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

高品質保証

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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 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwMEC1O|Ih|ryP M1;o[XNCVkeHUh?=
KASUMI-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjZSFBNUUN3ME2wMlAxQTFzIN88US=> NWTteXpqW0GQR1XS
HCC2218 NIizN3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvGTWM2OD1yLkCwPVg4KM7:TR?= Mn7sV2FPT0WU
KARPAS-45 NWHOfGJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHtV3VKSzVyPUCuNFE3PzFizszN NWLsTpRjW0GQR1XS
HSC-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkSyTWM2OD1yLkCxO|Q5KM7:TR?= MVjTRW5ITVJ?
CHL-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHkRWt2UUN3ME2wMlAyQDN7IN88US=> M4jDZnNCVkeHUh?=
KY821 M2nBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPacFBXUUN3ME2wMlAzODZizszN MlzuV2FPT0WU
NCI-N87 NWfBUpozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjDRVZKSzVyPUCuNFI4PzNizszN NV\je3kyW0GQR1XS
DOK MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMEOxPVQh|ryP NF21[pBUSU6JRWK=
DSH1 M1S4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4q1TWlEPTB;MD6wN|MyPCEQvF2= MkfsV2FPT0WU
MDA-MB-175-VII M{P3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK0d|ZKSzVyPUCuNFM1OTZizszN NES1fHpUSU6JRWK=
NCI-H2170 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\PbGNKSzVyPUCuNFM4OjhizszN MkLPV2FPT0WU
BT-474 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXTTWM2OD1yLkC0PVg3KM7:TR?= Ml65V2FPT0WU
EFO-27 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fUZmlEPTB;MD6wOVE5OiEQvF2= MWHTRW5ITVJ?
NCI-H720 NVXobVQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DneGlEPTB;MD6wOVMzPSEQvF2= MlPMV2FPT0WU
PC-14 NFq0SWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMEW2Olgh|ryP NFeyOlJUSU6JRWK=
EC-GI-10 NYrFcph6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwMEW5NVIh|ryP M4nLenNCVkeHUh?=
KYSE-450 NV:0UGc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnJTWM2OD1yLkC1PVc5KM7:TR?= MUTTRW5ITVJ?
BPH-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HNOmlEPTB;MD6wOVk5QCEQvF2= MXvTRW5ITVJ?
NCI-H292 M2S2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTxOoROUUN3ME2wMlA3ODlizszN NITl[5ZUSU6JRWK=
H9 NXu0TnVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvWTWM2OD1yLkC3NVMzKM7:TR?= NYTR[o9vW0GQR1XS
NCI-H526 MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HLVWlEPTB;MD6wO|gzOyEQvF2= NY\ONpdQW0GQR1XS
NCI-H1623 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\NSGlEPTB;MD6wPFAzPSEQvF2= MXvTRW5ITVJ?
KYSE-140 NFvwOmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMEizN{DPxE1? MYjTRW5ITVJ?
Ca9-22 NXLMfIdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMEizOVMh|ryP NEDL[VBUSU6JRWK=
AU565 NGfPOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rrOGlEPTB;MD6wPFUxPCEQvF2= MmTGV2FPT0WU
ZR-75-30 M{DldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwMEm1OFUh|ryP NHXac3lUSU6JRWK=
NCI-H1770 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjoTHQ6UUN3ME2wMlExOjhizszN MUHTRW5ITVJ?
LB2241-RCC NYfHZmZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETteYFKSzVyPUCuNVA5QDRizszN NED1dopUSU6JRWK=
CAL-39 NUHicY45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi5eItKSzVyPUCuNVE4QTJizszN M1PLTHNCVkeHUh?=
UACC-893 NFqy[nBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwMUG4PFUh|ryP NWjWWYc2W0GQR1XS
LU-65 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLqTWM2OD1yLkGyOlM{KM7:TR?= Mk\IV2FPT0WU
HN MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmKzTWM2OD1yLkGzNFc4KM7:TR?= M1zRSnNCVkeHUh?=
TI-73 NFLLNFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXOZ45nUUN3ME2wMlE1PzF3IN88US=> NIr6U4xUSU6JRWK=
KU812 M37vR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnTTWM2OD1yLkG1OFU3KM7:TR?= NYfWUVQyW0GQR1XS
SW13 NHn4Tm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkK3TWM2OD1yLkG2NlE3KM7:TR?= NXrvVo1NW0GQR1XS
BB30-HNC MmnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T0VWlEPTB;MD6xOlU4PiEQvF2= MYHTRW5ITVJ?
HSC-2 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrpTWM2OD1yLkG2PFM4KM7:TR?= NU\1TJhCW0GQR1XS
BV-173 NFGxb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ZeWlEPTB;MD6xO|U6PiEQvF2= MUXTRW5ITVJ?
CAL-27 NGDY[4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\JRpdiUUN3ME2wMlE4PjN4IN88US=> MXjTRW5ITVJ?
SBC-1 NYXnNmNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17WU2lEPTB;MD6xPFk2QSEQvF2= MXfTRW5ITVJ?
CAL-33 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH35N|NKSzVyPUCuNlAyQDRizszN M2\meXNCVkeHUh?=
NCI-H209 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jZNGlEPTB;MD6yNFQ3KM7:TR?= NWHHSnlMW0GQR1XS
COR-L105 NHqySG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nBXWlEPTB;MD6yNVA5PCEQvF2= MYHTRW5ITVJ?
HSC-3 M1TZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;Ge2lEPTB;MD6yNVE6QCEQvF2= NIrGUZVUSU6JRWK=
NCI-H69 MlXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTVV4M1UUN3ME2wMlIyPDVzIN88US=> NIjycW1USU6JRWK=
MOLT-13 M3m0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rFcGlEPTB;MD6yN|k4PSEQvF2= MojjV2FPT0WU
ML-2 NXzOXJZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMkS4NFIh|ryP MWDTRW5ITVJ?
IGROV-1 MmnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTOTWM2OD1yLkK1PVUzKM7:TR?= NFLYOINUSU6JRWK=
TK10 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7lbWFmUUN3ME2wMlI3PzN6IN88US=> M324bHNCVkeHUh?=
EoL-1-cell M4PTRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn4NY9KSzVyPUCuNlY5QTJizszN MnrGV2FPT0WU
HO-1-N-1 M4G2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LZRmlEPTB;MD6yO|g2OyEQvF2= NViyO2F5W0GQR1XS
BHY NXzMNZFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfEUY9KSzVyPUCuNlg3PTVizszN M{nwfHNCVkeHUh?=
LU-139 M{D0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ezUWlEPTB;MD6zNFUyKM7:TR?= NYX2VWlUW0GQR1XS
23132-87 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwM{G5NlMh|ryP NHvCWGJUSU6JRWK=
ACHN M3zHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHCOIpKSzVyPUCuN|E6QTRizszN MXHTRW5ITVJ?
DoTc2-4510 NH:wXJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DWUGlEPTB;MD6zNlIyQSEQvF2= M1vKd3NCVkeHUh?=
BB65-RCC M17G[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT2TWM2OD1yLkO0OVk{KM7:TR?= NEGzSpZUSU6JRWK=
HLE Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fjRWlEPTB;MD6zOVA1PiEQvF2= NVrI[Ig4W0GQR1XS
HCC1419 M{m2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPFXINKSzVyPUCuN|Y1ODhizszN M2ex[3NCVkeHUh?=
A388 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj3TWM2OD1yLkO2PFU4KM7:TR?= MXHTRW5ITVJ?
NUGC-3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwM{izO|Mh|ryP NUXNTpFSW0GQR1XS
KYSE-180 MlnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwM{mwPFkh|ryP NWDRXGpqW0GQR1XS
TE-6 MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTTNY1KSzVyPUCuOFAzPDZizszN MmXNV2FPT0WU
A498 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwNEC2O|Qh|ryP NXjye|ZGW0GQR1XS
NCI-H1648 NWnq[Y5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3wPWRKSzVyPUCuOFQyQDJizszN NGDFR5FUSU6JRWK=
DU-145 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfsTWNwUUN3ME2wMlQ1QDN|IN88US=> MVnTRW5ITVJ?
CW-2 NFL4UJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPDTWM2OD1yLkS2PVE1KM7:TR?= Mlf1V2FPT0WU
A431 M1vkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInHUlZKSzVyPUCuOFgzOzNizszN MYLTRW5ITVJ?
SAS MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlflTWM2OD1yLkS4N|k5KM7:TR?= NHzpNFNUSU6JRWK=
NCI-H2126 NX7oSJJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXlc5hEUUN3ME2wMlUyQTJ4IN88US=> NXHOdmVnW0GQR1XS
NCI-H358 NHGz[nVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K5RWlEPTB;MD61N|IyKM7:TR?= MmDtV2FPT0WU
FADU NXK4PFVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwNUS0NFQh|ryP NWi0c25[W0GQR1XS
ACN NUH5XJF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwNUWwPVQh|ryP NV\0OWVwW0GQR1XS
HCC70 NYHFUoxXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjmfJBQUUN3ME2wMlU4PjZzIN88US=> NV\hblN2W0GQR1XS
NCI-H1838 M{fP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUiwO|E4UUN3ME2wMlYxOjl7IN88US=> NEfqcmdUSU6JRWK=
CAL-54 M1zo[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwNkG2NlEh|ryP MWTTRW5ITVJ?
NCI-H1975 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XJbGlEPTB;MD62NVczQCEQvF2= M33kVnNCVkeHUh?=
COR-L88 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDweFRJUUN3ME2wMlY1OTF|IN88US=> NXr0[pZvW0GQR1XS
CTV-1 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fX[2lEPTB;MD62OFM6OiEQvF2= MXzTRW5ITVJ?
EW-18 M2TrU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\3TWM2OD1yLk[4Olk5KM7:TR?= MX\TRW5ITVJ?
HCC1806 NXT6cGhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\RRY9lUUN3ME2wMlY6PjZ4IN88US=> M{nU[3NCVkeHUh?=
HuP-T4 NYTLVVFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LnT2lEPTB;MD62PVc3KM7:TR?= NYe4dHc6W0GQR1XS
MDA-MB-361 MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPWTWM2OD1yLkeyOlYzKM7:TR?= MoDsV2FPT0WU
NCI-H1573 M1G3b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvVTWM2OD1yLkezOlMh|ryP M4fNWXNCVkeHUh?=
KU-19-19 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwN{e0OlQh|ryP MX3TRW5ITVJ?
COLO-678 NF\BWW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH6TWM2OD1yLkiwPFM1KM7:TR?= MkTvV2FPT0WU
C-33-A M1W5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwOEGyPVch|ryP M4nXWnNCVkeHUh?=
Calu-3 NWqxfnZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwOEG0N|Qh|ryP NFL4fnFUSU6JRWK=
AGS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\LbYRKUUN3ME2wMlg{PjR6IN88US=> NVew[4dFW0GQR1XS
SCC-25 NYDMU29jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7hbJR5UUN3ME2wMlg1OTdzIN88US=> NUnOfoxKW0GQR1XS
JVM-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1y5OmlEPTB;MD64PFI6QSEQvF2= M4LBc3NCVkeHUh?=
HCE-T M{fUVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwOEi0Nlgh|ryP M{TIU3NCVkeHUh?=
ES4 NUPhOYx4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL6[W9[UUN3ME2wMlk4QDN4IN88US=> M{jhWnNCVkeHUh?=
EKVX M1vHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELxVllKSzVyPUGuNFExPjRizszN NUfITm9oW0GQR1XS
D-542MG MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTuTWM2OD1zLkCxNFY1KM7:TR?= MY\TRW5ITVJ?
SW1116 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i4fWlEPTB;MT6wNVI5PyEQvF2= NGnGSZFUSU6JRWK=
5637 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrWSG5NUUN3ME2xMlAyPTFizszN MV;TRW5ITVJ?
HT-1376 M{HLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFwMEG1NVMh|ryP MYDTRW5ITVJ?
NB69 NHnLWotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnpTWM2OD1zLkCyPVQ2KM7:TR?= NFziT|BUSU6JRWK=
YKG-1 M2\XT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmyfoh[UUN3ME2xMlA2PDF7IN88US=> M1;jPHNCVkeHUh?=
EW-3 M{\vOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwMEe4PFMh|ryP MnHTV2FPT0WU
GCIY M1XqS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwMEixNFQh|ryP NHfxe25USU6JRWK=
SK-MES-1 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn3dG9KSzVyPUGuNVE1QDdizszN MmDCV2FPT0WU
PANC-08-13 NIXyPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\zT4lKSzVyPUGuNVY1OTZizszN MWrTRW5ITVJ?
SK-NEP-1 NHfKfIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwMUe1NVMh|ryP M1HDcHNCVkeHUh?=
SW954 NHz6PHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFwMkCyNVQh|ryP MoG0V2FPT0WU
NCI-SNU-5 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDSOGN5UUN3ME2xMlI{QSEQvF2= NIDCfYVUSU6JRWK=
SW48 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPTZ3hKSzVyPUGuNlU1OzJizszN NV70SIF[W0GQR1XS
HT-3 M4jxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nxWWlEPTB;MT6yPFc2OyEQvF2= M{\UfXNCVkeHUh?=
ETK-1 NWTDW|BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnznTWM2OD1zLkO3OFU3KM7:TR?= MnvSV2FPT0WU
SCC-15 NIXmRVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\GTWM2OD1zLkO5OFUyKM7:TR?= NIPxS4dUSU6JRWK=
DU-4475 NX;hOGx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPpTXlKSzVyPUGuOFAyOjFizszN MXzTRW5ITVJ?
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CFPAC-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTVTWM2OD1zLkSyOFk{KM7:TR?= NXK5c3gyW0GQR1XS
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HOS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfMdpFFUUN3ME2zPU43Ojd|IN88US=> MXPTRW5ITVJ?
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HT NI\pRlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTRyLk[2N|kh|ryP MWHTRW5ITVJ?
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HPAF-II M3vKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zWd2lEPTB;NEGuOlcxQSEQvF2= NHHnNGpUSU6JRWK=
UACC-257 Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jrSWlEPTB;NEGuO|M3QSEQvF2= MVzTRW5ITVJ?
EW-22 NHfsc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLWPHM6UUN3ME20NU45Pjl5IN88US=> M4TuSHNCVkeHUh?=
NCI-H1755 NUXYNpl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HJbGlEPTB;NEGuPFczPSEQvF2= MYDTRW5ITVJ?
KYSE-150 M1fEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3CTWM2OD12Mj6xO|gzKM7:TR?= NVTxcoRXW0GQR1XS
CGTH-W-1 NWH5NnByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHtTWM2OD12Mj60PVU2KM7:TR?= MW\TRW5ITVJ?
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KP-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f1O2lEPTB;NEKuPFg{OiEQvF2= NGTZTpdUSU6JRWK=
HCC38 NVT2b4E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L2bWlEPTB;NEKuPVYyQCEQvF2= NXjXO3NrW0GQR1XS
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CAL-62 MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LMfmlEPTB;NEOuOFAzQCEQvF2= M33CfnNCVkeHUh?=
NCI-H2029 NF;wT4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPiPW9KSzVyPUSzMlU2QDFizszN MXfTRW5ITVJ?
M14 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHtTWM2OD12ND6xN|MzKM7:TR?= NUXyNG5YW0GQR1XS
COLO-680N NHH1cYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfDTWM2OD12ND6zN|kh|ryP NULLd5VrW0GQR1XS
Hs-578-T NUG5c5EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofqTWM2OD12NT6wNlk1KM7:TR?= NV3j[otqW0GQR1XS
MSTO-211H M32yZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XkS2lEPTB;NEWuPVQ5OiEQvF2= NXjUXpJmW0GQR1XS
EW-1 NFOyWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUGxWItKUUN3ME20OU46Pjh7IN88US=> NHvGNXZUSU6JRWK=
SW948 MmLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTR4LkS0OlIh|ryP MnzNV2FPT0WU
NCI-H460 M33XT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TiTmlEPTB;NE[uOVI{KM7:TR?= M1qyW3NCVkeHUh?=
CAS-1 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\UTWM2OD12Nj63O|AyKM7:TR?= MYXTRW5ITVJ?
TGBC11TKB MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHXcoxKSzVyPUS3MlE4PzdizszN NFzLPWdUSU6JRWK=
HD-MY-Z NVPo[WFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfLOYg1UUN3ME20PE44QDZizszN MnHnV2FPT0WU
NCI-H226 NETGeJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC3flBwUUN3ME20PU44Pzh3IN88US=> MVzTRW5ITVJ?
PA-1 MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HqZmlEPTB;NEmuPFM{PSEQvF2= M3\CcXNCVkeHUh?=
LB2518-MEL MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm4PHJKSzVyPUS5Mlg4OjNizszN M2PlcHNCVkeHUh?=
A101D MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nYVWlEPTB;NEmuPVQzPSEQvF2= NVizdppwW0GQR1XS
NCI-H2087 M1vsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\xNJBuUUN3ME20PU46Pjh{IN88US=> NXLQV3hxW0GQR1XS

... 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 (34)

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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