Gefitinib (ZD1839)

For research use only.

Catalog No.S1025

348 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 348 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 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3jeVJKSzVyPUCuNFU1KM7:TR?= NH;3dHcyPjVzNkS3Ny=>
NIH3T3 NGiz[4JHfW6ldHnvckBCe3OjeR?= MWCwMlIh|ryP M1rQWVIhcA>? NV\HTItjTE2VTx?= M4DocGlvcGmkaYTpc44hd2ZiRVfGJJN1cW23bHH0[YQhcHWvYX6g[ZJjSjFiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMUS0JO69VQ>? NVvJWZczOTZ2OECyPFQ>
COS7 MoXXSpVv[3Srb36gRZN{[Xl? MoLOPVYh|ryP NX3Pb2lCUW6qaXLpeIlwdiCxZjDoeY1idiCMQVuyJHY3OTeIIH31eIFvfCCneIDy[ZN{\WR? Ml61NVcyPzh5MkK=
A549 NHz5[|JEgXSxdH;4bYMhSXO|YYm= NVjNdmpnQTZiaB?= MX3EUXNQ M3TKS2lEPTB;MUOuOVkh|ryP NGDMPIsyQDNzM{iwOy=>
K562 MWHDfZRwfG:6aXOgRZN{[Xl? M{nFdlk3KGh? MXrEUXNQ MXTJR|UxRTlwM{[g{txO NULQelNoOTh|MUO4NFc>
MDA-MB-231 MV3DfZRwfG:6aXOgRZN{[Xl? NXXoOY1qQTZiaB?= MXLEUXNQ MoX3TWM2OD1|Nj62NUDPxE1? MnzvNVg{OTN6MEe=
MOLT4 NFrGbppEgXSxdH;4bYMhSXO|YYm= NX3pRldDQTZiaB?= MWDEUXNQ NVnvdYpkUUN3ME2xOU4xOiEQvF2= MnnSNVg{OTN6MEe=
MCF7 NGHNNYZEgXSxdH;4bYMhSXO|YYm= M3i2[VUxKM7:TR?= NEi5Smc4OiCq MnvyTWM2OD1zMj6wOUDPxE1? NX[3Ro9wOTh5N{G4NVk>
BT474 M{PUTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu3NkBp M2nHWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS0O|Qh[2WubIOgc5ZmemW6cILld5NqdmdiRWLCZlIhf2m2aDDFR|UxKG:oIECuN{DPxE1? NFLa[mIyQTB{OESyOC=>
HN5 NFvaRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfheldrPzJiaB?= NInMSotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuczDveoVz\XiycnXzd4lv\yCHR1\SJJdqfGhiRVO1NEBw\iByLkCxJO69VQ>? NEn4UIEyQTB{OESyOC=>
BA/F3 NGXPc5VEgXSxdH;4bYMhSXO|YYm= MYC3NkBp NGDpSYxEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62IIfpeIghUUN3MDDv[kAxNjBzMEig{txO MWSxPVI{QTJ{OR?=
NIH3T3 M3rWPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj5T4FxPzJiaB?= NEK0WXVIem:5dHigbY5pcWKrdHnvckBw\iCvb4Xz[UBPUUhxM2SzJINmdGy|IHX4dJJme3Orbneg[ZJDOiCpZX7lJJdqfGhiSVO1NEBw\iByLkW0JO69VQ>? MUKxPVY3PTN5Nx?=
MCF7 MX NYqxWHYyTnWwY4Tpc44hSXO|YYm= M1;kb|MxKG2rbh?= MYDJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iBzLkGg{txO MnPwNVk6OzJ7NkC=
A431 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNEDPxE1? MV:3NkBp NF:0UoNIUTVyPUCuOVE1KM7:TR?= NEXT[GsyQTl4OUS2OS=>
A431 M3X6VWtqdmG|ZTDBd5NigQ>? MUewMlEh|ryP MknPNUBp Mnj5TY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvci=> NXK0eotrOTl7Nkm0OlU>
A431 M4XndGtqdmG|ZTDBd5NigQ>? M3T4UFExOCEQvF2= NW\OZVE1OTBibXnu Mn\SVJJwdG:wZ3XkJIlvcGmkaYTvdpkh[WO2aY\peJkhd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44> NVTlRWxqOTl7Nkm0OlU>
Sf9 M1vOS2tqdmG|ZTDBd5NigQ>? M{nNVVExKG2rbh?= MlfjSG1UVw>? NFTUblNKdmirYnn0bY9vKG:oIFXHSnIh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemWlZYD0c5Ih[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOzNizszN NVO1VIJ3OjByNU[0NlU>
NCI-H1975 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy1JO69VQ>? MVy3NkBp MmnqTWM2OD16LkK2JO69VQ>? M{LxcFIxOTVzNkew
NCI-H1975 MXPLbY5ie2ViQYPzZZk> NIfyfmEyOCEQvF2= NUXydohHUW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25? MkniNlAyPTF4N{C=
NCI-H1975 M3TrSmZ2dmO2aX;uJGF{e2G7 Mlq3NVAh|ryP M4L2UGlvcGmkaYTpc44hd2ZiRWLCRlIh[XW2b4Doc5NxcG:{eXzheIlwdg>? Mn3hNlAyPTF4N{C=
NCI-H1975 MmXWSpVv[3Srb36gRZN{[Xl? NI\GeoY2KM7:TR?= NW\X[G81PDhiaB?= MVfJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGG|c3Xzd4VlKGG|IHHjeIl3[XSrb36gc4Yh[2G|cHHz[U0{ MV:yNFE2OTZ5MB?=
A375 NYPlUZMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoizOFghcA>? NXK3[Y9VUUN3ME2yNE42PSEQvF2= MkTTNlA{ODR3M{e=
SMMC7721 NH3VSnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYq0PEBp M2DNNWlEPTB;M{OuNVIh|ryP M3r6[|IxOzB2NUO3
DU145 M4HvTmN6fG:2b4jpZ{BCe3OjeR?= NYTLb|RJPSCm M1PQOWROW09? NXPwUGJRUUN3ME20Nk4yPyEQvF2= MX2yNFQ3PjV3NR?=
MIAPaCa2 M17MU2N6fG:2b4jpZ{BCe3OjeR?= MmnIOUBl NXTr[5ZzTE2VTx?= NYixUFd5UUN3ME21NE43OiEQvF2= NUD2VIRTOjB2Nk[1OVU>
PANC1 NYXTcm06S3m2b4TvfIlkKEG|c3H5 MYe1JIQ> MUDEUXNQ M2rycGlEPTB;NECuOFIh|ryP MmPtNlA1PjZ3NUW=
PC9 NIT5RZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TrVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSWdHWi2mZX\pZ4lmdnRiaIXtZY4hWEN7IHPlcIx{KHerdHigSWM2OCCxZjCwMlAyPyEQvF2= MlXBNlEzODh6MEK=
PC9 M2[yVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jMSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sg[5Jwf3SqLYLld4l{fGGwdDDoeY1idiCSQ{mgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEV5NE\fRVc2OC:WN{mwUUBufXSjboSge4l1cCCHQ{WwJI9nKDdizszN MlzQNlEzODh6MEK=
PC3 M37KbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNEDPxE1? NXzRSmcxPzJiaB?= MnP3SG1UVw>? Ml3uTWM2OD15LkSg{txO MVuyNVM2OzV2Nh?=
MDA-MB-468 NG\ySIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PV[|ExOCEQvF2= MX:0PEBp NYDweHdpTE2VTx?= NIf2fodCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fS=> Mme5NlE1Ojl4M{K=
Plasmodium falciparum MUXxTHRUKHC{b3\pcIlv\yCob4KgbY5pcWKrdH;yd{Bw\iCSbHHzcY9lcXWvIH\hcINqeGG{dX2gdJJwdGmoZYLheIlwdg>? NFvF[YEzOThzN{C0OS=>
NCI-H1993 NFuydmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfmVGhLPzJiaB?= MUnEUXNQ M{TEXmlEPTB;MD6xJO69VQ>? M1vqNVIyQTF4NEOz
NCI-H292 M4q3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW5O|IhcA>? MnfaSG1UVw>? NI\3NllKSzVyPUCuNFIh|ryP MlexNlE6OTZ2M{O=
A431 NXrHOGxCU2mwYYPlJGF{e2G7 MUSyJIg> M1ixRWROW09? NIDreYlKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIFG0N|Ehf2m2aDDJR|UxKG:oIECuNFAyKM7:TR?= NWLldHZDOjJzMEGxN|I>
MCF7 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H6d|ExOMLizsznM41N NWqzc|BOPDhiaB?= MVvEUXNQ MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDn[Y5mKHerdHigTWM2OCCxZjCxNk4xPSEQvF2= MYCyNlEyQTF|MB?=
BT474 M2TENmN6fG:2b4jpZ{BCe3OjeR?= NXr4XowxOTBizszN M1fCb|Q5KGh? MWfDfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKEKWNEe0JINmdGy| MUiyNlE{QDNyOB?=
MCF7 MUXDfZRwfG:6aXOgRZN{[Xl? MmHsNVAh|ryP MkDWOFghcA>? MYDDfZRwfG:6aXPpeJkh[WejaX7zeEB{\XK3bT3zeIFzfmWmIHj1cYFvKE2FRkegZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEW{YlKyJINmdGy| NGXlS5YzOjF|OEOwPC=>
HCC827 MWfLbY5ie2ViQYPzZZk> MXWwMlEzPSEQvF2= M3PzWlI1KGh? MkjQSG1UVw>? NIXrcYJKdmirYnn0bY9vKG:oIFXHSnIh\GWuIFW3OFYuSTd3MDDteZRidnRiWUGwOlgh[XW2b4Doc5NxcG:{eXzheIlwdg>? Mli4NlI{Ozl|NEK=
HCC827 MoCwT4lv[XOnIFHzd4F6 M3TQe|AvOTJ3IN88US=> NY\SO2s{OjRiaB?= M{HSSGROW09? M2fEU2lvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfC2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:w MWiyNlM{QTN2Mh?=
HCC827 NI\0Zo1McW6jc3WgRZN{[Xl? NFr2RpUxNjF{NTFOwG0> MmTlNlQhcA>? M4LDOGROW09? M2rtRWlvcGmkaYTpc44hd2ZiRVfGVkBl\WxiRUe0Ok1CPzVyIH31eIFvfC2vZXTpZZRm\CCDa4SgdIhwe3Cqb4L5cIF1cW:w MVGyNlM{QTN2Mh?=
A431 MXfLbY5ie2ViQYPzZZk> MmT5NVAxKM7:TR?= MmTMN|AhdWmw M{TodGlvcGmkaYTpc44hd2ZiRVfGVkBl\XKrdnXkJIZzd21iaIXtZY4hSTR|MTDj[YxtKG2nbXLyZY5mKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheG:ueT3HcJUuXHm{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNU4xQCEQvF2= NH6wbXQzOjZ7OEe4Ni=>
H460 MV;DfZRwfG:6aXOgRZN{[Xl? NXvNPIRRPzJiaB?= MUDJR|UxRTVwNUmg{txO MoHnNlI4Ojd2NEm=
HT-29 M{\ZSmN6fG:2b4jpZ{BCe3OjeR?= NGX1RWY4OiCq M4G4b2lEPTB;Mz6zOkDPxE1? NEjaRVYzOjd{N{S0PS=>
SGC7901 M3LENGN6fG:2b4jpZ{BCe3OjeR?= MkS0O|IhcA>? NVXLeZFRUUN3ME2xNE4zPiEQvF2= NUWyWIR{OjJ5Mke0OFk>
A498 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfTVZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOg[ZhxemW|c3nu[{BGT0[UIHHu[EBUWkNid3n0bEBKSzVyIH;mJFgvPiEQvF2= M{TxT|IzQDF6OES4
Calu3 MWjDfZRwfG:6aXOgRZN{[Xl? NWDlPVFsOTBizsznM41N M1vQcFczKGh? M13DSmlEPTB;MT62JO69VQ>? MYmyN|EyPjF4OB?=
FADU NIP1fmtEgXSxdH;4bYMhSXO|YYm= Ml\UNVAh|rypL33M M1HUOVczKGh? M{\QbmlEPTB;MD6wOUDPxE1? MXeyN|EyPjF4OB?=
HCC827 MUTDfZRwfG:6aXOgRZN{[Xl? MX[xNEDPxGdxbVy= MY[3NkBp MmfXTWM2OD1yLkCwNVUh|ryP NEXZUm8zOzFzNkG2PC=>
PC9 NEjKOYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3wUmw2OTBizsznM41N MlfCO|IhcA>? NGf4XINKSzVyPUCuNFE1KM7:TR?= NHPz[HIzOzFzNkG2PC=>
Sf9 MnLnT4lv[XOnIFHzd4F6 NUjJWI5ZOSCq M3[yTmROW09? NHrMOJVKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD30ZYdo\WRiRVfGVkBNQDN2UjDteZRidnRiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> M3fOeVI{PjFzNkmx
16HBE14o- MkTsR5l1d3SxeHnjJGF{e2G7 MnL6NVAh|ryP MlXhO|IhcA>? MmnMSG1UVw>? MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxOmhDTTF2bz2gZ4VtdHNiaHHyZo9zcW6pIIfpcIQhfHmyZTDFS2ZTKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAyOi55MTFOwG0> MkPWNlM3Pjh2NEG=
NCI-H1975 NWfGWodOS3m2b4TvfIlkKEG|c3H5 MV:xNEDPxE1? MkToO|IhcA>? MlzqSG1UVw>? MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBo\W[rdHnubYIuemW|aYP0ZY51KGi3bXHuJG5EUS2KMUm3OUBk\WyuczDoZZJjd3KrbnegSWdHWiCOOEW4Vk9VPzlyTTDkc5VjdGVibYX0ZY51KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kA3NjlzNzFOwG0> NIDlSJkzOzZ4OES0NS=>
16HBE Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp MlXtSG1UVw>? Mn;oRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiBzNljCSUBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBGT0[UIIfpeIghUUN3MDDv[kAyNjZyMTFOwG0> M3nFU|I{Pzl{M{G4
16HBE NHrFZ2hHfW6ldHnvckBCe3OjeR?= MorVNVAxKM7:TR?= MVmxOVAhdWmw MWfEUXNQ MlWwTY5lfWO2aX;uJI9nKG6rdILpZ{BwgGmmZTDwdo9lfWO2aX;uJIlvKGi3bXHuJFE3UEKHIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXHSnI> MkPNNlM4QTJ|MUi=
A549 MoXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXwZWN5PzJiaB?= MoWxSG1UVw>? NVvFW4l5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEB4cWymIIT5dIUhTUeIUj;rMXJieyCmZYDlcoRmdnRiaIXtZY4hSTV2OTDj[YxteyC5aYToJGlEPTBib3[gOE43OjZizszN MlHjNlM4QTJ|MUi=
SH-SY5Y M3e4OmN6fG:2b4jpZ{BCe3OjeR?= MVS3NkBp MnjMTWM2OD1zOD6yNUDPxE1? NH3YN4QzOzh5MUmwPS=>
LoVo NIj4S3ZMcW6jc3WgRZN{[Xl? MWqyJEBp MlPFSG1UVw>? M2j0dmlvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwME[yJO69VQ>? MkL4NlM6OzB7OUS=
PC9 M4jkbmtqdmG|ZTDBd5NigQ>? NXTne4M{OiCq NXjUcpY5TE2VTx?= NEDvRo9KdmirYnn0bY9vKG:oIFXHSnIh\XixbjCxPUBl\WyndHnvckBi[3SrdnH0bY5oKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gVGM6KGOnbHzzJJdqfGhiSVO1NEBw\iByLkCwPFch|ryP NXXn[5FWOjN7M{C5PVQ>
HCC827 M4PIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHacJM4OiCq MknyTWM2OD1yLkCxNkDPxE1? M33Hd|I{QTd|MU[4
A549 NYrqUWt3U2mwYYPlJGF{e2G7 MlzkNUDPxE1? NUfRdJRIOSCq NFXP[m1FVVOR Mn76TY5pcWKrdHnvckBw\iCHR1\SJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFM6QSEQvF2= NVLLdWpLOjN7OEizOVQ>
A549 MY\GeY5kfGmxbjDBd5NigQ>? M1vXN|Eh|ryP NGrScHcyKGh? NWTydolDTE2VTx?= NWD3W49ZS2WubIXsZZIhfXC2YXvl M4DFSVI{QTh6M{W0
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HN NF3BNoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13QUGlEPTB;NUG3MlM5KG6P MV;TRW5ITVJ?
SCC-15 NXPJXId5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTV{NT62PEBvVQ>? M124[3NCVkeHUh?=
NCI-H358 MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LWRWlEPTB;NUK3MlY3KG6P MkK4V2FPT0WU
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NCI-H82 NXvPVWdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTV2MD61JI5O NV[yTHNtW0GQR1XS
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Ca9-22 NH;se5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTV6OD62OEBvVQ>? M3zxS3NCVkeHUh?=
CAL-39 NH7Z[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXYOIxKSzVyPUW5Ok4{KG6P Mn3MV2FPT0WU
NCI-H1623 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyzTWM2OD13OUmuN|Yhdk1? MlvXV2FPT0WU
FADU MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfOW4FKSzVyPU[wOE43QSCwTR?= MXHTRW5ITVJ?
NB69 NIf2eVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\FTWM2OD14MUSuN|Uhdk1? MoDJV2FPT0WU
Ramos-2G6-4C10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkntTWM2OD14MkGuOFYhdk1? M{m3NXNCVkeHUh?=
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MV-4-11 NXz2U2hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\KTWM2OD14MkeuO{BvVQ>? NVvpOmRtW0GQR1XS
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ETK-1 M3PjVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHIcHhQUUN3ME22OlIvPTlibl2= NIPmS2lUSU6JRWK=
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LU-134-A NEf0XoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[1TWM2OD15MUmuNFkhdk1? NWHUV4N3W0GQR1XS
NCI-H1770 NUXObnR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHXTWM2OD15MkKuOEBvVQ>? NYP5eW5yW0GQR1XS
HAL-01 NXi4OW53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP0TWM2OD15M{SuO|Ehdk1? NGqyfWpUSU6JRWK=
COLO-684 NWj5SmlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvBdppKSzVyPUe1N{4xOSCwTR?= M2O5XnNCVkeHUh?=
TE-6 NYnDUmJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTkfIJZUUN3ME23OlQvOzFibl2= MlXPV2FPT0WU
A431 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHoT3lQUUN3ME23PFAvODRibl2= NILuPWxUSU6JRWK=
LU-135 NHnPdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTd6Mz6wN{BvVQ>? M{eydHNCVkeHUh?=
EC-GI-10 NFTzcoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTd6OD61NkBvVQ>? M2Tr[HNCVkeHUh?=
TE-12 NHz1PZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvMd3ZXUUN3ME24NlEvOTFibl2= NH7BR|FUSU6JRWK=
LoVo M1S3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXQPVVXUUN3ME24OVkvODZibl2= NYn4XVFyW0GQR1XS
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AU565 MoXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\i[mlEPTB;OE[5MlYhdk1? MlvSV2FPT0WU
DEL M4TTeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPPTWM2OD16N{euOlUhdk1? MmH6V2FPT0WU
COR-L88 NVfTU3VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfPNpNKSzVyPUi4Nk4zPiCwTR?= MVzTRW5ITVJ?
NCI-H2126 NWjweFZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTh6Mj64N{BvVQ>? NHXHVmpUSU6JRWK=
CAPAN-1 NEHSTJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\OW2lEPTB;OEizMlI6KG6P MWHTRW5ITVJ?
BT-474 M{LiPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXzTWM2OD17M{iuNVQhdk1? MU\TRW5ITVJ?
BHY NHmxNIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjTWmFKUUN3ME25O|UvPDhibl2= NFjVSXhUSU6JRWK=
HT-3 NUTKVmVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTl6Mj60NUBvVQ>? MUfTRW5ITVJ?
SK-NEP-1 M1rMTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fSbWlEPTB;OUi5MlQ1KG6P MU\TRW5ITVJ?
MS-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\PT2lEPTB;OUm0MlY6KG6P MUHTRW5ITVJ?
DOHH-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fDZmlEPTB;MT6wNFAzOSEQvF2= M4G2TXNCVkeHUh?=
NCI-H1304 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXuTWM2OD1zLkCxOlQ{KM7:TR?= MW\TRW5ITVJ?
EM-2 MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\hS2lEPTB;MT6wN|AyPiEQvF2= NITYZ2RUSU6JRWK=
MHH-PREB-1 M4TKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;ETWM2OD1zLkC4OFUyKM7:TR?= NVLVfWNiW0GQR1XS
KU-19-19 MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfJcXVQUUN3ME2xMlA5PTRzIN88US=> MWPTRW5ITVJ?
NCI-H1648 M3nibGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP6R29IUUN3ME2xMlExPjF4IN88US=> MX7TRW5ITVJ?
MKN1 M3ruPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLreHVKSzVyPUGuNlE6QDdizszN NEPnUGFUSU6JRWK=
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OAW-42 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzjTWM2OD1zLkK3PFI2KM7:TR?= NH\V[3hUSU6JRWK=
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SW1088 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHsNFBKSzVyPUGuNlk3ODdizszN MW\TRW5ITVJ?
GCIY NIi4NJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn3cYwyUUN3ME2xMlMxOTN{IN88US=> M2\NRXNCVkeHUh?=
CTV-1 NH3wVVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrXTWM2OD1zLkOwPEDPxE1? NFy2VllUSU6JRWK=
NCI-H1092 MlrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2yRnZKSzVyPUGuN|A5PSEQvF2= MUnTRW5ITVJ?
NKM-1 NVHBSVRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFwM{K1PVch|ryP NXK0OYZnW0GQR1XS
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SW954 M4jRcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3WXHNlUUN3ME2xMlM1ODR6IN88US=> NHzKfGNUSU6JRWK=
SW48 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwM{[2NVgh|ryP MXrTRW5ITVJ?
SK-N-DZ M2\pZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TkR2lEPTB;MT6zOlk1PyEQvF2= M1j2[nNCVkeHUh?=
KMOE-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nHWmlEPTB;MT6zPVgyPSEQvF2= MYHTRW5ITVJ?
NB5 M2DuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fhZmlEPTB;MT60NFg6PCEQvF2= MY\TRW5ITVJ?
CCRF-CEM MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC2Z2pCUUN3ME2xMlQyOTFizszN NI\aVHlUSU6JRWK=
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NCI-H526 NWP3T2Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vQS2lEPTB;MT60N|gzPiEQvF2= NG\Kbm5USU6JRWK=
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J82 MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVyxXXZlUUN3ME2xMlQ2PzZ4IN88US=> MYPTRW5ITVJ?
BE-13 NXXROG9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\OWWlEPTB;MT61NFY4OSEQvF2= M{jwWnNCVkeHUh?=
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SCC-25 NYrPUnJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzSOppzUUN3ME2xMlUzOzJ{IN88US=> NXXvbHUxW0GQR1XS
LAMA-84 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPaTJNKSzVyPUGuOVM5OTVizszN MWXTRW5ITVJ?
HSC-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHyVppKSzVyPUGuOVQ{QCEQvF2= MmXCV2FPT0WU
BT-549 M3PEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHuTWM2OD1zLkW4O|Q4KM7:TR?= NIqySGxUSU6JRWK=
ML-2 NVv5VItUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwNkSwNlkh|ryP NGDlWINUSU6JRWK=
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PANC-03-27 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j1PWlEPTB;MT63NFE{QSEQvF2= MVPTRW5ITVJ?
COLO-678 MmP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PaeGlEPTB;MT63N|Q1PCEQvF2= MUDTRW5ITVJ?
NCI-H1666 NVK3O2U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPifJN3UUN3ME2xMlc1PzB2IN88US=> MYnTRW5ITVJ?
NCI-H209 NXjrT4VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDtTWM2OD1zLke3NlY6KM7:TR?= MXLTRW5ITVJ?
EPLC-272H NUfqdop{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTqTWM2OD1zLki1OVQ6KM7:TR?= M3jMdHNCVkeHUh?=
OMC-1 M{\IUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nYeWlEPTB;MT65PVg5QCEQvF2= M3HUdHNCVkeHUh?=
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CAL-12T M37WRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJwMEG4OlEh|ryP MmnGV2FPT0WU
TGBC24TKB NETu[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;qVGlEPTB;Mj6wNlk3OSEQvF2= NEL3e3pUSU6JRWK=
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SW1116 MkG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm5PZNCUUN3ME2yMlA3ODB7IN88US=> MV3TRW5ITVJ?
NCI-H2009 NVi3O5VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjRfW1MUUN3ME2yMlA3OjF2IN88US=> NHjJbpVUSU6JRWK=
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KARPAS-45 NWTxcIZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrKfnZiUUN3ME2yMlEzPDd7IN88US=> NWfr[Hg4W0GQR1XS
RXF393 MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjVN4xKSzVyPUKuNVMxOzZizszN MXjTRW5ITVJ?
786-0 NFracZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUSy[2Y{UUN3ME2yMlE5PDB4IN88US=> NWH2cnZHW0GQR1XS
SCC-4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDBRW42UUN3ME2yMlIyPzd4IN88US=> MX;TRW5ITVJ?
BT-20 NWfES2dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfWN|RUUUN3ME2yMlI3PzR2IN88US=> MlrEV2FPT0WU
A498 NIHkPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTVT5RRUUN3ME2yMlI6PDF3IN88US=> NWH2e48{W0GQR1XS
IGROV-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfKUml[UUN3ME2yMlMyOjN5IN88US=> MXXTRW5ITVJ?
JVM-3 NI\VcZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjQb|VKSzVyPUKuN|Q3PDNizszN M{LPN3NCVkeHUh?=
NCI-H2170 M3rpW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETSS3hKSzVyPUKuN|Q4QDNizszN NFO4ZYJUSU6JRWK=
EW-18 NGrXVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LPSGlEPTB;Mj6zOVQ4OSEQvF2= NXPtT2wzW0GQR1XS
KU812 NXrNdIJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPsUW5KSzVyPUKuN|Y4PzlizszN Mm\EV2FPT0WU
NY M3vjbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPSUXpKSzVyPUKuN|czPyEQvF2= MVvTRW5ITVJ?
HTC-C3 M4XPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDXcpN[UUN3ME2yMlQzOjZ5IN88US=> Ml;lV2FPT0WU
CFPAC-1 M4D6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITwXnpKSzVyPUKuOFM5PjRizszN MWDTRW5ITVJ?
HH NH;jTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr6TWM2OD1{LkS5PFU1KM7:TR?= MYnTRW5ITVJ?
MKN7 M360eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LTNWlEPTB;Mj62Nlc1QCEQvF2= M12yUHNCVkeHUh?=
TE-8 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[4fmlEPTB;Mj62N|Y2OyEQvF2= MkDwV2FPT0WU
MC-IXC M{TaWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OyVGlEPTB;Mj62OFQ2OyEQvF2= NHHRVJNUSU6JRWK=
DMS-79 MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:zbXRKSzVyPUKuOlkzQDRizszN M2e5OnNCVkeHUh?=
Detroit562 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDZXFlJUUN3ME2yMlY6QDR3IN88US=> M4XDOXNCVkeHUh?=
HuP-T4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LoOmlEPTB;Mj63NlgyQCEQvF2= NWG2V5AxW0GQR1XS
QIMR-WIL NFfhU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnZc3ZFUUN3ME2yMlc2QTV{IN88US=> Mn:0V2FPT0WU
BB65-RCC NVrUdXRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXDTWM2OD1{LkiwO|E{KM7:TR?= MmLQV2FPT0WU
PC-3 MoC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHO3dpZKSzVyPUKuPFM{OTdizszN NXLF[npzW0GQR1XS
OVCAR-3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJwOEW1PVQh|ryP M33CO3NCVkeHUh?=
KYSE-510 NUXyTZh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwOE[3PFYh|ryP NGW5NIxUSU6JRWK=
HC-1 MkjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jtfmlEPTB;Mj65OFAyOiEQvF2= NITYeGVUSU6JRWK=
NCI-H1693 MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJwOUW4PVch|ryP M3LWZ3NCVkeHUh?=
DU-4475 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K1VmlEPTB;Mj65PVA2OiEQvF2= MoPtV2FPT0WU
COLO-680N MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVf5VmgyUUN3ME2zMlAxPDl3IN88US=> NUDaeYFDW0GQR1XS
MN-60 M2\EWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXFdnFKSzVyPUOuNFQ6PzRizszN M3nje3NCVkeHUh?=
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H-EMC-SS NEjwcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR3Lke2PVMh|ryP MYLTRW5ITVJ?
NCI-H2052 NF35RWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\BTWM2OD12NT65NFI4KM7:TR?= MXHTRW5ITVJ?
SW684 NWLBUWJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz6XpJKSzVyPUS3MlAxQDFizszN NW\5Vol5W0GQR1XS
HCC1569 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIT3boVKSzVyPUS3MlE3PThizszN M3LlXXNCVkeHUh?=
KGN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn63TWM2OD12Nz6zN|EyKM7:TR?= M1HWZ3NCVkeHUh?=
LCLC-103H M1PRNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS0[pIzUUN3ME20O{41PDB2IN88US=> M4S3Z3NCVkeHUh?=
SW780 M2npW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVmyXndEUUN3ME20O{43OzVzIN88US=> NV7WW2F6W0GQR1XS
NCI-H1703 NUfQe5NIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zaVWlEPTB;NEiuN|M2OiEQvF2= M2jTN3NCVkeHUh?=
HCC1395 Mn\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTR6Lke0N|Ih|ryP NFHTOHRUSU6JRWK=

... 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)
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

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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