Gefitinib (ZD1839)

Gefitinib (ZD-1839)は一種のEGFR阻害剤で、NR6wtEGFRとNR6Wの細胞中のTyr1173、Tyr992、Tyr1173とTyr992に作用する時のIC50値が37 nM、37nM、26 nMと57 nMにそれぞれ分かれることです。

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Gefitinib (ZD1839) 化学構造
分子量: 446.90

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MSDS

製品説明

  • Compare EGFR Inhibitors
    EGFR製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Gefitinib (ZD-1839)は一種のEGFR阻害剤で、NR6wtEGFRとNR6Wの細胞中のTyr1173、Tyr992、Tyr1173とTyr992に作用する時のIC50値が37 nM、37nM、26 nMと57 nMにそれぞれ分かれることです。
ターゲット Tyr1173 (NR6wtEGFR cells) Tyr992 (NR6wtEGFR cells) Tyr1173 (NR6W cells) Tyr992 (NR6W cells)
IC50 37 nM 37nM 26 nM 57 nM [1]
In vitro試験 Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. [1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. [2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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TK10 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TvSGlEPTB;NUG1MlEyKG6P NH\BNXZUSU6JRWK=
HN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLJTWM2OD13MUeuN|ghdk1? M3q4fHNCVkeHUh?=
SCC-15 M4LrZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVSzRWpvUUN3ME21NlUvPjhibl2= NWjV[olUW0GQR1XS
NCI-H358 NEnkZWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTV{Nz62OkBvVQ>? NXTjdVhXW0GQR1XS
KYSE-180 NGPIPHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rpOWlEPTB;NUOwMlYzKG6P MmOzV2FPT0WU
NCI-H82 NUDFT4pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTV2MD61JI5O MonDV2FPT0WU
NB7 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny0TWM2OD13NE[uN|Ihdk1? Ml\TV2FPT0WU
DSH1 M4nGcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3mTWM2OD13Nk[uPFghdk1? NHfrV3dUSU6JRWK=
RS4-11 NFrucYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH4TWM2OD13NkiuOVkhdk1? M2Kw[nNCVkeHUh?=
CAN Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHZTXVKSzVyPUW4NE44PiCwTR?= M131VXNCVkeHUh?=
Ca9-22 MkXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n5OGlEPTB;NUi4MlY1KG6P Mnm1V2FPT0WU
CAL-39 NVzCbXh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XBfGlEPTB;NUm2MlMhdk1? M{n6UHNCVkeHUh?=
NCI-H1623 MlexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjNS2JHUUN3ME21PVkvOzZibl2= NGXPVVdUSU6JRWK=
FADU M1fiS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTZyND62PUBvVQ>? NV;4OJl2W0GQR1XS
NB69 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;TeWlEPTB;NkG0MlM2KG6P MkToV2FPT0WU
Ramos-2G6-4C10 NIPsfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnEcYF1UUN3ME22NlEvPDZibl2= MojRV2FPT0WU
LB1047-RCC NXfrPIxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorqTWM2OD14MkWuNlkhdk1? NWntPVlIW0GQR1XS
MV-4-11 Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXSSnBKSzVyPU[yO{44KG6P M3zvPXNCVkeHUh?=
DBTRG-05MG NHfUXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL5PVhiUUN3ME22N|IvOjhibl2= Mo\CV2FPT0WU
ME-180 NEjVXWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7oTYFKSzVyPU[zNk46KG6P M3PYNnNCVkeHUh?=
NBsusSR MofRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn32TWM2OD14NE[uOVIhdk1? MkLUV2FPT0WU
COR-L105 Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTZ4Mj61N{BvVQ>? MVfTRW5ITVJ?
ETK-1 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTCNppKSzVyPU[2Nk42QSCwTR?= M{fwUXNCVkeHUh?=
L-363 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;zTWM2OD14N{GuPVQhdk1? MnqzV2FPT0WU
LU-134-A M{\wdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTdzOT6wPUBvVQ>? M4nvTnNCVkeHUh?=
NCI-H1770 NYe0U4RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLOTWM2OD15MkKuOEBvVQ>? MWDTRW5ITVJ?
HAL-01 M{jiTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13pR2lEPTB;N{O0MlcyKG6P NGHLZ4VUSU6JRWK=
COLO-684 NHPDXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO2TWM2OD15NUOuNFEhdk1? NFLoRZpUSU6JRWK=
TE-6 M3vCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTd4ND6zNUBvVQ>? NXqw[5VFW0GQR1XS
A431 NGjaZXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DXXWlEPTB;N{iwMlA1KG6P Mlf4V2FPT0WU
LU-135 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTd6Mz6wN{BvVQ>? MVTTRW5ITVJ?
EC-GI-10 M4S0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLUTWM2OD15OEiuOVIhdk1? NIn2XIlUSU6JRWK=
TE-12 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fCWWlEPTB;OEKxMlEyKG6P M4TWfnNCVkeHUh?=
LoVo M2nnb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH0b2x3UUN3ME24OVkvODZibl2= MY\TRW5ITVJ?
23132-87 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[ydXBWUUN3ME24OlQvOjhibl2= NVP2XFBsW0GQR1XS
AU565 NWjnUGJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLyZ21KSzVyPUi2PU43KG6P NVnWU45yW0GQR1XS
DEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXyb|hKSzVyPUi3O{43PSCwTR?= M{D4cHNCVkeHUh?=
COR-L88 NHqzZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;2OndJUUN3ME24PFIvOjZibl2= NFH5fJFUSU6JRWK=
NCI-H2126 M17Rdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPUVmZsUUN3ME24PFIvQDNibl2= NGnQdGNUSU6JRWK=
CAPAN-1 M1;sVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPmTW9yUUN3ME24PFMvOjlibl2= M2rTTHNCVkeHUh?=
BT-474 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:xc5ZKSzVyPUmzPE4yPCCwTR?= NWn0PVRQW0GQR1XS
BHY NGfDVWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S1fWlEPTB;OUe1MlQ5KG6P MYPTRW5ITVJ?
HT-3 NV\FR5RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHTTWM2OD17OEKuOFEhdk1? MUjTRW5ITVJ?
SK-NEP-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W0VmlEPTB;OUi5MlQ1KG6P NHf4fVJUSU6JRWK=
MS-1 MnTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTl7ND62PUBvVQ>? Mkn4V2FPT0WU
DOHH-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rIfWlEPTB;MT6wNFAzOSEQvF2= NX7pe3ZHW0GQR1XS
NCI-H1304 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrkTWM2OD1zLkCxOlQ{KM7:TR?= M4HTbHNCVkeHUh?=
EM-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vCb2lEPTB;MT6wN|AyPiEQvF2= MX\TRW5ITVJ?
MHH-PREB-1 NEP1S4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS4TWM2OD1zLkC4OFUyKM7:TR?= MWfTRW5ITVJ?
KU-19-19 M4jpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL0[GVYUUN3ME2xMlA5PTRzIN88US=> NHSzRW1USU6JRWK=
NCI-H1648 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMUC2NVYh|ryP MnLEV2FPT0WU
MKN1 NXHwVmR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPjU3JkUUN3ME2xMlIyQTh5IN88US=> M1K4R3NCVkeHUh?=
SNU-449 NGW4d|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf5TWM2OD1zLkKyNlA5KM7:TR?= MnrHV2FPT0WU
OAW-42 NFvPV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LycmlEPTB;MT6yO|gzPSEQvF2= NHnzOWZUSU6JRWK=
769-P MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DhcWlEPTB;MT6yO|kyQCEQvF2= NF3hSVhUSU6JRWK=
SW1088 NH7HVnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LlbWlEPTB;MT6yPVYxPyEQvF2= NGnkbYVUSU6JRWK=
GCIY NX\KV25{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPzNGVoUUN3ME2xMlMxOTN{IN88US=> Mke4V2FPT0WU
CTV-1 M33j[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3tWHFKSzVyPUGuN|A5KM7:TR?= M3fsR3NCVkeHUh?=
NCI-H1092 NHrjRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFwM{C4OUDPxE1? MVHTRW5ITVJ?
NKM-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LqcWlEPTB;MT6zNlU6PyEQvF2= Ml3lV2FPT0WU
NCI-H1650 NGnkXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOzTWM2OD1zLkOzOFgzKM7:TR?= MXXTRW5ITVJ?
SW954 NYK5TmJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDiVplKSzVyPUGuN|QxPDhizszN M3S2WnNCVkeHUh?=
SW48 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC1ZYxSUUN3ME2xMlM3PjF6IN88US=> Mnz1V2FPT0WU
SK-N-DZ NXTtbZNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwM{[5OFch|ryP MlrKV2FPT0WU
KMOE-2 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfwTWM2OD1zLkO5PFE2KM7:TR?= NW\kOlJ1W0GQR1XS
NB5 M2fqUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHsTWM2OD1zLkSwPFk1KM7:TR?= M{nmcXNCVkeHUh?=
CCRF-CEM MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu1TWM2OD1zLkSxNVEh|ryP M3z6WHNCVkeHUh?=
RH-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2r1WGlEPTB;MT60NVE{PiEQvF2= NHm5bJVUSU6JRWK=
NCI-H526 NWTYSFRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFwNEO4NlYh|ryP NV3DOVg5W0GQR1XS
697 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[zOoZKSzVyPUGuOFQyODRizszN NYLCdpZ{W0GQR1XS
J82 NGfNbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnkdFZwUUN3ME2xMlQ2PzZ4IN88US=> NWXxfWczW0GQR1XS
BE-13 NF21cWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzSW5hKSzVyPUGuOVA3PzFizszN MUjTRW5ITVJ?
SAS NWDZdWhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M330fWlEPTB;MT61NVYzOiEQvF2= M3PidnNCVkeHUh?=
SCC-25 M3\ESWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLKTWM2OD1zLkWyN|IzKM7:TR?= MmLhV2FPT0WU
LAMA-84 MoLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwNUO4NVUh|ryP NFHPUGRUSU6JRWK=
HSC-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFwNUSzPEDPxE1? NHezVVRUSU6JRWK=
BT-549 NIfPZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFwNUi3OFch|ryP NYHFXYxYW0GQR1XS
ML-2 MnPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTFwNkSwNlkh|ryP MVXTRW5ITVJ?
BB30-HNC MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjmS2xKSzVyPUGuOlg6PzJizszN MWrTRW5ITVJ?
PANC-03-27 NX;5XWpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrR[|lKSzVyPUGuO|AyOzlizszN MYHTRW5ITVJ?
COLO-678 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnx[29DUUN3ME2xMlc{PDR2IN88US=> M1LWcnNCVkeHUh?=
NCI-H1666 NVK0c493T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL3SFVKSzVyPUGuO|Q4ODRizszN MV\TRW5ITVJ?
NCI-H209 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[z[JlKSzVyPUGuO|czPjlizszN MYPTRW5ITVJ?
EPLC-272H NWXEWFBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17sVGlEPTB;MT64OVU1QSEQvF2= NHr5[IpUSU6JRWK=
OMC-1 M{nPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;sTWM2OD1zLkm5PFg5KM7:TR?= NEnOfpJUSU6JRWK=
HCC70 NFvieoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PRW2lEPTB;Mj6wNFgyPSEQvF2= MXTTRW5ITVJ?
CAL-12T Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHGyZVBKSzVyPUKuNFE5PjFizszN NWruTlk5W0GQR1XS
TGBC24TKB NYO5O4d3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfmfIRKSzVyPUKuNFI6PjFizszN NX3tWWhQW0GQR1XS
EKVX NFzK[YVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\xTWM2OD1{LkC0PVM6KM7:TR?= M1XVbnNCVkeHUh?=
SW1116 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLXTWM2OD1{LkC2NFA6KM7:TR?= NWThSIZKW0GQR1XS
NCI-H2009 NYX5NZpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC5TWM2OD1{LkC2NlE1KM7:TR?= M3\aeXNCVkeHUh?=
RPMI-8866 NXfHZWNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF2wc|BKSzVyPUKuNFg1QDFizszN MnHUV2FPT0WU
KARPAS-45 NHPLPXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHoTWM2OD1{LkGyOFc6KM7:TR?= M13IeXNCVkeHUh?=
RXF393 NUKyR|V{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fTVWlEPTB;Mj6xN|A{PiEQvF2= NX7VXJhqW0GQR1XS
786-0 M{npbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HoRWlEPTB;Mj6xPFQxPiEQvF2= MVrTRW5ITVJ?
SCC-4 MmHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HBN2lEPTB;Mj6yNVc4PiEQvF2= M2D0dnNCVkeHUh?=
BT-20 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[x[4xKSzVyPUKuNlY4PDRizszN MVPTRW5ITVJ?
A498 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q4WWlEPTB;Mj6yPVQyPSEQvF2= M{[zUHNCVkeHUh?=
IGROV-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[1TWM2OD1{LkOxNlM4KM7:TR?= MVjTRW5ITVJ?
JVM-3 M33ibmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfXVlhSUUN3ME2yMlM1PjR|IN88US=> MoPrV2FPT0WU
NCI-H2170 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjKeG9JUUN3ME2yMlM1Pzh|IN88US=> M1v5THNCVkeHUh?=
EW-18 M4jYNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonFTWM2OD1{LkO1OFcyKM7:TR?= NITrSWpUSU6JRWK=
KU812 Mo\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7ybZZKSzVyPUKuN|Y4PzlizszN MlnMV2FPT0WU
NY Ml[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHsemJKSzVyPUKuN|czPyEQvF2= MlK3V2FPT0WU
HTC-C3 NEHRVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf3WJlIUUN3ME2yMlQzOjZ5IN88US=> NEDVVmxUSU6JRWK=
CFPAC-1 NGPhdJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJwNEO4OlQh|ryP NYi4fY5uW0GQR1XS
HH NXm1PGZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLsTWM2OD1{LkS5PFU1KM7:TR?= M1vpVHNCVkeHUh?=
MKN7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXBNWsyUUN3ME2yMlYzPzR6IN88US=> NYDYc4tVW0GQR1XS
TE-8 NIP2PJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TWWGlEPTB;Mj62N|Y2OyEQvF2= NHnMZmFUSU6JRWK=
MC-IXC NFXkRXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DjS2lEPTB;Mj62OFQ2OyEQvF2= NFPNboJUSU6JRWK=
DMS-79 NYLQcItXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrLTWM2OD1{Lk[5Nlg1KM7:TR?= NUC3OIVEW0GQR1XS
Detroit562 M1vXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmxdZBNUUN3ME2yMlY6QDR3IN88US=> NWG0O2xZW0GQR1XS
HuP-T4 M4HQ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjxTWM2OD1{LkeyPFE5KM7:TR?= NV3oTYFKW0GQR1XS
QIMR-WIL NYHEO5MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLHcnNGUUN3ME2yMlc2QTV{IN88US=> MlrPV2FPT0WU
BB65-RCC Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\kTWM2OD1{LkiwO|E{KM7:TR?= NXvNUHZ{W0GQR1XS
PC-3 M1HTWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[1TlJKSzVyPUKuPFM{OTdizszN NXrxcJNLW0GQR1XS
OVCAR-3 NELiVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3kTWM2OD1{Lki1OVk1KM7:TR?= MYPTRW5ITVJ?
KYSE-510 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJwOE[3PFYh|ryP NFn1S4tUSU6JRWK=
HC-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS2VnQ{UUN3ME2yMlk1ODF{IN88US=> NWrKbWM3W0GQR1XS
NCI-H1693 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\OcmNQUUN3ME2yMlk2QDl5IN88US=> Ml\rV2FPT0WU
DU-4475 NEnKT|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvMTWM2OD1{Lkm5NFUzKM7:TR?= NXfL[4RoW0GQR1XS
COLO-680N MnvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTNwMEC0PVUh|ryP MlfmV2FPT0WU
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H-EMC-SS MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\oUodKSzVyPUS1Mlc3QTNizszN M3L5dnNCVkeHUh?=
NCI-H2052 MlT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDrXItLUUN3ME20OU46ODJ5IN88US=> NYHRVlRCW0GQR1XS
SW684 M134W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jQdWlEPTB;NEeuNFA5OSEQvF2= NWrzXIZmW0GQR1XS
HCC1569 NFWw[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;jTWM2OD12Nz6xOlU5KM7:TR?= MXPTRW5ITVJ?
KGN NXrSdIh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;CTWM2OD12Nz6zN|EyKM7:TR?= NHvHPY9USU6JRWK=
LCLC-103H M3rTSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojQTWM2OD12Nz60OFA1KM7:TR?= NV;OfmJmW0GQR1XS
SW780 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTR5Lk[zOVEh|ryP MYLTRW5ITVJ?
NCI-H1703 MmHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnOT5c5UUN3ME20PE4{OzV{IN88US=> M2\zdnNCVkeHUh?=
HCC1395 NU\BS2tDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR6Lke0N|Ih|ryP MorZV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo試験 Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. [3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. [4]
臨床試験 Gefitinib has entered in a phase II clinical trial in the treatment of non small cell lung cancer.
特集 A potent EGFR tyrosine kinase inhibitor.

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 NR6, NR6M and NR6W cells
濃度 0-2 μM
反応時間 72 hours
実験の流れ Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.

動物実験: [3]

動物モデル Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
製剤 0.5% polysorbate
投薬量 100 mg/kg
投与方法 Once daily by oral administration (0.1 mL/10 g body weight) for 14 days

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Gefitinib (ZD1839) SDF
分子量 446.90
化学式

C22H24ClFN4O3

CAS No. 184475-35-2
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 89 mg/mL (199.14 mM)
Ethanol 4 mg/mL (8.95 mM)
Water <1 mg/mL
In vivo 5% DMSO+corn oil 2.5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

文献中の引用 (91)

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.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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