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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RH-1 M1rQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTEbphKSzVyPUGuOFEyOzZizszN MX7TRW5ITVJ?
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BCPAP MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTNwMEiyPVUh|ryP NYS0PXZoW0GQR1XS
647-V MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HLO2lEPTB;Mz6xOlIzKM7:TR?= MXXTRW5ITVJ?
HT-1376 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T1W2lEPTB;Mz6yNFUxPiEQvF2= NYXURWR5W0GQR1XS
NCI-H1793 NEPicIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\nPWlEPTB;Mz6yNVA6QCEQvF2= Ml3NV2FPT0WU
SW1463 NFjwRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\sWmlEPTB;Mz6yOlE6OiEQvF2= NF;T[FRUSU6JRWK=
NCI-H727 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[1d2lEPTB;Mz6zPFU5PCEQvF2= MXzTRW5ITVJ?
LB771-HNC NFPseJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPRUXFKSzVyPUOuN|kyOjZizszN MmfjV2FPT0WU
D-542MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVriWoY4UUN3ME2zMlQ1OjJ{IN88US=> Ml;JV2FPT0WU
NTERA-S-cl-D1 NXvBW|Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjCUndZUUN3ME2zMlQ1QTV5IN88US=> MUPTRW5ITVJ?
C8166 NI\UTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4freGlEPTB;Mz60OlUzOSEQvF2= MYfTRW5ITVJ?
639-V NE\nNXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LZS2lEPTB;Mz61O|c6OiEQvF2= M1\TSXNCVkeHUh?=
TE-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j1OmlEPTB;Mz61PVE3QSEQvF2= M3HmfHNCVkeHUh?=
OAW-28 NInXZplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nMUGlEPTB;Mz61PVQzPiEQvF2= MYPTRW5ITVJ?
SK-LU-1 NHvDN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPyTWM2OD1|Lk[wOlQ2KM7:TR?= M4P2VnNCVkeHUh?=
CaR-1 NHPwU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIH3UZBKSzVyPUOuOlExPDhizszN NHHrTFhUSU6JRWK=
A2780 M1frPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3IOVFYUUN3ME2zMlY1ODh7IN88US=> NGrsd5dUSU6JRWK=
C2BBe1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrVTWM2OD1|Lk[0OFA4KM7:TR?= MoXwV2FPT0WU
SK-MES-1 M4Hjcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC1TWM2OD1|Lk[0OlE1KM7:TR?= M3zYUnNCVkeHUh?=
PANC-10-05 NVXQbWo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjETWM2OD1|LkeyNFczKM7:TR?= NF\GWIZUSU6JRWK=
J-RT3-T3-5 MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn3TWM2OD1|Lke1OFA3KM7:TR?= MX3TRW5ITVJ?
ES4 M4joUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LF[2lEPTB;Mz64NlI5PiEQvF2= MmHOV2FPT0WU
NCI-H28 NUTLWlg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DudmlEPTB;Mz64Nlk3OSEQvF2= MXHTRW5ITVJ?
NCI-H1155 MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH3TWM2OD1|Lki0NVU6KM7:TR?= M{PpSHNCVkeHUh?=
KURAMOCHI MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\Gb2lEPTB;Mz64OlA2PiEQvF2= NGTuNJdUSU6JRWK=
NCI-H69 NHP0XFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXMT5pKSzVyPUOuPVAyPzhizszN NXW5[nM1W0GQR1XS
IST-MES1 NIHtVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr4TWM2OD1|Lkm0NFI6KM7:TR?= M2HwZXNCVkeHUh?=
NH-12 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml60TWM2OD1|Lkm0NVg4KM7:TR?= MkPsV2FPT0WU
JVM-2 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULw[ItyUUN3ME2zMlk1PzV{IN88US=> NYrKUW15W0GQR1XS
EW-16 NVrvd5ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LmXGlEPTB;Mz65OVU4PyEQvF2= NUDwZW1[W0GQR1XS
NCI-H441 NGnENllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHiTWM2OD1|Lkm3NFE1KM7:TR?= M{SwN3NCVkeHUh?=
RCC10RGB NVXZSGd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m4UmlEPTB;ND6wNVI1PiEQvF2= MWHTRW5ITVJ?
TCCSUP MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S0WmlEPTB;ND6xNVA2KM7:TR?= MmPpV2FPT0WU
HL-60 NXHzOHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUW4[IoxUUN3ME20MlEzOjRzIN88US=> NHzD[JBUSU6JRWK=
EW-11 NFKzS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\KUm9iUUN3ME20MlE{OjZzIN88US=> M{HpeHNCVkeHUh?=
KARPAS-299 NVOwdFk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn2zTWM2OD12LkOxNFE{KM7:TR?= Ml7vV2FPT0WU
SNU-C2B MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3qUnBCUUN3ME20MlM1Pjh4IN88US=> M4q1S3NCVkeHUh?=
LU-139 NIHvOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:yephKSzVyPUSuN|czPDdizszN NWT0Uo51W0GQR1XS
HCC1937 M2DWemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf4bJRKSzVyPUSuN|c6QTNizszN MY\TRW5ITVJ?
GR-ST MnzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLpTWM2OD12LkSzNVgh|ryP MXXTRW5ITVJ?
SK-OV-3 NUnaZW95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXvR|hKSzVyPUSuOFYxPDJizszN M1KwcXNCVkeHUh?=
A172 NULLfoZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2PYhFUUN3ME20MlU2PTJzIN88US=> M4HqZnNCVkeHUh?=
NB10 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTxTWM2OD12LkW5O|gyKM7:TR?= M1WwRnNCVkeHUh?=
P30-OHK M4HaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfhTWM2OD12LkixPVI6KM7:TR?= M33NVnNCVkeHUh?=
KYSE-520 M{SwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTlWlJKSzVyPUSuPFgxOThizszN NU\KTopEW0GQR1XS
KNS-62 NVf1UXdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnBUFRKSzVyPUSuPVA5ODdizszN NGj1TodUSU6JRWK=
ES1 M{\qbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X3XmlEPTB;ND65OlA{PSEQvF2= MVHTRW5ITVJ?
KOSC-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjKdZZKSzVyPUSuPVk6PTlizszN Mn;aV2FPT0WU
TE-9 NFm5SVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrtTWM2OD13LkCxOVI2KM7:TR?= M1;ON3NCVkeHUh?=
NCI-H1838 M1XDXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLncJZKSzVyPUWuNFIxPzZizszN NIXD[lBUSU6JRWK=
KP-N-YN NHXQWWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGD6bIVKSzVyPUWuNVI2QTFizszN MX7TRW5ITVJ?
ALL-PO MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf6bndKSzVyPUWuNlI2QDdizszN Mk\OV2FPT0WU
NOMO-1 NHTQPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorrTWM2OD13LkKzNVc3KM7:TR?= Mkj5V2FPT0WU
CGTH-W-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTVwM{i1PFQh|ryP M{XIeXNCVkeHUh?=
ATN-1 NHHBSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTVwNEGxPFQh|ryP NXmzT|kzW0GQR1XS
AGS MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEGwWJpKSzVyPUWuOFk3OThizszN MXTTRW5ITVJ?
SW13 NVLEUFFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T1VGlEPTB;NT61N|I3PSEQvF2= M1;Fd3NCVkeHUh?=
SW1990 NH;MVo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DHd2lEPTB;NT62NlI5PSEQvF2= M1;Zd3NCVkeHUh?=
BFTC-905 NXXjS21iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP3TWM2OD13Lk[1PFc5KM7:TR?= NWO0eJFZW0GQR1XS
RMG-I MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HTc2lEPTB;NT62OVk1OiEQvF2= MX;TRW5ITVJ?
HD-MY-Z NX7VNmZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTWTWM2OD13Lk[4OVgyKM7:TR?= MYPTRW5ITVJ?
HCC1187 NGO3cmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j4T2lEPTB;NT63NVA{OiEQvF2= MV\TRW5ITVJ?
HCC2998 M4Pt[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTVwN{G4O|ch|ryP NGX1ZYZUSU6JRWK=
RT-112 NUHRWHgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;RdWlEPTB;NT65NFI1PSEQvF2= Mkn4V2FPT0WU
CAKI-1 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnHTWM2OD14LkCwPVg2KM7:TR?= M120dnNCVkeHUh?=
HDLM-2 M1WxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTZwMEG0PFkh|ryP NUHaWWZzW0GQR1XS
TE-10 NFe0ZVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTZwMES4N|Mh|ryP MULTRW5ITVJ?
KE-37 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2O4R2lEPTB;Nj6wO|I2QCEQvF2= MorSV2FPT0WU
RCM-1 MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DlU2lEPTB;Nj6wO|cyQSEQvF2= M1eyc3NCVkeHUh?=
Mewo Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTZwMUG0PFch|ryP NWXHRYJJW0GQR1XS
L-428 NXfUUWVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzWTWM2OD14LkG4NFM4KM7:TR?= NVfHVFFbW0GQR1XS
8-MG-BA MkXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ad2lEPTB;Nj6xPVM4QSEQvF2= M4HyZ3NCVkeHUh?=
SK-MEL-28 NH;2T5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7YfVg5UUN3ME22MlIxQTZ5IN88US=> Mk[3V2FPT0WU
VA-ES-BJ MnnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYra[W1kUUN3ME22MlMxPDZ{IN88US=> MUfTRW5ITVJ?
CAL-120 M2XDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\ETWM2OD14LkS1NVYzKM7:TR?= M4DCcHNCVkeHUh?=
GAMG M1mxZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjnO3N2UUN3ME22MlUxPjJizszN MUfTRW5ITVJ?
MSTO-221H NXnhSlZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPKWG9GUUN3ME22MlUyOTdizszN MUHTRW5ITVJ?
GCT MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTZwNUOzPFch|ryP Mn\FV2FPT0WU
SH-4 NGDOfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTZwNUi4OFQh|ryP MV\TRW5ITVJ?
Calu-3 M1jaXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTZwNkW1Olgh|ryP MWfTRW5ITVJ?
SK-HEP-1 NF\HdFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXSS4JKSzVyPU[uO|E4PTNizszN NF;4eI5USU6JRWK=
PFSK-1 NHnQZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7CTWM2OD14LkezOFc5KM7:TR?= Mm\aV2FPT0WU
NB12 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\uZWlEPTB;Nj63PFQxPCEQvF2= NGLCblBUSU6JRWK=
A388 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTZwOEm1NkDPxE1? NGXhc4tUSU6JRWK=
KLE NGfSdZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrDTWM2OD14Lkm2OVE3KM7:TR?= NEfDb3JUSU6JRWK=
TE-11 NXH1flBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\5SmlEPTB;Nz6wOFk3PyEQvF2= NGfYRnZUSU6JRWK=
NCI-H2405 NIHid3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfQ[plPUUN3ME23MlA5Ozl|IN88US=> NGfpcW9USU6JRWK=
OVCAR-4 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfk[|R3UUN3ME23MlE2OzVizszN MXTTRW5ITVJ?
KP-N-YS NHLwXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfDTnlYUUN3ME23MlE5OTRizszN NEC2ZWtUSU6JRWK=
NOS-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr2UnZKSzVyPUeuNlU5OjhizszN MXzTRW5ITVJ?
DMS-114 MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37PemlEPTB;Nz6yPVY{OSEQvF2= MlfEV2FPT0WU
NCI-H2030 NFTxb3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK1fpZKSzVyPUeuN|M3QThizszN NILHcGZUSU6JRWK=
HEL M2S5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfWWmZKSzVyPUeuN|c2OjFizszN NGn2NVFUSU6JRWK=
CAL-62 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTdwM{m4OlYh|ryP NVHKXo1nW0GQR1XS
COLO-668 M4X3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK4dmcxUUN3ME23MlQ{QTZ5IN88US=> M2LzZ3NCVkeHUh?=
SKG-IIIa MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjEe4tbUUN3ME23MlQ2OzhzIN88US=> NWTJdm16W0GQR1XS
HCC1419 MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDNTWM2OD15LkS2PFM{KM7:TR?= M{LXOXNCVkeHUh?=
OS-RC-2 NWrGfW1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTdwNEm4PVQh|ryP MlrlV2FPT0WU
COLO-829 M4nV[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTdwNk[0OlMh|ryP NITOTGhUSU6JRWK=
NB13 M{fPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;JPGtKSzVyPUeuPFI3PjdizszN NFP6PGxUSU6JRWK=
DK-MG Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fk[2lEPTB;Nz64N|IxOSEQvF2= MXLTRW5ITVJ?
SHP-77 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4W5dmlEPTB;Nz64OlY2OyEQvF2= MYfTRW5ITVJ?
NCI-H661 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGxNodNUUN3ME24MlA2QDZ5IN88US=> NWXmeGNNW0GQR1XS
AM-38 NEHLcFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPVTWM2OD16LkG2Nlgh|ryP Mlr3V2FPT0WU
VM-CUB-1 M{fzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fp[2lEPTB;OD6xO|AzQSEQvF2= MY\TRW5ITVJ?
KYSE-70 M{j2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nMS2lEPTB;OD6xPVc3OSEQvF2= Mn7xV2FPT0WU
5637 NEnsOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDVTWM2OD16LkOxNFU2KM7:TR?= MX3TRW5ITVJ?
TGBC11TKB M{Xod2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPoTWM2OD16LkS2NVY1KM7:TR?= NIK2Z2RUSU6JRWK=
EGI-1 NHfUOXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnsO45HUUN3ME24MlYxODh6IN88US=> MnjMV2FPT0WU
D-392MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDhTWM2OD16Lk[2NlE1KM7:TR?= M3PmW3NCVkeHUh?=
A673 NUj6UWRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn1RpRGUUN3ME24MlY4PjFzIN88US=> NV65clVIW0GQR1XS
COLO-792 M2m5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XoSGlEPTB;OD63OFk1PiEQvF2= M4j6cXNCVkeHUh?=
NCI-H1792 M3LNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRThwOEi5NFMh|ryP MXLTRW5ITVJ?
LS-1034 NHXoNnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TRTGlEPTB;OD65OFY2OiEQvF2= MnjHV2FPT0WU
D-566MG M3\QTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPHTWM2OD17LkCxPFEh|ryP M4PNPXNCVkeHUh?=
NCI-H226 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV32e2Z{UUN3ME25MlA6KM7:TR?= NVraOI0{W0GQR1XS
ChaGo-K-1 NFXNcYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDrTWM2OD17LkGwOVc6KM7:TR?= MlPBV2FPT0WU
NCI-H2228 MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTlwMUGwPFEh|ryP MWPTRW5ITVJ?
RPMI-8226 NFe3enNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PiTmlEPTB;OT6xNVMxPCEQvF2= NIPkdJhUSU6JRWK=
BFTC-909 M2H0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nsfWlEPTB;OT6xPFI6PyEQvF2= MlvVV2FPT0WU
HPAF-II M3vL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW2TWM2OD17LkKyOVE5KM7:TR?= NIrKbolUSU6JRWK=
Capan-2 NULad5U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjqU2xKSzVyPUmuOFAyODlizszN Moe4V2FPT0WU
IA-LM NHfJUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HufWlEPTB;OT60NVk3PiEQvF2= NXrkZWZ5W0GQR1XS
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H-EMC-SS MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR3Lke2PVMh|ryP M1OwdnNCVkeHUh?=
NCI-H2052 NYLXXWJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXztd2YzUUN3ME20OU46ODJ5IN88US=> NFG1[VRUSU6JRWK=
SW684 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PCRmlEPTB;NEeuNFA5OSEQvF2= M1;HdXNCVkeHUh?=
HCC1569 NI\oXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR5LkG2OVgh|ryP MlvsV2FPT0WU
KGN NYXONZhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVW5fnJ5UUN3ME20O{4{OzFzIN88US=> NGHycY5USU6JRWK=
LCLC-103H Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:3cGlEPTB;NEeuOFQxPCEQvF2= MYTTRW5ITVJ?
SW780 M3HGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR5Lk[zOVEh|ryP M1iySXNCVkeHUh?=
NCI-H1703 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWSzPGpwUUN3ME20PE4{OzV{IN88US=> NHnFVXBUSU6JRWK=
HCC1395 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\UenNKSzVyPUS4Mlc1OzJizszN MoLoV2FPT0WU

... 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 (90)

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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