Afatinib (BIBW2992)

Afatinib (BIBW2992)は不可逆的にEGF受容体/ HER2含むEGF受容体を抑制、 EGFR L858R , EGFR L858R/T790M と HER2を作用すると、 IC50がそれぞれ0.5 nM, 0.4 nM, 10 nM, 14 nMとなる。

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Afatinib (BIBW2992) 化学構造
分子量: 485.94

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カスタマーフィードバック(3)

Quality Control & 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
  • Afatinib (BIBW2992)のメカニズム

製品の説明

生物活性

製品説明 Afatinib (BIBW2992)は不可逆的にEGF受容体/ HER2含むEGF受容体を抑制、 EGFR L858R , EGFR L858R/T790M と HER2を作用すると、 IC50がそれぞれ0.5 nM, 0.4 nM, 10 nM, 14 nMとなる。
ターゲット

EGFRwt

EGFRL858R

EGFR L858R/T790M

HER2

IC50

0.5 nM

0.4 nM

10 nM

14 nM [1]

In vitro試験 BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HDLM-2 MoTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEC1O|Ih|ryP M1;ybnNCVkeHUh?=
KASUMI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWxTWM2OD1yLkCwPVEyKM7:TR?= M3vrb3NCVkeHUh?=
HCC2218 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XvWWlEPTB;MD6wNFk5PyEQvF2= MYDTRW5ITVJ?
KARPAS-45 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rHfmlEPTB;MD6wNVY4OSEQvF2= NGq5XlBUSU6JRWK=
HSC-4 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLzTWM2OD1yLkCxO|Q5KM7:TR?= NGTNbpJUSU6JRWK=
CHL-1 NET2OZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;XVIxHUUN3ME2wMlAyQDN7IN88US=> MnL1V2FPT0WU
KY821 NWGweFNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHCNnZJUUN3ME2wMlAzODZizszN NVjEOXo{W0GQR1XS
NCI-N87 NVTLPJd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPMPG1KSzVyPUCuNFI4PzNizszN M{jmPHNCVkeHUh?=
DOK NGrJOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS1OHBKSzVyPUCuNFMyQTRizszN M2rQOnNCVkeHUh?=
DSH1 NWjRT2NET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HCXGlEPTB;MD6wN|MyPCEQvF2= MU\TRW5ITVJ?
MDA-MB-175-VII MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXHTWM2OD1yLkCzOFE3KM7:TR?= M2LEZXNCVkeHUh?=
NCI-H2170 MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DpZmlEPTB;MD6wN|czQCEQvF2= M3XNU3NCVkeHUh?=
BT-474 NIjjfYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{naNWlEPTB;MD6wOFk5PiEQvF2= NHOzcW1USU6JRWK=
EFO-27 NF7Q[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjncFFKSzVyPUCuNFUyQDJizszN NIC1flJUSU6JRWK=
NCI-H720 M1nnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTKe21bUUN3ME2wMlA2OzJ3IN88US=> NYi2S2VZW0GQR1XS
PC-14 NYrl[GZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP5fnJKSzVyPUCuNFU3PjhizszN MlXxV2FPT0WU
EC-GI-10 NXW4NXdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrYTWM2OD1yLkC1PVEzKM7:TR?= NXfkbHU5W0GQR1XS
KYSE-450 NUf3bItiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGThbJhKSzVyPUCuNFU6PzhizszN MVfTRW5ITVJ?
BPH-1 NYfpN4ZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\kTWM2OD1yLkC1PVg5KM7:TR?= NYTmfnRIW0GQR1XS
NCI-H292 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jDcGlEPTB;MD6wOlA6KM7:TR?= MWLTRW5ITVJ?
H9 NEnLdZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwMEexN|Ih|ryP MWTTRW5ITVJ?
NCI-H526 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYWwd5h2UUN3ME2wMlA4QDJ|IN88US=> Mn7JV2FPT0WU
NCI-H1623 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\xTWM2OD1yLkC4NFI2KM7:TR?= MVPTRW5ITVJ?
KYSE-140 NID0WWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLD[IxKSzVyPUCuNFg{OyEQvF2= NYnWNXRGW0GQR1XS
Ca9-22 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PDcmlEPTB;MD6wPFM2OyEQvF2= MWfTRW5ITVJ?
AU565 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7qOWt7UUN3ME2wMlA5PTB2IN88US=> MWfTRW5ITVJ?
ZR-75-30 MoG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPPS4hKSzVyPUCuNFk2PDVizszN NX7xS3c3W0GQR1XS
NCI-H1770 MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7sb5gzUUN3ME2wMlExOjhizszN NUjSRo53W0GQR1XS
LB2241-RCC M{\vbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD0PYhiUUN3ME2wMlExQDh2IN88US=> M{O1NnNCVkeHUh?=
CAL-39 MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwMUG3PVIh|ryP Mk\UV2FPT0WU
UACC-893 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGP3OWlKSzVyPUCuNVE5QDVizszN M1XVTHNCVkeHUh?=
LU-65 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwMUK2N|Mh|ryP MWjTRW5ITVJ?
HN M3O3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP6TWM2OD1yLkGzNFc4KM7:TR?= NITwWINUSU6JRWK=
TI-73 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMUS3NVUh|ryP M2KxbnNCVkeHUh?=
KU812 M4PPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXMc21rUUN3ME2wMlE2PDV4IN88US=> MUTTRW5ITVJ?
SW13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO5cXB7UUN3ME2wMlE3OjF4IN88US=> NX\aUpRFW0GQR1XS
BB30-HNC M4GzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfCd4dDUUN3ME2wMlE3PTd4IN88US=> NXzibVBCW0GQR1XS
HSC-2 MoPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[x[W5mUUN3ME2wMlE3QDN5IN88US=> M{m2[XNCVkeHUh?=
BV-173 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7uTWM2OD1yLkG3OVk3KM7:TR?= NGDNcpNUSU6JRWK=
CAL-27 MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzxXY9KSzVyPUCuNVc3OzZizszN M4W5enNCVkeHUh?=
SBC-1 NG\YepBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X5d2lEPTB;MD6xPFk2QSEQvF2= M{XjS3NCVkeHUh?=
CAL-33 NGjab3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrm[mVZUUN3ME2wMlIxOTh2IN88US=> NFHVXZNUSU6JRWK=
NCI-H209 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jBOGlEPTB;MD6yNFQ3KM7:TR?= NIjKc3NUSU6JRWK=
COR-L105 NGnyfmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHaUIdKSzVyPUCuNlExQDRizszN Mni0V2FPT0WU
HSC-3 Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrL[pVKSzVyPUCuNlEyQThizszN MYfTRW5ITVJ?
NCI-H69 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fZPGlEPTB;MD6yNVQ2OSEQvF2= MnWwV2FPT0WU
MOLT-13 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTJfmc6UUN3ME2wMlI{QTd3IN88US=> MXTTRW5ITVJ?
ML-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i0bmlEPTB;MD6yOFgxOiEQvF2= M1rj[XNCVkeHUh?=
IGROV-1 NY\hVFlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHRTVlKSzVyPUCuNlU6PTJizszN NXjKWIRSW0GQR1XS
TK10 NFrUbWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrFTWM2OD1yLkK2O|M5KM7:TR?= MXnTRW5ITVJ?
EoL-1-cell MnvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe3TWM2OD1yLkK2PFkzKM7:TR?= NHSybmhUSU6JRWK=
HO-1-N-1 NFzwb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPsbVV1UUN3ME2wMlI4QDV|IN88US=> NIS2U45USU6JRWK=
BHY M4fxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT1TWM2OD1yLkK4OlU2KM7:TR?= NHzrV5VUSU6JRWK=
LU-139 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXSd49KSzVyPUCuN|A2OSEQvF2= NIS0U41USU6JRWK=
23132-87 M2nqSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDOTWM2OD1yLkOxPVI{KM7:TR?= NGrGZpRUSU6JRWK=
ACHN NELSWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHUcIpCUUN3ME2wMlMyQTl2IN88US=> Ml;TV2FPT0WU
DoTc2-4510 M17wbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwM{KyNVkh|ryP NV\WN4hyW0GQR1XS
BB65-RCC M3rRO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLFNGVKSzVyPUCuN|Q2QTNizszN NXr3fHQ{W0GQR1XS
HLE MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljMTWM2OD1yLkO1NFQ3KM7:TR?= NYrwNJVsW0GQR1XS
HCC1419 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO3eFZKSzVyPUCuN|Y1ODhizszN MmqwV2FPT0WU
A388 NWXwSXBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zZd2lEPTB;MD6zOlg2PyEQvF2= MYfTRW5ITVJ?
NUGC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwM{izO|Mh|ryP MWLTRW5ITVJ?
KYSE-180 NYPwWm91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\EU2lEPTB;MD6zPVA5QSEQvF2= MlPFV2FPT0WU
TE-6 NWjRRVdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;xOG5RUUN3ME2wMlQxOjR4IN88US=> Mom2V2FPT0WU
A498 M{H6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nUTWlEPTB;MD60NFY4PCEQvF2= NWD4[4g2W0GQR1XS
NCI-H1648 NIS5fldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGWxWZBKSzVyPUCuOFQyQDJizszN MWnTRW5ITVJ?
DU-145 M4P1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwNES4N|Mh|ryP NY\SW4RDW0GQR1XS
CW-2 NVj5[|NGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP5cWZKSzVyPUCuOFY6OTRizszN NEnUZndUSU6JRWK=
A431 NYjDfIIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfCVWx2UUN3ME2wMlQ5OjN|IN88US=> MY\TRW5ITVJ?
SAS Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHYTJhKSzVyPUCuOFg{QThizszN MmfuV2FPT0WU
NCI-H2126 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPqN4t5UUN3ME2wMlUyQTJ4IN88US=> M1HlenNCVkeHUh?=
NCI-H358 NFf4NXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwNUOyNUDPxE1? NXK0coJCW0GQR1XS
FADU MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\rTWM2OD1yLkW0OFA1KM7:TR?= NELKNXlUSU6JRWK=
ACN NXvSbZA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwNUWwPVQh|ryP M1P3OHNCVkeHUh?=
HCC70 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\4N4hKSzVyPUCuOVc3PjFizszN NVG3NYZ4W0GQR1XS
NCI-H1838 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nxNGlEPTB;MD62NFI6QSEQvF2= M{XOcnNCVkeHUh?=
CAL-54 NIHISnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PORmlEPTB;MD62NVYzOSEQvF2= MVzTRW5ITVJ?
NCI-H1975 MoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrNTWM2OD1yLk[xO|I5KM7:TR?= M1njcXNCVkeHUh?=
COR-L88 NXfQboxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofjTWM2OD1yLk[0NVE{KM7:TR?= Mnm0V2FPT0WU
CTV-1 NHnBS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDuRmZ7UUN3ME2wMlY1Ozl{IN88US=> NWSyVppZW0GQR1XS
EW-18 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwNki2PVgh|ryP MV3TRW5ITVJ?
HCC1806 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;UXnhKSzVyPUCuOlk3PjZizszN MofNV2FPT0WU
HuP-T4 M172TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz1TWM2OD1yLk[5O|Yh|ryP M1\VSXNCVkeHUh?=
MDA-MB-361 NXzVZXNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwN{K2OlIh|ryP MoPhV2FPT0WU
NCI-H1573 NXjYSZpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv2SnpKSzVyPUCuO|M3OyEQvF2= M13qN3NCVkeHUh?=
KU-19-19 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DQXGlEPTB;MD63O|Q3PCEQvF2= NUD3NHdVW0GQR1XS
COLO-678 NFrnZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGxfWNCUUN3ME2wMlgxQDN2IN88US=> M2XT[XNCVkeHUh?=
C-33-A MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwOEGyPVch|ryP MVXTRW5ITVJ?
Calu-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXYU5hKSzVyPUCuPFE1OzRizszN NHnyeIpUSU6JRWK=
AGS MlfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwOEO2OFgh|ryP NWPMT413W0GQR1XS
SCC-25 NXjvWHlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwOESxO|Eh|ryP NXi2PY06W0GQR1XS
JVM-2 M3jvbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLUTWM2OD1yLki4Nlk6KM7:TR?= MWjTRW5ITVJ?
HCE-T M4rTNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITsTZVKSzVyPUCuPFg1OjhizszN NXK4XnMxW0GQR1XS
ES4 M{Lkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwOUe4N|Yh|ryP NGn4UJJUSU6JRWK=
EKVX MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\UTWM2OD1zLkCxNFY1KM7:TR?= MoXxV2FPT0WU
D-542MG NEXmTotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFwMEGwOlQh|ryP M2HpNnNCVkeHUh?=
SW1116 MlzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknITWM2OD1zLkCxNlg4KM7:TR?= NWXNcIF6W0GQR1XS
5637 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TaVWlEPTB;MT6wNVUyKM7:TR?= NGnxWFJUSU6JRWK=
HT-1376 M{HPZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33UT2lEPTB;MT6wNVUyOyEQvF2= NH3KVHdUSU6JRWK=
NB69 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO3XGZbUUN3ME2xMlAzQTR3IN88US=> NHSzNohUSU6JRWK=
YKG-1 MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jlXmlEPTB;MT6wOVQyQSEQvF2= NIHzeFBUSU6JRWK=
EW-3 NXj4c3JIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDJTWM2OD1zLkC3PFg{KM7:TR?= NEDyWXRUSU6JRWK=
GCIY MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[1ZmVOUUN3ME2xMlA5OTB2IN88US=> MmnxV2FPT0WU
SK-MES-1 M4jM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnFWHJKSzVyPUGuNVE1QDdizszN M{LkVXNCVkeHUh?=
PANC-08-13 NX;sNXo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofkTWM2OD1zLkG2OFE3KM7:TR?= MmjlV2FPT0WU
SK-NEP-1 M2rLTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFwMUe1NVMh|ryP NWPmeINYW0GQR1XS
SW954 NFuzeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFwMkCyNVQh|ryP MXzTRW5ITVJ?
NCI-SNU-5 M3\1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHGNJlKSzVyPUGuNlM6KM7:TR?= MlTTV2FPT0WU
SW48 NXXMe2N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnxV2J{UUN3ME2xMlI2PDN{IN88US=> MYrTRW5ITVJ?
HT-3 NFj5[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfkNGRrUUN3ME2xMlI5PzV|IN88US=> NIPwfHhUSU6JRWK=
ETK-1 NILreIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PLfGlEPTB;MT6zO|Q2PiEQvF2= NWfEbIdDW0GQR1XS
SCC-15 NFPRcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG3fVNKSzVyPUGuN|k1PTFizszN MnvjV2FPT0WU
DU-4475 M171dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFwNECxNlEh|ryP NH\HPYxUSU6JRWK=
NB5 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnabIhKSzVyPUGuOFE{OTdizszN MV\TRW5ITVJ?
CFPAC-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7iTWM2OD1zLkSyOFk{KM7:TR?= NVzsb2p6W0GQR1XS
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HAL-01 NHHqZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rTfmlEPTB;OD61NVkyKM7:TR?= NFnZVHZUSU6JRWK=
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BALL-1 NFnYUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\0TVlwUUN3ME25MlIyQTB5IN88US=> M2HiN3NCVkeHUh?=
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CAMA-1 M4DuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nFN2lEPTB;OT6yPFEzQCEQvF2= MnHoV2FPT0WU
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NCI-H1650 M4DyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTLTWM2OD17Lk[wPVQ3KM7:TR?= M4TW[nNCVkeHUh?=
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CAL-85-1 M4DvbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHKUllKSzVyPUmuPFc{QDNizszN M3O3R3NCVkeHUh?=
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DEL M3vLfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[1e|NoUUN3ME2xNE4{QTR4IN88US=> NVrDUHVEW0GQR1XS
HuCCT1 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHkTWM2OD1zMD62NFM{KM7:TR?= MYPTRW5ITVJ?
OVCAR-4 M3S0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\0SYRKSzVyPUGwMlg5OzVizszN MoX5V2FPT0WU
CAL-72 MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFyLkmzPVEh|ryP M2PUcnNCVkeHUh?=
HCC1954 Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTHTWM2OD1zMT6wO|U1KM7:TR?= MU\TRW5ITVJ?
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ALL-PO M2LTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTFTWM2OD1zMT6yOVEzKM7:TR?= MXrTRW5ITVJ?
T84 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSwTmIzUUN3ME2xNU4{QTB5IN88US=> NXe4OYxTW0GQR1XS
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SW626 MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFzLkW3OVUh|ryP MUXTRW5ITVJ?
RPMI-2650 M{DUcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXiyRXV3UUN3ME2xNU42QDh3IN88US=> MmT3V2FPT0WU
MC-IXC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL1UW1IUUN3ME2xNU43PzJ6IN88US=> NUHOdJZpW0GQR1XS
HOP-62 NYDFcW5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jQWWlEPTB;MUGuOlc3PCEQvF2= MkD4V2FPT0WU
NOS-1 NFX1WpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLWTWM2OD1zMT63NVA6KM7:TR?= MlzqV2FPT0WU
SW1573 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXFTWM2OD1zMT63Nlk2KM7:TR?= M4X1fHNCVkeHUh?=
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HuO9 MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTBTWM2OD1zMT64O|c1KM7:TR?= M1XkPXNCVkeHUh?=
YAPC MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFzLkmyOVkh|ryP M4\wcnNCVkeHUh?=
MDA-MB-453 NY[wUmhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLiXJdKSzVyPUGxMlk2OTVizszN M4HQU3NCVkeHUh?=
NCI-H596 Mk\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fmXWlEPTB;MUKuNFM3QSEQvF2= Mn73V2FPT0WU
A172 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\vTWM2OD1zMj6wO|k5KM7:TR?= NWfZclE1W0GQR1XS
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SW837 M1HYd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrLOlVKSzVyPUGyMlkxOjhizszN NUPXe3k4W0GQR1XS
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SK-UT-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3L3PGlEPTB;MUOuNVA5OyEQvF2= NETXb3NUSU6JRWK=
OVCAR-5 MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnsTWM2OD1zMz6xOVk{KM7:TR?= MV3TRW5ITVJ?
8505C Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF|LkKwOlch|ryP MWPTRW5ITVJ?
SK-MEL-1 NGXGbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfJdJNKSzVyPUGzMlcyOzVizszN NWfKSJB[W0GQR1XS
LK-2 M3W0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq2S2xOUUN3ME2xN{44PjN7IN88US=> MljuV2FPT0WU
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Ramos-2G6-4C10 NFjnN2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\3TWM2OD1zND6wNlAzKM7:TR?= MmTlV2FPT0WU
EW-13 NIXWPI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DrW2lEPTB;MUSuNFM2OiEQvF2= MormV2FPT0WU
NCI-H1793 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTF2LkKwPFch|ryP MXnTRW5ITVJ?
BHT-101 Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF2LkK0NUDPxE1? M2HYPHNCVkeHUh?=
RKO NEnyZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXPT2hpUUN3ME2xOE42ODd3IN88US=> M1XMUXNCVkeHUh?=
NEC8 NHv2SlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvEUJl4UUN3ME2xOE42PDd{IN88US=> NH\sWHFUSU6JRWK=
PANC-10-05 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;1SVRHUUN3ME2xOE43OjR5IN88US=> NGLaOoVUSU6JRWK=
NCI-H2030 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLWTWM2OD1zND62OFQ5KM7:TR?= NHXpb3FUSU6JRWK=
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EM-2 MnfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPTRpJmUUN3ME2xOE45PTd4IN88US=> NWn4TVJ[W0GQR1XS
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SW1463 M4PtSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHaT|lFUUN3ME2xOU4xPDh3IN88US=> NXTERmJsW0GQR1XS
J82 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF3LkC1O{DPxE1? MV7TRW5ITVJ?
CAL-120 NEHZZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X1dmlEPTB;MUWuNVQ1PyEQvF2= NH7URlNUSU6JRWK=
COLO-824 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f3RmlEPTB;MUWuNVU4QSEQvF2= NWP1OIh4W0GQR1XS
LNCaP-Clone-FGC MkP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVS0[HdxUUN3ME2xOU41OjR6IN88US=> NWfG[nd4W0GQR1XS
CP66-MEL MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT6SJpMUUN3ME2xOU41Pjh6IN88US=> MmHSV2FPT0WU
OC-314 NGOxVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7LcVBKSzVyPUG1MlQ4OTRizszN MlLhV2FPT0WU
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MFE-280 NHO0[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jFe2lEPTB;MU[uNFQ5QCEQvF2= M4C3ZnNCVkeHUh?=
MHH-NB-11 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HJeGlEPTB;MU[uNFg{QSEQvF2= M3viR3NCVkeHUh?=
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U-266 M{exeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPoZoU1UUN3ME2xOk4zOjl7IN88US=> MWHTRW5ITVJ?
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RH-18 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvv[VRKSzVyPUG4MlAxOzVizszN MYjTRW5ITVJ?
D-283MED MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[0bGlEPTB;MUiuNFA5QCEQvF2= MX3TRW5ITVJ?
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A704 NY\F[IV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTyXIlyUUN3ME2xPE41PzV|IN88US=> M3fKUXNCVkeHUh?=
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Mo-T Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHlTWM2OD1zOD64NlA1KM7:TR?= Ml\BV2FPT0WU
Saos-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rV[2lEPTB;MUmuNVE3OiEQvF2= Ml\WV2FPT0WU
SW684 NWT3d3ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS5TWM2OD1zOT6xN|I3KM7:TR?= M2jvXHNCVkeHUh?=
KMOE-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{O0SGlEPTB;MUmuNlI1OiEQvF2= NEnFS5FUSU6JRWK=
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LCLC-103H NY\FcohLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7GTWM2OD1|Nj63PFA{KM7:TR?= M2jP[HNCVkeHUh?=
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NCI-H446 NUDGSnRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTN5LkS4OlIh|ryP MWDTRW5ITVJ?
LU-99A NGnyN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN5LkW3N|Eh|ryP Mn;rV2FPT0WU
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SCC-9 Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy1cWQzUUN3ME2zO{44QDN6IN88US=> MY\TRW5ITVJ?
EFM-19 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTN5Lke5Olch|ryP MVfTRW5ITVJ?
A427 MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTN5LkmxNFch|ryP M4\1OHNCVkeHUh?=
LB831-BLC M3HhVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD4TWM2OD1|OD62NFM6KM7:TR?= MVfTRW5ITVJ?
HOS MmPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTN7Lk[yO|Mh|ryP M2O0PHNCVkeHUh?=
LAN-6 NFXQPI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSyTWM2OD12MD6wNVEzKM7:TR?= NIP2T5pUSU6JRWK=
U251 MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrvcZlKSzVyPUSwMlQxPTRizszN NGnOPIlUSU6JRWK=
SNU-387 NV\MTnhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTRyLkS1OVMh|ryP NVTEcoFnW0GQR1XS
DMS-79 NUnS[GJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjBTWM2OD12MD61PFg6KM7:TR?= M{XwRnNCVkeHUh?=
SK-LU-1 NIHyOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHWTJJ1UUN3ME20NE43PTZ6IN88US=> MXvTRW5ITVJ?
HT M1Pze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTRyLk[2N|kh|ryP MVTTRW5ITVJ?
KP-N-YS M1[0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL1TWM2OD12MD62O|Y5KM7:TR?= NUTuNZA1W0GQR1XS
DMS-114 MmP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iwdmlEPTB;NECuPFM4PCEQvF2= Mn;CV2FPT0WU
HUTU-80 NX\LN|FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTRzLkC1Olkh|ryP NWPSZ|BMW0GQR1XS
ONS-76 NIqwUYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\HZ2ZXUUN3ME20NU41PzB7IN88US=> MWTTRW5ITVJ?
A673 NIHUW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkToTWM2OD12MT61NVU4KM7:TR?= NHPZfpRUSU6JRWK=
HPAF-II NX[4bYFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn6TWM2OD12MT62O|A6KM7:TR?= MnHwV2FPT0WU
UACC-257 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjQTWM2OD12MT63N|Y6KM7:TR?= MVjTRW5ITVJ?
EW-22 M1r4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37G[GlEPTB;NEGuPFY6PyEQvF2= MXzTRW5ITVJ?
NCI-H1755 NXrNbFlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTRzLki3NlUh|ryP NEXGdGZUSU6JRWK=
KYSE-150 NHW3cXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXhRoVKSzVyPUSyMlE4QDJizszN NXPIPGRJW0GQR1XS
CGTH-W-1 NEfFd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DhRWlEPTB;NEKuOFk2PSEQvF2= MmLKV2FPT0WU
NB13 NEPRNI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTR{Lk[yNVch|ryP MVTTRW5ITVJ?
SW872 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHpTWM2OD12Mj62N|MyKM7:TR?= MkXqV2FPT0WU
KP-4 M2jtb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLveFBKSzVyPUSyMlg5OzJizszN MYnTRW5ITVJ?
HCC38 NIqwdplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vX[GlEPTB;NEKuPVYyQCEQvF2= Ml;DV2FPT0WU
BB49-HNC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj4[olKSzVyPUSzMlI{PTZizszN M4fBUXNCVkeHUh?=
CAL-62 NX3CcnBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT1c5FFUUN3ME20N{41ODJ6IN88US=> MYjTRW5ITVJ?
NCI-H2029 NEPhTm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTR|LkW1PFEh|ryP MUXTRW5ITVJ?
M14 NX20Xo81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrzb4V2UUN3ME20OE4yOzN{IN88US=> NEHKN|lUSU6JRWK=
COLO-680N M4TYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR2LkOzPUDPxE1? Mn3DV2FPT0WU
Hs-578-T NWTQcm9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfKcpNKSzVyPUS1MlAzQTRizszN NGf4e3FUSU6JRWK=
MSTO-211H NEniS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL4SXpKSzVyPUS1Mlk1QDJizszN M3;XZXNCVkeHUh?=
EW-1 NULLNHl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7LZYlwUUN3ME20OU46Pjh7IN88US=> NGnBOIZUSU6JRWK=
SW948 MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7HO4lWUUN3ME20Ok41PDZ{IN88US=> NGCyfnlUSU6JRWK=
NCI-H460 MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnTTWM2OD12Nj61NlMh|ryP NVjS[3NsW0GQR1XS
CAS-1 NXWwOo81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR4Lke3NFEh|ryP MnPWV2FPT0WU
TGBC11TKB NWTvVW5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXGzNJRVUUN3ME20O{4yPzd5IN88US=> M{DUdXNCVkeHUh?=
HD-MY-Z NXHVbmkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXaTWM2OD12OD63PFYh|ryP MmiyV2FPT0WU
NCI-H226 Mlj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofoTWM2OD12OT63O|g2KM7:TR?= M1fpTHNCVkeHUh?=
PA-1 M2PtOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR7LkizN|Uh|ryP NHryco1USU6JRWK=
LB2518-MEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH4blRKSzVyPUS5Mlg4OjNizszN MoXHV2FPT0WU
A101D MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR7Lkm0NlUh|ryP MkfTV2FPT0WU
NCI-H2087 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KwOmlEPTB;NEmuPVY5OiEQvF2= Mn7FV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo試験 Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like lapatinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies. [1]
臨床試験 A Phase II clinical trial of BIBW2992 for the treatment of cancer has been terminated.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

In vitro kinase activity assays The wild type tyrosine kinase domain of the human EGFR as well as that of the EGFR L858R/T790M double mutant are fused to Glutathione-S-transferase (GST), and extracted. Enzyme activity is then assayed in the presence of the inhibitor BIBW2992, serially diluted in 50% DMSO. A random polymer pEY (4:1) is used as substrate and biotinylated pEY (bio-pEY) is added as a tracer substrate. The kinase domain of HER2 is cloned using the baculovirus system and extracted similarly to that of EGFR kinase. Details of assays for EGFR, HER2, SRC, BIRK and VEGFR2 kinase activity are available in Supplementary information.

細胞アッセイ:

[1]

細胞株 NSCLC cells
濃度 0-10 μM
反応時間 1 hour
実験の流れ

1 × 104 NSCLC cells are transferred into each well of a 96-well plate and cultured overnight in serum-free media for the EGFR phosphorylation assay. After addition of BIBW2992 on the next day, the plates are incubated at 37 °C for 1 hour. EGF-stimulation is done using 100 ng/mL for 10 min at room temperature. Cells are washed with ice cold PBS, extracted with 120 μL HEPEX buffer per well and shaken at room temperature for 1 hour. In all 2 × 104 cells per well is used for the HER2 phosphorylation assay. Streptavidin precoated plates are coated with anti-EGFR-biotin at 1:100 dilution in blocking buffer and c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin. Cell extracts is then transferred to the antibody-coated wells and incubated at room temperature for 1 hour. Extinction is measured at 450 nm.

動物実験:

[1]

動物モデル Athymic NMRI-nu/nu female mice
製剤 In 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
投薬量 20 mg/kg
投与方法 Oral administration

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 Afatinib (BIBW2992) SDF
分子量 485.94
化学式

C24H25ClFN5O3

CAS No. 439081-18-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 97 mg/mL (199.61 mM)
エタノール 15 mg/mL (30.86 mM)
<1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose+0.2% Tween 80 30 mg/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 (S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide

カスタマーフィードバック (3)


Click to enlarge
Rating
Source Int J Proteomics, 2011, 2011, 215496. Afatinib (BIBW2992) purchased from Selleck
Method CEER assay
Cell Lines H460/A549/RFU cell lines
Concentrations 0-10 μM
Incubation Time 4 h
Results This data showed that a potent dose-dependent inhibition of the HER1 and HER2 pathways in the HCC827 cells was observed by treatment with BIBW-2992. Other HER1 and/or HER2 pathway-activated cell lines, H1975 and H1650, were likewise had these pathway activations blocked by the treatment with BIBW-2992.

Click to enlarge
Rating
Source Int J Proteomics, 2011, 2011, 215496. Afatinib (BIBW2992) purchased from Selleck
Method Nikon inverted-phase microscope
Cell Lines lung tumor cell lines
Concentrations 0.1/1 µM
Incubation Time two weeks
Results Reduction of cell colony size formation was observed by the treatment with the irreversible HER1/2 inhibitor BIBW-2992 in H1975 and H1650 cells as seen when these cells were grown in an anchorage-dependent manner.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. Afatinib (BIBW2992) purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-1 nM
Incubation Time 3 h
Results BIBW2992 treatment resulted in a reduction of EGFR phosphorylation in Breast cancer cells.

文献中の引用 (35)

Frequently Asked Questions

  • Question 1
    What’s the recommendation about reconstitution of the compound for in vivo animal study?

    Answer: For in vivo experiment of afatinib, we recommend 0.5% methylcellulose/0.2% Tween 80 as vehicle.

技術サポート&よくある質問(FAQ)

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Related EGFR 阻害剤

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    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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  • Poziotinib (HM781-36B)

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  • AZ5104

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  • Gefitinib (ZD1839)

    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。

    Features:A potent EGFR tyrosine kinase inhibitor.

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    Erlotinib HCl (OSI-744)は、2nMのIC50によるHER1/EGFR阻害剤です。

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  • Lapatinib

    ラパチニブ(Lapatinib Ditosylateの形で使われる)は、有力なEGFRErbB2 阻害剤で、IC50 がそれぞれ 10.8 と 9.2 nMです。

  • AG-490 (Tyrphostin B42)

    AG-490 (Tyrphostin B42)は、EGFRの選択的な阻害剤、ErbB2とJAK2で、IC50 がそれぞれ 0.1 μM、 13.5 μM、 and ~10 μMです。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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