Afatinib (BIBW2992)

製品コードS1011

Afatinib (BIBW2992)化学構造

分子量(MW):485.94

Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively.

サイズ 価格(税別)  
JPY 39840.00
JPY 19920.00
JPY 34860.00
JPY 94620.00

文献中の使用例(37)

カスタマーフィードバック(4)

  • Cytoxicity of irreversible EGFR TKIS and ethacrynic acid on breast cells lines. A, Mean IC50 value of Afatinib.

    Oncotarget, 2016, 7(36):58038-58050. Afatinib (BIBW2992) purchased from Selleck.

    Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.

    Int J Proteomics 2011 2011, 215496. Afatinib (BIBW2992) purchased from Selleck.

  • Inhibition of anchorage-independent growth of lung tumor cell lines by selected inhibitors. Each selected cell line was treated with the indicated inhibitor at 0.1 μM and 1 μM concentrations for two weeks and cell colony size formation was scored under the Nikon inverted-phase microscope.

    Int J Proteomics 2011 2011, 215496. Afatinib (BIBW2992) purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of BIBW2992 for 3h,followed by 15-minute stimolation of 100ng/ml EGF

    Dr. Zhang of Tianjin Medical University. Afatinib (BIBW2992) purchased from Selleck.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively.
ターゲット
EGFR (L858R) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
EGFR (L858R/T790M) [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
0.4 nM 0.5 nM 10 nM 14 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwMEC1O|Ih|ryP MYjTRW5ITVJ?
KASUMI-1 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEC5NVEh|ryP NW[5NGtRW0GQR1XS
HCC2218 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvDTWM2OD1yLkCwPVg4KM7:TR?= M3WwXXNCVkeHUh?=
KARPAS-45 NX\vbodET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmD1TWM2OD1yLkCxOlcyKM7:TR?= NVe1UYFOW0GQR1XS
HSC-4 M3XSZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMEG3OFgh|ryP NXHXWG9CW0GQR1XS
CHL-1 NU\EbXlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwMEG4N|kh|ryP Mkj2V2FPT0WU
KY821 M4SwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe1OoVQUUN3ME2wMlAzODZizszN MX\TRW5ITVJ?
NCI-N87 NH7V[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PjfWlEPTB;MD6wNlc4OyEQvF2= M4L3VnNCVkeHUh?=
DOK M4rrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PoWmlEPTB;MD6wN|E6PCEQvF2= MmHqV2FPT0WU
DSH1 M1zZOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHryWpVKSzVyPUCuNFM{OTRizszN MkfQV2FPT0WU
MDA-MB-175-VII NXKzc4NoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXiTWM2OD1yLkCzOFE3KM7:TR?= NXvacIxvW0GQR1XS
NCI-H2170 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEO3Nlgh|ryP M{S0N3NCVkeHUh?=
BT-474 NYPHV|gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwMES5PFYh|ryP Mki2V2FPT0WU
EFO-27 M2O5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\oWYlKSzVyPUCuNFUyQDJizszN MYfTRW5ITVJ?
NCI-H720 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvsVnNKSzVyPUCuNFU{OjVizszN M2m5Z3NCVkeHUh?=
PC-14 NXHOfnQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTjcG1jUUN3ME2wMlA2PjZ6IN88US=> Ml22V2FPT0WU
EC-GI-10 NWixe3dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DucmlEPTB;MD6wOVkyOiEQvF2= NWq1eYlRW0GQR1XS
KYSE-450 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjab5dKSzVyPUCuNFU6PzhizszN NYfTfI95W0GQR1XS
BPH-1 NHmzdohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vEbGlEPTB;MD6wOVk5QCEQvF2= Ml7iV2FPT0WU
NCI-H292 NWHEfYRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\MdYFlUUN3ME2wMlA3ODlizszN M1P1ZXNCVkeHUh?=
H9 NU\nfWdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHISVdKSzVyPUCuNFcyOzJizszN NXr3OZpTW0GQR1XS
NCI-H526 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMEe4NlMh|ryP MXrTRW5ITVJ?
NCI-H1623 MlfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrGfHdWUUN3ME2wMlA5ODJ3IN88US=> M3e0enNCVkeHUh?=
KYSE-140 NEC1NoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zRO2lEPTB;MD6wPFM{KM7:TR?= MmjpV2FPT0WU
Ca9-22 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwMEizOVMh|ryP NF\H[3JUSU6JRWK=
AU565 NFfYZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfxW2VMUUN3ME2wMlA5PTB2IN88US=> NIW0fJhUSU6JRWK=
ZR-75-30 M120cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPWXGxFUUN3ME2wMlA6PTR3IN88US=> NF76S2JUSU6JRWK=
NCI-H1770 NEPaXGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMUCyPEDPxE1? MkDxV2FPT0WU
LB2241-RCC NUnNfIc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMUC4PFQh|ryP NETuV29USU6JRWK=
CAL-39 MmiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVT2TGJpUUN3ME2wMlEyPzl{IN88US=> MVnTRW5ITVJ?
UACC-893 NVrjOVZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3ldGxwUUN3ME2wMlEyQDh3IN88US=> MlHTV2FPT0WU
LU-65 M4LseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfETWM2OD1yLkGyOlM{KM7:TR?= MVvTRW5ITVJ?
HN NFnQb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T6WGlEPTB;MD6xN|A4PyEQvF2= MkW1V2FPT0WU
TI-73 NIXXfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwMUS3NVUh|ryP NVXzOZdsW0GQR1XS
KU812 M1fYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPZTWM2OD1yLkG1OFU3KM7:TR?= NF;JeolUSU6JRWK=
SW13 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMU[yNVYh|ryP MnnJV2FPT0WU
BB30-HNC NUD4TJZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLJ[VVXUUN3ME2wMlE3PTd4IN88US=> M{\qVnNCVkeHUh?=
HSC-2 M12xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMU[4N|ch|ryP MVrTRW5ITVJ?
BV-173 NYTwc|liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMUe1PVYh|ryP NIPhV4ZUSU6JRWK=
CAL-27 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwMUe2N|Yh|ryP NVHodGRbW0GQR1XS
SBC-1 M4PpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXjeplKSzVyPUCuNVg6PTlizszN NFH3TWtUSU6JRWK=
CAL-33 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\nRmlEPTB;MD6yNFE5PCEQvF2= MVvTRW5ITVJ?
NCI-H209 NFno[ZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPMZYM5UUN3ME2wMlIxPDZizszN NVfufXI5W0GQR1XS
COR-L105 NGnGRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwMkGwPFQh|ryP MXnTRW5ITVJ?
HSC-3 NYLwcolqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HYXWlEPTB;MD6yNVE6QCEQvF2= MknDV2FPT0WU
NCI-H69 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS2NoxKSzVyPUCuNlE1PTFizszN M3nyenNCVkeHUh?=
MOLT-13 MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITmN2ZKSzVyPUCuNlM6PzVizszN MnzSV2FPT0WU
ML-2 NIK0SYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXHT21KSzVyPUCuNlQ5ODJizszN MXrTRW5ITVJ?
IGROV-1 M4HYNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPXUZBKSzVyPUCuNlU6PTJizszN NIrJfoxUSU6JRWK=
TK10 NVrMc|RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnj[FMxUUN3ME2wMlI3PzN6IN88US=> NYDQV3N1W0GQR1XS
EoL-1-cell MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7qTWM2OD1yLkK2PFkzKM7:TR?= Mn;nV2FPT0WU
HO-1-N-1 NInTSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTmTWM2OD1yLkK3PFU{KM7:TR?= NVrxSIdbW0GQR1XS
BHY M2LVOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXqTWM2OD1yLkK4OlU2KM7:TR?= NE\rSJVUSU6JRWK=
LU-139 M1OwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP3fmVKSzVyPUCuN|A2OSEQvF2= MYDTRW5ITVJ?
23132-87 NFzoRVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq2PXRKSzVyPUCuN|E6OjNizszN M33i[nNCVkeHUh?=
ACHN MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS5RZBKSzVyPUCuN|E6QTRizszN MXjTRW5ITVJ?
DoTc2-4510 M{i5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPDTY54UUN3ME2wMlMzOjF7IN88US=> NVX1NWIzW0GQR1XS
BB65-RCC M4S5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojvTWM2OD1yLkO0OVk{KM7:TR?= Mnr0V2FPT0WU
HLE NInSNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwM{WwOFYh|ryP NX7te4p2W0GQR1XS
HCC1419 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzQXnAyUUN3ME2wMlM3PDB6IN88US=> MnzqV2FPT0WU
A388 NX\VZnU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S2fWlEPTB;MD6zOlg2PyEQvF2= MnPkV2FPT0WU
NUGC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPqTWM2OD1yLkO4N|c{KM7:TR?= NXz2cJFIW0GQR1XS
KYSE-180 M2fxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLU[pZKSzVyPUCuN|kxQDlizszN NGTD[2tUSU6JRWK=
TE-6 NWnHZ2xmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfTNotKSzVyPUCuOFAzPDZizszN M{PHXnNCVkeHUh?=
A498 NI\vcJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[5dm5KSzVyPUCuOFA3PzRizszN NHrse25USU6JRWK=
NCI-H1648 NVzuZ4xiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLSTWM2OD1yLkS0NVgzKM7:TR?= MUnTRW5ITVJ?
DU-145 M1yy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zLU2lEPTB;MD60OFg{OyEQvF2= MVLTRW5ITVJ?
CW-2 NVXQbWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjOSWltUUN3ME2wMlQ3QTF2IN88US=> NX7LT4FLW0GQR1XS
A431 NFOyRnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC3U41KSzVyPUCuOFgzOzNizszN NVHicpE4W0GQR1XS
SAS MkPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonZTWM2OD1yLkS4N|k5KM7:TR?= Ml\PV2FPT0WU
NCI-H2126 NXGwRVRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHFfHIxUUN3ME2wMlUyQTJ4IN88US=> NWftZo1wW0GQR1XS
NCI-H358 MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluxTWM2OD1yLkWzNlEh|ryP NUHDUGxlW0GQR1XS
FADU Mnu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvOUo9KSzVyPUCuOVQ1ODRizszN MnjzV2FPT0WU
ACN NFPPSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHDTWM2OD1yLkW1NFk1KM7:TR?= Mn[2V2FPT0WU
HCC70 NX;XV2hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLXOFZWUUN3ME2wMlU4PjZzIN88US=> Mmr1V2FPT0WU
NCI-H1838 NXrwNIN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnRTWM2OD1yLk[wNlk6KM7:TR?= M13oNHNCVkeHUh?=
CAL-54 MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjLTWM2OD1yLk[xOlIyKM7:TR?= NVHXWHBXW0GQR1XS
NCI-H1975 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonBTWM2OD1yLk[xO|I5KM7:TR?= M1jjZnNCVkeHUh?=
COR-L88 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDiTWM2OD1yLk[0NVE{KM7:TR?= Mly5V2FPT0WU
CTV-1 M1WzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2xUIYyUUN3ME2wMlY1Ozl{IN88US=> NIP1bnRUSU6JRWK=
EW-18 Mk\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrHTHRKSzVyPUCuOlg3QThizszN NF2xeWJUSU6JRWK=
HCC1806 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Dwb2lEPTB;MD62PVY3PiEQvF2= M1rsSnNCVkeHUh?=
HuP-T4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nZemlEPTB;MD62PVc3KM7:TR?= NG\jO3lUSU6JRWK=
MDA-MB-361 M2Thfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXoeoJpUUN3ME2wMlczPjZ{IN88US=> MoGxV2FPT0WU
NCI-H1573 M2jXZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVewW2t[UUN3ME2wMlc{PjNizszN M{DZ[3NCVkeHUh?=
KU-19-19 MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonoTWM2OD1yLke3OFY1KM7:TR?= NI\PcoVUSU6JRWK=
COLO-678 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TWSWlEPTB;MD64NFg{PCEQvF2= MnvaV2FPT0WU
C-33-A MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwOEGyPVch|ryP M1\XNHNCVkeHUh?=
Calu-3 M2DhXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwOEG0N|Qh|ryP MXHTRW5ITVJ?
AGS NEjEe|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXZOGRwUUN3ME2wMlg{PjR6IN88US=> MWXTRW5ITVJ?
SCC-25 M2\1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwOESxO|Eh|ryP MmL2V2FPT0WU
JVM-2 NF\SdYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTvfWxuUUN3ME2wMlg5Ojl7IN88US=> NFXLSGdUSU6JRWK=
HCE-T MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fDcmlEPTB;MD64PFQzQCEQvF2= M{Xme3NCVkeHUh?=
ES4 NVLyb444T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwOUe4N|Yh|ryP M3XmdHNCVkeHUh?=
EKVX MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\HV5BKSzVyPUGuNFExPjRizszN Ml\NV2FPT0WU
D-542MG M3XMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLpTWM2OD1zLkCxNFY1KM7:TR?= NX3oUXY4W0GQR1XS
SW1116 NXfleJY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwMEGyPFch|ryP MYLTRW5ITVJ?
5637 M2DZ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW2[pBKSzVyPUGuNFE2OSEQvF2= MnTKV2FPT0WU
HT-1376 M1OxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwMEG1NVMh|ryP Mn7pV2FPT0WU
NB69 Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nGOWlEPTB;MT6wNlk1PSEQvF2= MWnTRW5ITVJ?
YKG-1 NWDMUZl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[wcWlEPTB;MT6wOVQyQSEQvF2= NFH5R2RUSU6JRWK=
EW-3 NWPNO4hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnsNIZKSzVyPUGuNFc5QDNizszN M{m0WnNCVkeHUh?=
GCIY NF3yd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXxTWM2OD1zLkC4NVA1KM7:TR?= M2jDWHNCVkeHUh?=
SK-MES-1 NHX6WXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;BdWlEPTB;MT6xNVQ5PyEQvF2= NYPGNIU6W0GQR1XS
PANC-08-13 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzKTWM2OD1zLkG2OFE3KM7:TR?= NWnKT|JTW0GQR1XS
SK-NEP-1 MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DUb2lEPTB;MT6xO|UyOyEQvF2= M365O3NCVkeHUh?=
SW954 NHj5dFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3wTWM2OD1zLkKwNlE1KM7:TR?= M{K1RXNCVkeHUh?=
NCI-SNU-5 NYr3e|JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tnb2lEPTB;MT6yN|kh|ryP M4Pse3NCVkeHUh?=
SW48 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:zWWlEPTB;MT6yOVQ{OiEQvF2= NWLJR5kxW0GQR1XS
HT-3 NIfLfYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLaTWM2OD1zLkK4O|U{KM7:TR?= MVjTRW5ITVJ?
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Mewo MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn4TWM2OD1|ND6xN|Q6KM7:TR?= M1zNSXNCVkeHUh?=
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KM-H2 NWX1R4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTseY5KSzVyPUO0MlE4PzlizszN NWrBVYUxW0GQR1XS
NCI-H2122 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPXXJFKSzVyPUO0MlM1PzFizszN M4O4RnNCVkeHUh?=
ABC-1 Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\zW2lEPTB;M{SuN|Y6OyEQvF2= M3jzS3NCVkeHUh?=
NCI-H1355 NV;3[3RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjHXHVnUUN3ME2zOE4{QDh7IN88US=> NIflVmVUSU6JRWK=
NOMO-1 NXPje|d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3YTWM2OD1|ND61O|A{KM7:TR?= MU\TRW5ITVJ?
MZ7-mel NFXmSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnyeHZbUUN3ME2zOE43PDh5IN88US=> NXP2S45IW0GQR1XS
NCI-H810 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN2LkeyO|gh|ryP NInu[mVUSU6JRWK=
D-392MG NFe4Z29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW5TWM2OD1|NT6wOVY2KM7:TR?= NE\nT3ZUSU6JRWK=
LB771-HNC M3P2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32wNGlEPTB;M{WuNVY2QCEQvF2= NFfyfVBUSU6JRWK=
COLO-679 NGDsdJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m3XmlEPTB;M{WuN|g5KM7:TR?= MnL2V2FPT0WU
SK-PN-DW NVfY[IYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN3LkSzOlkh|ryP NXLOPIhDW0GQR1XS
VA-ES-BJ NInIS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TPemlEPTB;M{WuOFY1QSEQvF2= M{fvV3NCVkeHUh?=
KNS-42 MmfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV63WVlEUUN3ME2zOU42QDJ4IN88US=> NHO1TJRUSU6JRWK=
RVH-421 NWXIVnBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN3Lke2OFUh|ryP NWLENVNqW0GQR1XS
P30-OHK M3;FVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjFUW9tUUN3ME2zOU45PzV{IN88US=> MYTTRW5ITVJ?
G-402 NFH1RYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XjZmlEPTB;M{WuPVg3PyEQvF2= M4Xv[XNCVkeHUh?=
S-117 NGPNNXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fqemlEPTB;M{[uN|AxQCEQvF2= NWj1bZdHW0GQR1XS
RXF393 M3LxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHZN|Q1UUN3ME2zOk4{Pzh3IN88US=> NUDhdodvW0GQR1XS
LCLC-103H M1fMRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXFTWM2OD1|Nj63PFA{KM7:TR?= MXfTRW5ITVJ?
U-118-MG M{frb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPETWM2OD1|Nj64PFQ4KM7:TR?= NUjH[pJ4W0GQR1XS
8-MG-BA Ml[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTN4Lkm0PFMh|ryP M4flSnNCVkeHUh?=
MFH-ino NITxdZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTN5LkOzO|Eh|ryP NInOeolUSU6JRWK=
NCI-H23 M2fWTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fUXmlEPTB;M{euOFE6PiEQvF2= Ml3GV2FPT0WU
NCI-H446 M2PxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;Od3N5UUN3ME2zO{41QDZ{IN88US=> NWe0[nY5W0GQR1XS
LU-99A MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN5LkW3N|Eh|ryP M{nlRnNCVkeHUh?=
KP-N-YN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvZTWM2OD1|Nz62NVk2KM7:TR?= NIn1Z3lUSU6JRWK=
SCC-9 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTN5Lke4N|gh|ryP M2nneXNCVkeHUh?=
EFM-19 M2[5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH0XppKSzVyPUO3Mlc6PjdizszN M4L4VnNCVkeHUh?=
A427 NXP0V2FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mom3TWM2OD1|Nz65NVA4KM7:TR?= MVnTRW5ITVJ?
LB831-BLC NVjj[GNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFezZ4VKSzVyPUO4MlYxOzlizszN NHW4VGtUSU6JRWK=
HOS M13zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX2bnVCUUN3ME2zPU43Ojd|IN88US=> M3rVRXNCVkeHUh?=
LAN-6 NF\hXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljTTWM2OD12MD6wNVEzKM7:TR?= MkfGV2FPT0WU
U251 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jsUmlEPTB;NECuOFA2PCEQvF2= MkHkV2FPT0WU
SNU-387 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDsTWM2OD12MD60OVU{KM7:TR?= MkTsV2FPT0WU
DMS-79 M1PrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHNZnpxUUN3ME20NE42QDh7IN88US=> Ml7jV2FPT0WU
SK-LU-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfDOlF7UUN3ME20NE43PTZ6IN88US=> MWnTRW5ITVJ?
HT NH:2fWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq0Wml[UUN3ME20NE43PjN7IN88US=> MWjTRW5ITVJ?
KP-N-YS M2G0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPnc2dKUUN3ME20NE43PzZ6IN88US=> MWHTRW5ITVJ?
DMS-114 MnT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLFe|FKSzVyPUSwMlg{PzRizszN M3XsUHNCVkeHUh?=
HUTU-80 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:3d2lEPTB;NEGuNFU3QSEQvF2= NWPhR5lVW0GQR1XS
ONS-76 NXy1dYRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTRzLkS3NFkh|ryP NYHOPGx{W0GQR1XS
A673 NWf1[ZkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT2TWM2OD12MT61NVU4KM7:TR?= MWLTRW5ITVJ?
HPAF-II M3rnb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTRzLk[3NFkh|ryP Ml3GV2FPT0WU
UACC-257 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\JTWM2OD12MT63N|Y6KM7:TR?= NWDBVGlGW0GQR1XS
EW-22 M{jQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTRzLki2PVch|ryP MkHsV2FPT0WU
NCI-H1755 NVTnSYxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXvTWM2OD12MT64O|I2KM7:TR?= NYKzSmhMW0GQR1XS
KYSE-150 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e1cGlEPTB;NEKuNVc5OiEQvF2= M4jRenNCVkeHUh?=
CGTH-W-1 MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP2[JhKSzVyPUSyMlQ6PTVizszN MUPTRW5ITVJ?
NB13 NVrJeoNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFntNWZKSzVyPUSyMlYzOTdizszN NYPqPHlQW0GQR1XS
SW872 M{D2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnO4TWM2OD12Mj62N|MyKM7:TR?= M4HvSXNCVkeHUh?=
KP-4 NFn1XIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\xUWlEPTB;NEKuPFg{OiEQvF2= M1nLenNCVkeHUh?=
HCC38 NYHyR3pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XCXGlEPTB;NEKuPVYyQCEQvF2= NXfiTnVmW0GQR1XS
BB49-HNC NEm3Z4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTR|LkKzOVYh|ryP M3;4cXNCVkeHUh?=
CAL-62 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3zTY1SUUN3ME20N{41ODJ6IN88US=> M3vWUXNCVkeHUh?=
NCI-H2029 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTR|LkW1PFEh|ryP MVHTRW5ITVJ?
M14 MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR2LkGzN|Ih|ryP NVe2[YZwW0GQR1XS
COLO-680N NV;IVlUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHtVVBKSzVyPUS0MlM{QSEQvF2= Ml70V2FPT0WU
Hs-578-T NHTMc3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnNVYZKSzVyPUS1MlAzQTRizszN Mmf2V2FPT0WU
MSTO-211H NVjlUYhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H1[2lEPTB;NEWuPVQ5OiEQvF2= M37zc3NCVkeHUh?=
EW-1 MmP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHOV4ZKSzVyPUS1Mlk3QDlizszN NXK5OoFvW0GQR1XS
SW948 NFrHUWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUK2[FBDUUN3ME20Ok41PDZ{IN88US=> M2TuS3NCVkeHUh?=
NCI-H460 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTR4LkWyN{DPxE1? MlviV2FPT0WU
CAS-1 NHfQe5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTR4Lke3NFEh|ryP NIjoPFFUSU6JRWK=
TGBC11TKB MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO4TWM2OD12Nz6xO|c4KM7:TR?= NYWyOJo6W0GQR1XS
HD-MY-Z NWTycoQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGm2TVNKSzVyPUS4Mlc5PiEQvF2= MnvyV2FPT0WU
NCI-H226 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\RZZVKSzVyPUS5Mlc4QDVizszN M1m5XXNCVkeHUh?=
PA-1 MkjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnW[FVkUUN3ME20PU45OzN3IN88US=> MUXTRW5ITVJ?
LB2518-MEL M17GNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr5U4FKSzVyPUS5Mlg4OjNizszN MnT5V2FPT0WU
A101D M4jjfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR7Lkm0NlUh|ryP MlnKV2FPT0WU
NCI-H2087 NWXpRo5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTR7Lkm2PFIh|ryP MXnTRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 485.94
化学式

C24H25ClFN5O3

CAS No. 439081-18-2
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02795156 Recruiting Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer September 28, 2016 Phase 2
NCT03054038 Not yet recruiting Non-Small Cell Lung Carcinoma Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) February 2017 Phase 1
NCT02979977 Not yet recruiting Squamous Cell Cancers of the Head and Neck Aarti Bhatia|National Comprehensive Cancer Network|Boehringer Ingelheim|Yale University December 2016 Phase 2
NCT02876081 Not yet recruiting SMALL CELL LUNG CARCINOMA Groupe Hospitalier Paris Saint Joseph December 2016 Phase 2
NCT02183883 Recruiting Non-small Cell Lung Cancer University College, London|Boehringer Ingelheim December 2016 Phase 2
NCT02423525 Recruiting Brain Cancer Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute October 2016 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

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

  • 回答:

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

EGFRシグナル伝達経路

EGFR Inhibitors with Unique Features

相関EGFR製品

Tags: Afatinib (BIBW2992)を買う | Afatinib (BIBW2992) ic50 | Afatinib (BIBW2992)供給者 | Afatinib (BIBW2992)を購入する | Afatinib (BIBW2992)費用 | Afatinib (BIBW2992)生産者 | オーダーAfatinib (BIBW2992) | Afatinib (BIBW2992)化学構造 | Afatinib (BIBW2992)分子量 | Afatinib (BIBW2992)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID