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 (ZD1839) は、NR6wtEGFRとNR6W細胞のTyr1173、Tyr992、Tyr1173とTyr992のためのEGFR阻害剤で、IC50 がそれぞれ 37 nM、 37nM、 26 nM 、57 nM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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A549 MoDGR5l1d3SxeHnjJGF{e2G7 MnfXPVYhcA>? MUXEUXNQ NVfsO3ZFUUN3ME2xN{42QSEQvF2= NIHWc5kyQDNzM{iwOy=>
K562 M{[1WmN6fG:2b4jpZ{BCe3OjeR?= MmDTPVYhcA>? NIC3NXpFVVOR M1vNOGlEPTB;OT6zOkDPxE1? NIHR[2cyQDNzM{iwOy=>
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Plasmodium falciparum MXnxTHRUKHC{b3\pcIlv\yCob4KgbY5pcWKrdH;yd{Bw\iCSbHHzcY9lcXWvIH\hcINqeGG{dX2gdJJwdGmoZYLheIlwdg>? MYGyNVgyPzB2NR?=
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MCF7 M374dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXy[JpFOTBywrFOwIcwdUx? MYi0PEBp MYHEUXNQ NV34OnlwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXHSnIh\2WwZTD3bZRpKEmFNUCgc4YhOTJwMEWg{txO NG\PR3UzOjFzOUGzNC=>
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COR-L88 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:1c2NKSzVyPUi4Nk4zPiCwTR?= M1m3ZXNCVkeHUh?=
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TE-1 M{HoU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jzTGlEPTB;Mz61PVE3QSEQvF2= NFHBT2dUSU6JRWK=
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NCI-H28 NYrvNZJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnX1TWM2OD1|LkiyPVYyKM7:TR?= NX\lUY9tW0GQR1XS
NCI-H1155 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17KTmlEPTB;Mz64OFE2QSEQvF2= MVvTRW5ITVJ?
KURAMOCHI M1fCXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXVTWM2OD1|Lki2NFU3KM7:TR?= M2PpfnNCVkeHUh?=
NCI-H69 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnZO49KSzVyPUOuPVAyPzhizszN M4XKbnNCVkeHUh?=
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NH-12 NEK1d4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTmN3BGUUN3ME2zMlk1OTh5IN88US=> NHzpVYtUSU6JRWK=
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EW-16 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvvXHBrUUN3ME2zMlk2PTd5IN88US=> M2Lmd3NCVkeHUh?=
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HL-60 NEfEeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DaZmlEPTB;ND6xNlI1OSEQvF2= MmL2V2FPT0WU
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KARPAS-299 M1zzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq1WnBKSzVyPUSuN|ExOTNizszN NXP5[5d4W0GQR1XS
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LU-139 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTRwM{eyOFch|ryP MXvTRW5ITVJ?
HCC1937 NXPO[4lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\aNWlEPTB;ND6zO|k6OyEQvF2= Mk\4V2FPT0WU
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SK-OV-3 M3ThNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLGTWM2OD12LkS2NFQzKM7:TR?= MV7TRW5ITVJ?
A172 NI[1WYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTRwNUW1NlEh|ryP Mn\oV2FPT0WU
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P30-OHK MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WzVGlEPTB;ND64NVkzQSEQvF2= MYnTRW5ITVJ?
KYSE-520 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTRwOEiwNVgh|ryP NHfDepFUSU6JRWK=
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KOSC-2 NFXrTppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LMfGlEPTB;ND65PVk2QSEQvF2= M37YZXNCVkeHUh?=
TE-9 NFW5RmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj4SGxYUUN3ME21MlAyPTJ3IN88US=> NH\kRXBUSU6JRWK=
NCI-H1838 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTVwMEKwO|Yh|ryP M4H5WnNCVkeHUh?=
KP-N-YN NU\RUppLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLDTWM2OD13LkGyOVkyKM7:TR?= MXvTRW5ITVJ?
ALL-PO NVT3eoVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;IS2hsUUN3ME21MlIzPTh5IN88US=> MoT0V2FPT0WU
NOMO-1 M17IVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXNNpNKSzVyPUWuNlMyPzZizszN NXvnXnpxW0GQR1XS
CGTH-W-1 Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrIbIZKSzVyPUWuN|g2QDRizszN NF3LRYpUSU6JRWK=
ATN-1 NWPuc4VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTVwNEGxPFQh|ryP MWLTRW5ITVJ?
AGS NV\3SZRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT6UnAzUUN3ME21MlQ6PjF6IN88US=> MV3TRW5ITVJ?
SW13 Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnkTWM2OD13LkWzNlY2KM7:TR?= M1jBXnNCVkeHUh?=
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BFTC-905 NE[4dHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[3WHhXUUN3ME21MlY2QDd6IN88US=> MUPTRW5ITVJ?
RMG-I MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HOT2lEPTB;NT62OVk1OiEQvF2= NWLXUnNGW0GQR1XS
HD-MY-Z MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG4WGhRUUN3ME21MlY5PThzIN88US=> M{HQUHNCVkeHUh?=
HCC1187 NInCZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTVwN{GwN|Ih|ryP NVLjOYl1W0GQR1XS
HCC2998 M37iWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;pRmgxUUN3ME21MlcyQDd5IN88US=> MV;TRW5ITVJ?
RT-112 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH3TWM2OD13LkmwNlQ2KM7:TR?= M4qwVnNCVkeHUh?=
CAKI-1 MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfrNIRrUUN3ME22MlAxQTh3IN88US=> M2\zfnNCVkeHUh?=
HDLM-2 NV7hRYtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTZwMEG0PFkh|ryP M3HVbXNCVkeHUh?=
TE-10 NWPMOnF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO0T3NKSzVyPU[uNFQ5OzNizszN M{f1TnNCVkeHUh?=
KE-37 NUPkdlJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzaSWlYUUN3ME22MlA4OjV6IN88US=> NHX5W2FUSU6JRWK=
RCM-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C3TGlEPTB;Nj6wO|cyQSEQvF2= NXTZ[2UxW0GQR1XS
Mewo MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDtTWM2OD14LkGxOFg4KM7:TR?= MVPTRW5ITVJ?
L-428 M4Hxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHqTWM2OD14LkG4NFM4KM7:TR?= M1:zUHNCVkeHUh?=
8-MG-BA NVTFdpFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETJZYlKSzVyPU[uNVk{PzlizszN NXTXVZJnW0GQR1XS
SK-MEL-28 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTZwMkC5Olch|ryP MVLTRW5ITVJ?
VA-ES-BJ NGfLcm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUno[lE6UUN3ME22MlMxPDZ{IN88US=> NEnqSXRUSU6JRWK=
CAL-120 NXrEdo5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHYfnZoUUN3ME22MlQ2OTZ{IN88US=> NHi4VFNUSU6JRWK=
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MSTO-221H Ml\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:4bVJKSzVyPU[uOVEyPyEQvF2= M{\Q[XNCVkeHUh?=
GCT NH7uW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXkZ3pEUUN3ME22MlU{Ozh5IN88US=> NVmxe413W0GQR1XS
SH-4 NXLUNpU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHld|RKSzVyPU[uOVg5PDRizszN MYPTRW5ITVJ?
Calu-3 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjRTWM2OD14Lk[1OVY5KM7:TR?= M2DQSHNCVkeHUh?=
SK-HEP-1 M2rXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmzeoxFUUN3ME22MlcyPzV|IN88US=> NX7l[WpPW0GQR1XS
PFSK-1 M{nZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfqNYp4UUN3ME22Mlc{PDd6IN88US=> NF7SSVhUSU6JRWK=
NB12 NUm3eGt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXaTWM2OD14Lke4OFA1KM7:TR?= MXXTRW5ITVJ?
A388 NGnacW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DydGlEPTB;Nj64PVUzKM7:TR?= NWPueGU{W0GQR1XS
KLE MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTINlduUUN3ME22Mlk3PTF4IN88US=> NX\FZ5Q6W0GQR1XS
TE-11 NGjRPVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrLNohKSzVyPUeuNFQ6PjdizszN M13hTnNCVkeHUh?=
NCI-H2405 MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TqW2lEPTB;Nz6wPFM6OyEQvF2= MmnEV2FPT0WU
OVCAR-4 Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHXZmZKSzVyPUeuNVU{PSEQvF2= MY\TRW5ITVJ?
KP-N-YS NILwOI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK0VmNZUUN3ME23MlE5OTRizszN MmPTV2FPT0WU
NOS-1 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\DVWlEPTB;Nz6yOVgzQCEQvF2= NYD1TZRSW0GQR1XS
DMS-114 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HlTWlEPTB;Nz6yPVY{OSEQvF2= MonQV2FPT0WU
NCI-H2030 NIO4[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjS[2RoUUN3ME23MlM{Pjl6IN88US=> Ml7CV2FPT0WU
HEL MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL0TWM2OD15LkO3OVIyKM7:TR?= MX7TRW5ITVJ?
CAL-62 NV;KXYN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\0SZZKSzVyPUeuN|k5PjZizszN MXzTRW5ITVJ?
COLO-668 NGnoOGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HxS2lEPTB;Nz60N|k3PyEQvF2= M332R3NCVkeHUh?=
SKG-IIIa NXHHd2JRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7CRVgyUUN3ME23MlQ2OzhzIN88US=> M4PBdnNCVkeHUh?=
HCC1419 M2TYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTdwNE[4N|Mh|ryP MYLTRW5ITVJ?
OS-RC-2 NH\CT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\aOGlEPTB;Nz60PVg6PCEQvF2= MkjKV2FPT0WU
COLO-829 MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWSze|cxUUN3ME23MlY3PDZ|IN88US=> NHm2U3FUSU6JRWK=
NB13 NFvkSYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXTTWM2OD15LkiyOlY4KM7:TR?= NWPScoZkW0GQR1XS
DK-MG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTdwOEOyNFEh|ryP NWnxUGJRW0GQR1XS
SHP-77 Mn;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[yNmlEPTB;Nz64OlY2OyEQvF2= NHzCVGdUSU6JRWK=
NCI-H661 NX[4dHdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLBPWI{UUN3ME24MlA2QDZ5IN88US=> NUTPXGtjW0GQR1XS
AM-38 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRThwMU[yPEDPxE1? NELp[XBUSU6JRWK=
VM-CUB-1 MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\n[WlEPTB;OD6xO|AzQSEQvF2= M1TEVXNCVkeHUh?=
KYSE-70 NHnYVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRThwMUm3OlEh|ryP NHfycW9USU6JRWK=
5637 M3LOcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDFTWM2OD16LkOxNFU2KM7:TR?= MXPTRW5ITVJ?
TGBC11TKB M33Dcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXlTWM2OD16LkS2NVY1KM7:TR?= MnL6V2FPT0WU
EGI-1 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj0Zo9KSzVyPUiuOlAxQDhizszN NFnnPXdUSU6JRWK=
D-392MG MnP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRThwNk[yNVQh|ryP M{jPWnNCVkeHUh?=
A673 M13udGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4G5U2lEPTB;OD62O|YyOSEQvF2= M{C2UXNCVkeHUh?=
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NCI-H1792 M2\ifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofqTWM2OD16Lki4PVA{KM7:TR?= NUWyS5VMW0GQR1XS
LS-1034 NH\UcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGS2VmJKSzVyPUiuPVQ3PTJizszN M3;FO3NCVkeHUh?=
D-566MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[1dWdKSzVyPUmuNFE5OSEQvF2= Mn\qV2FPT0WU
NCI-H226 M4\wR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz0TWM2OD17LkC5JO69VQ>? NFHZUGNUSU6JRWK=
ChaGo-K-1 MoL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn24TWM2OD17LkGwOVc6KM7:TR?= NFjvWI1USU6JRWK=
NCI-H2228 NV;5UnVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF65U21KSzVyPUmuNVExQDFizszN MYTTRW5ITVJ?
RPMI-8226 M16wXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTlwMUGzNFQh|ryP NX6zb29HW0GQR1XS
BFTC-909 M1Ha[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\tSHBKSzVyPUmuNVgzQTdizszN NUfMfGtkW0GQR1XS
HPAF-II NFvlWJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[yeGlEPTB;OT6yNlUyQCEQvF2= NWHD[mtxW0GQR1XS
Capan-2 NFPmfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LDSWlEPTB;OT60NFExQSEQvF2= MYDTRW5ITVJ?
IA-LM M2DZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4H0VWlEPTB;OT60NVk3PiEQvF2= MYHTRW5ITVJ?
KP-4 NVvqWpNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTlwNEi4N|gh|ryP MoK3V2FPT0WU
A101D NE\yNW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HyUWlEPTB;OT61NVcyQSEQvF2= NYK4O5o1W0GQR1XS
EFO-21 NH3rTGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTlwNUi3N|Uh|ryP NVPm[4lmW0GQR1XS
C32 NUi3Z4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fMUGlEPTB;OT62N|M1KM7:TR?= MWrTRW5ITVJ?
SW837 NWj4d2tvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILQ[m1KSzVyPUmuPFQ5OiEQvF2= M1zNS3NCVkeHUh?=
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LCLC-103H NHnrVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzSd5RsUUN3ME20O{41PDB2IN88US=> M2PMPHNCVkeHUh?=
SW780 MkT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfaNoNnUUN3ME20O{43OzVzIN88US=> NGflSpdUSU6JRWK=
NCI-H1703 NXLyR2JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTR6LkOzOVIh|ryP M{HKfHNCVkeHUh?=
HCC1395 M4W3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTP[YpKSzVyPUS4Mlc1OzJizszN NGD1cJlUSU6JRWK=

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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