLQ{WwJI9nKDFwNkCxJO69VQ>? Mm\CNlM4QTJ|MUi=
16HBE NWj0R5ZGTnWwY4Tpc44hSXO|YYm= MWWxNFAh|ryP NV6zemRyOTVyIH3pci=> MX3EUXNQ Mkf4TY5lfWO2aX;uJI9nKG6rdILpZ{BwgGmmZTDwdo9lfWO2aX;uJIlvKGi3bXHuJFE3UEKHIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXHSnI> NUXmWpYxOjN5OUKzNVg>
A549 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYS3NkBp NInlWINFVVOR MorqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDD3bYxlKHS7cHWgSWdHWi:tLWLhd{Bl\XCnbnTlcpQhcHWvYX6gRVU1QSClZXzsd{B4cXSqIFnDOVAhd2ZiND62NlYh|ryP M4O2fFI{Pzl{M{G4
SH-SY5Y M1vFOWN6fG:2b4jpZ{BCe3OjeR?= NXzQZmg6PzJiaB?= NWPsdpNPUUN3ME2xPE4zOSEQvF2= MVqyN|g4OTlyOR?=
LoVo M{nMfGtqdmG|ZTDBd5NigQ>? NG\GNWQzKCCq Mn[5SG1UVw>? MVfJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB4MjFOwG0> M1\nXlI{QTNyOUm0
PC9 NUfZeZQ4U2mwYYPlJGF{e2G7 M4L5fVIhcA>? M4fLfmROW09? NWX0PG1JUW6qaXLpeIlwdiCxZjDFS2ZTKGW6b36gNVkh\GWuZYTpc44h[WO2aY\heIlv\yCvdYThcpQheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHBEQSClZXzsd{B4cXSqIFnDOVAhd2ZiMD6wNFg4KM7:TR?= NHzzPIMzOzl|MEm5OC=>
HCC827 NXHwbYVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH65[WI4OiCq NGfrenpKSzVyPUCuNFEzKM7:TR?= NH7kc|YzOzl5M{G2PC=>
A549 Mn7yT4lv[XOnIFHzd4F6 MVKxJO69VQ>? NGX2UpQyKGh? M{j0W2ROW09? M2HxcWlvcGmkaYTpc44hd2ZiRVfGVkBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlA{QTlizszN M3fJ[|I{QTh6M{W0
A549 M3KxTGZ2dmO2aX;uJGF{e2G7 M{P0N|Eh|ryP NVeyUFdROSCq NU\xZ4d{TE2VTx?= NX[1eGwzS2WubIXsZZIhfXC2YXvl MUmyN|k5QDN3NB?=
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KYSE-180 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\PVppKSzVyPUWzNE43OiCwTR?= M{\GRXNCVkeHUh?=
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NCI-H1770 NInLbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\qOWlEPTB;N{KyMlQhdk1? MXrTRW5ITVJ?
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DEL Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Hq[mlEPTB;OEe3MlY2KG6P NFr3cFRUSU6JRWK=
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NCI-H1648 MofaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLuUGJGUUN3ME2xMlExPjF4IN88US=> MkW2V2FPT0WU
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CTV-1 NV3PbGhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPyTWM2OD1zLkOwPEDPxE1? MU\TRW5ITVJ?
NCI-H1092 NH\JbY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFwM{C4OUDPxE1? MlHCV2FPT0WU
NKM-1 MmP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jGU2lEPTB;MT6zNlU6PyEQvF2= NGH5bWFUSU6JRWK=
NCI-H1650 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP1TWM2OD1zLkOzOFgzKM7:TR?= NGTpTHhUSU6JRWK=
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RH-1 NGCyVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Lu[mlEPTB;MT60NVE{PiEQvF2= MmDtV2FPT0WU
NCI-H526 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwNEO4NlYh|ryP NEHVVmFUSU6JRWK=
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COLO-678 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwN{O0OFQh|ryP NXXDO4RNW0GQR1XS
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EPLC-272H NVXibZYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrITWM2OD1zLki1OVQ6KM7:TR?= MYPTRW5ITVJ?
OMC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fVZWlEPTB;MT65PVg5QCEQvF2= MWXTRW5ITVJ?
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CAL-12T NFK5PHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUW5[4hHUUN3ME2yMlAyQDZzIN88US=> NVThc4VVW0GQR1XS
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NCI-H2009 NX\BZmNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\kTWM2OD1{LkC2NlE1KM7:TR?= MV3TRW5ITVJ?
RPMI-8866 NW\6PWp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVSwR5hnUUN3ME2yMlA5PDhzIN88US=> NYO0UIFsW0GQR1XS
KARPAS-45 MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXlUFFKSzVyPUKuNVI1PzlizszN NH3Z[pBUSU6JRWK=
RXF393 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO0TWM2OD1{LkGzNFM3KM7:TR?= MY\TRW5ITVJ?
786-0 NIS5WVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPDTWM2OD1{LkG4OFA3KM7:TR?= MUPTRW5ITVJ?
SCC-4 NIHXd4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjoNHZ[UUN3ME2yMlIyPzd4IN88US=> MkO5V2FPT0WU
BT-20 MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2eyZWlEPTB;Mj6yOlc1PCEQvF2= MYHTRW5ITVJ?
A498 NEHBdo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJwMkm0NVUh|ryP NYG2U4FwW0GQR1XS
IGROV-1 NXziRoRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjjTWM2OD1{LkOxNlM4KM7:TR?= MorpV2FPT0WU
JVM-3 Mn34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\CTWM2OD1{LkO0OlQ{KM7:TR?= NWDHZoRZW0GQR1XS
NCI-H2170 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWX3UJdbUUN3ME2yMlM1Pzh|IN88US=> NHm2[FNUSU6JRWK=
EW-18 NFXrcWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\vU4pVUUN3ME2yMlM2PDdzIN88US=> NF;iVFVUSU6JRWK=
KU812 NUnJeYUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX0OlJGUUN3ME2yMlM3Pzd7IN88US=> M370ZXNCVkeHUh?=
NY NWDuW2szT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7obZN2UUN3ME2yMlM4OjdizszN NV;4S2xFW0GQR1XS
HTC-C3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zkZmlEPTB;Mj60NlI3PyEQvF2= M{C2OXNCVkeHUh?=
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HH NVizSVVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qySmlEPTB;Mj60PVg2PCEQvF2= MXLTRW5ITVJ?
MKN7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJwNkK3OFgh|ryP NVS1Tm5JW0GQR1XS
TE-8 M1TBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnUVYlTUUN3ME2yMlY{PjV|IN88US=> M4PvcHNCVkeHUh?=
MC-IXC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHZTWM2OD1{Lk[0OFU{KM7:TR?= NVLUdZZFW0GQR1XS
DMS-79 MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe5eZNKSzVyPUKuOlkzQDRizszN MoP1V2FPT0WU
Detroit562 M3zWcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe0cpZKSzVyPUKuOlk5PDVizszN MXfTRW5ITVJ?
HuP-T4 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{SwdmlEPTB;Mj63NlgyQCEQvF2= M{[xfHNCVkeHUh?=
QIMR-WIL NXfO[GMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnDXIZPUUN3ME2yMlc2QTV{IN88US=> Mne2V2FPT0WU
BB65-RCC NELxXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;nbI5KSzVyPUKuPFA4OTNizszN NWHMZ3FuW0GQR1XS
PC-3 NVLxVoZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnT6TWM2OD1{LkizN|E4KM7:TR?= NYLm[mhlW0GQR1XS
OVCAR-3 NWWxU4tkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki0TWM2OD1{Lki1OVk1KM7:TR?= NHS1T5FUSU6JRWK=
KYSE-510 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJwOE[3PFYh|ryP NGfsSG9USU6JRWK=
HC-1 M2jVXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDpbXE6UUN3ME2yMlk1ODF{IN88US=> MlmxV2FPT0WU
NCI-H1693 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO5bGZKSzVyPUKuPVU5QTdizszN NFnDPVJUSU6JRWK=
DU-4475 MmnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3tTWM2OD1{Lkm5NFUzKM7:TR?= MXnTRW5ITVJ?
COLO-680N NFTifFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTNwMEC0PVUh|ryP NGnV[ZFUSU6JRWK=
MN-60 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTNwMES5O|Qh|ryP M1fSSHNCVkeHUh?=
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NCI-H2052 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3xTWM2OD12NT65NFI4KM7:TR?= MVHTRW5ITVJ?
SW684 NVr4dFl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1i1PGlEPTB;NEeuNFA5OSEQvF2= Mn3hV2FPT0WU
HCC1569 NW\1fpNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTR5LkG2OVgh|ryP NHX1S|NUSU6JRWK=
KGN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTR5LkOzNVEh|ryP M4PLPHNCVkeHUh?=
LCLC-103H M2HpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfITWM2OD12Nz60OFA1KM7:TR?= MlHXV2FPT0WU
SW780 NWq5e|hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR5Lk[zOVEh|ryP NWTC[Ih7W0GQR1XS
NCI-H1703 NYOwcJNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLQTWM2OD12OD6zN|UzKM7:TR?= M4XTUHNCVkeHUh?=
HCC1395 M1y3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVmzbZNlUUN3ME20PE44PDN{IN88US=> M1TrOXNCVkeHUh?=

... 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.
  • 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)
Water Insoluble
Ethanol ''4 mg/mL
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(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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)

  • Mass
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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 )

  • C1
    V1
    C2
    V2

* 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

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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