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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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 NXX2NZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLlNW1KSzVyPUCuNFA2PzJizszN NV7qfplJW0GQR1XS
KASUMI-1 NIiwcpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PwXmlEPTB;MD6wNFkyOSEQvF2= MWPTRW5ITVJ?
HCC2218 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fVVGlEPTB;MD6wNFk5PyEQvF2= MWjTRW5ITVJ?
KARPAS-45 M{izcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\KOGlEPTB;MD6wNVY4OSEQvF2= MUTTRW5ITVJ?
HSC-4 NF\ISFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoflTWM2OD1yLkCxO|Q5KM7:TR?= MnzaV2FPT0WU
CHL-1 M{mzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf0TWM2OD1yLkCxPFM6KM7:TR?= Ml\BV2FPT0WU
KY821 M3rGZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7BTWM2OD1yLkCyNFYh|ryP NFPmeI5USU6JRWK=
NCI-N87 NHex[WFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\vbmlEPTB;MD6wNlc4OyEQvF2= NFPx[GpUSU6JRWK=
DOK NUnWOotnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nYO2lEPTB;MD6wN|E6PCEQvF2= MVjTRW5ITVJ?
DSH1 NGrBSZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwMEOzNVQh|ryP M4XPbHNCVkeHUh?=
MDA-MB-175-VII M1jqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXezO4NnUUN3ME2wMlA{PDF4IN88US=> NYX6NoZOW0GQR1XS
NCI-H2170 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMEO3Nlgh|ryP MVnTRW5ITVJ?
BT-474 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwMES5PFYh|ryP MmLMV2FPT0WU
EFO-27 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L0V2lEPTB;MD6wOVE5OiEQvF2= NW\6clFVW0GQR1XS
NCI-H720 NED3UGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\OcWtXUUN3ME2wMlA2OzJ3IN88US=> MYnTRW5ITVJ?
PC-14 NES2Z4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwMEW2Olgh|ryP M{i4NnNCVkeHUh?=
EC-GI-10 M1u4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMEW5NVIh|ryP NV3xUGZzW0GQR1XS
KYSE-450 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe2XGFKSzVyPUCuNFU6PzhizszN NHn3PW1USU6JRWK=
BPH-1 NUL0WpdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMEW5PFgh|ryP NWG3Ro1IW0GQR1XS
NCI-H292 M{\LTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjiO3lKSzVyPUCuNFYxQSEQvF2= M{fmdHNCVkeHUh?=
H9 NYnvUXN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7mW4lKSzVyPUCuNFcyOzJizszN M2TacHNCVkeHUh?=
NCI-H526 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHDXWl6UUN3ME2wMlA4QDJ|IN88US=> MkjpV2FPT0WU
NCI-H1623 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke1TWM2OD1yLkC4NFI2KM7:TR?= NVPpS2x[W0GQR1XS
KYSE-140 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Tn[2lEPTB;MD6wPFM{KM7:TR?= NIfL[nVUSU6JRWK=
Ca9-22 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\WTWM2OD1yLkC4N|U{KM7:TR?= NHz5ZoVUSU6JRWK=
AU565 NX;YOG83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwMEi1NFQh|ryP NH\KU2tUSU6JRWK=
ZR-75-30 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwMEm1OFUh|ryP M3H4OnNCVkeHUh?=
NCI-H1770 NXK0UpZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjXTWM2OD1yLkGwNlgh|ryP MXPTRW5ITVJ?
LB2241-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfBTWM2OD1yLkGwPFg1KM7:TR?= MYjTRW5ITVJ?
CAL-39 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnj4TWM2OD1yLkGxO|kzKM7:TR?= MkXPV2FPT0WU
UACC-893 NV\PPG5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwMUG4PFUh|ryP NIjVfGdUSU6JRWK=
LU-65 NUTXboliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwMUK2N|Mh|ryP M3XFdXNCVkeHUh?=
HN M3;NZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTn[pF1UUN3ME2wMlE{ODd5IN88US=> Mlq0V2FPT0WU
TI-73 NFrCR29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHSTWM2OD1yLkG0O|E2KM7:TR?= MnHNV2FPT0WU
KU812 M2LuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvRTWM2OD1yLkG1OFU3KM7:TR?= MXzTRW5ITVJ?
SW13 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMU[yNVYh|ryP NXnpWXFjW0GQR1XS
BB30-HNC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXkV4dKSzVyPUCuNVY2PzZizszN Mkf0V2FPT0WU
HSC-2 M{LoO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXZTWM2OD1yLkG2PFM4KM7:TR?= NGrBUJNUSU6JRWK=
BV-173 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMUe1PVYh|ryP NYHMZWlbW0GQR1XS
CAL-27 M2riOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDWTWM2OD1yLkG3OlM3KM7:TR?= MnLCV2FPT0WU
SBC-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HOSmlEPTB;MD6xPFk2QSEQvF2= Ml3XV2FPT0WU
CAL-33 M4fmW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[xTWM2OD1yLkKwNVg1KM7:TR?= NHnp[pRUSU6JRWK=
NCI-H209 NXLzOYpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV6wNHF3UUN3ME2wMlIxPDZizszN NWrZSJYyW0GQR1XS
COR-L105 NYnJVVBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXJU5BKSzVyPUCuNlExQDRizszN NVT5NYlZW0GQR1XS
HSC-3 NWXuTVJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jSN2lEPTB;MD6yNVE6QCEQvF2= M3PXTXNCVkeHUh?=
NCI-H69 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LDfWlEPTB;MD6yNVQ2OSEQvF2= M4K3[nNCVkeHUh?=
MOLT-13 NYHYNpp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorvTWM2OD1yLkKzPVc2KM7:TR?= MV;TRW5ITVJ?
ML-2 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGS4WnlKSzVyPUCuNlQ5ODJizszN MVfTRW5ITVJ?
IGROV-1 M4\GVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fwZWlEPTB;MD6yOVk2OiEQvF2= MkT6V2FPT0WU
TK10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:wTWM2OD1yLkK2O|M5KM7:TR?= MlnJV2FPT0WU
EoL-1-cell Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rJVGlEPTB;MD6yOlg6OiEQvF2= MVnTRW5ITVJ?
HO-1-N-1 NVHnTmFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXThVVY{UUN3ME2wMlI4QDV|IN88US=> MYTTRW5ITVJ?
BHY M{Pve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvVcZZKSzVyPUCuNlg3PTVizszN M4T0[3NCVkeHUh?=
LU-139 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37LXGlEPTB;MD6zNFUyKM7:TR?= NILOe5dUSU6JRWK=
23132-87 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3jdWdKSzVyPUCuN|E6OjNizszN NY\qT4N1W0GQR1XS
ACHN MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwM{G5PVQh|ryP MULTRW5ITVJ?
DoTc2-4510 NV\oV5RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwM{KyNVkh|ryP Ml3PV2FPT0WU
BB65-RCC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PRdGlEPTB;MD6zOFU6OyEQvF2= MWTTRW5ITVJ?
HLE NHHRelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD2TWM2OD1yLkO1NFQ3KM7:TR?= Mn;oV2FPT0WU
HCC1419 MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3yxOGlEPTB;MD6zOlQxQCEQvF2= NIPIeIJUSU6JRWK=
A388 NUXw[5NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTFUHc2UUN3ME2wMlM3QDV5IN88US=> M4jEc3NCVkeHUh?=
NUGC-3 NVHRVVZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwM{izO|Mh|ryP NVXFfIg4W0GQR1XS
KYSE-180 M3jDWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDVe2ZKSzVyPUCuN|kxQDlizszN NGjMSXpUSU6JRWK=
TE-6 NVLDblNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPjZWJKSzVyPUCuOFAzPDZizszN M2rCNHNCVkeHUh?=
A498 NEXmOHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\oTWM2OD1yLkSwOlc1KM7:TR?= NEXNdY1USU6JRWK=
NCI-H1648 NF3CVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknoTWM2OD1yLkS0NVgzKM7:TR?= NH7Nc2dUSU6JRWK=
DU-145 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwNES4N|Mh|ryP MV3TRW5ITVJ?
CW-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L1S2lEPTB;MD60OlkyPCEQvF2= MYrTRW5ITVJ?
A431 M3nYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwNEiyN|Mh|ryP Ml35V2FPT0WU
SAS NX;IeHJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHxV2hMUUN3ME2wMlQ5Ozl6IN88US=> M4LHcXNCVkeHUh?=
NCI-H2126 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnucoNKSzVyPUCuOVE6OjZizszN MVjTRW5ITVJ?
NCI-H358 MkLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHwTldKSzVyPUCuOVMzOSEQvF2= MmnqV2FPT0WU
FADU MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPsWYJKSzVyPUCuOVQ1ODRizszN NGG2S5dUSU6JRWK=
ACN NX\JW5p2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNUWwPVQh|ryP M1niTnNCVkeHUh?=
HCC70 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrqNmJKSzVyPUCuOVc3PjFizszN MnjyV2FPT0WU
NCI-H1838 NUnEclZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwNkCyPVkh|ryP Mkf5V2FPT0WU
CAL-54 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnj[XY1UUN3ME2wMlYyPjJzIN88US=> MVLTRW5ITVJ?
NCI-H1975 NFfHTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVKwOoh1UUN3ME2wMlYyPzJ6IN88US=> NXLWe3ZkW0GQR1XS
COR-L88 M1rvdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnKTWM2OD1yLk[0NVE{KM7:TR?= NWqy[2pCW0GQR1XS
CTV-1 M4W0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XZVWlEPTB;MD62OFM6OiEQvF2= NFLkRYpUSU6JRWK=
EW-18 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\YTWM2OD1yLk[4Olk5KM7:TR?= NYDU[nloW0GQR1XS
HCC1806 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNkm2OlYh|ryP NEnMNIpUSU6JRWK=
HuP-T4 NIexWXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwNkm3OkDPxE1? MnXXV2FPT0WU
MDA-MB-361 MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwN{K2OlIh|ryP NVvFUlFtW0GQR1XS
NCI-H1573 NUPwR5VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL2TWM2OD1yLkezOlMh|ryP M2XxZnNCVkeHUh?=
KU-19-19 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjDXHFKSzVyPUCuO|c1PjRizszN NGS4S4hUSU6JRWK=
COLO-678 MnjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwOEC4N|Qh|ryP MWHTRW5ITVJ?
C-33-A M17U[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwOEGyPVch|ryP MUfTRW5ITVJ?
Calu-3 NELFeXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfWTWM2OD1yLkixOFM1KM7:TR?= MVHTRW5ITVJ?
AGS NGK0PINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHVTWM2OD1yLkizOlQ5KM7:TR?= Mn\hV2FPT0WU
SCC-25 MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\0TWM2OD1yLki0NVcyKM7:TR?= NHvMO|lUSU6JRWK=
JVM-2 MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrDNGhkUUN3ME2wMlg5Ojl7IN88US=> NIDEfWhUSU6JRWK=
HCE-T NXTlWJN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwOEi0Nlgh|ryP M13uNnNCVkeHUh?=
ES4 M1nQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjCNYxKSzVyPUCuPVc5OzZizszN NUezOWZDW0GQR1XS
EKVX MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37iWmlEPTB;MT6wNVA3PCEQvF2= MWrTRW5ITVJ?
D-542MG MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDoTWM2OD1zLkCxNFY1KM7:TR?= M3OwTXNCVkeHUh?=
SW1116 M{LtSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\ldFZKSzVyPUGuNFEzQDdizszN M{SzVXNCVkeHUh?=
5637 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfGRY1KSzVyPUGuNFE2OSEQvF2= NUmzd3F5W0GQR1XS
HT-1376 MoXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfN[4ZSUUN3ME2xMlAyPTF|IN88US=> MVrTRW5ITVJ?
NB69 NYniPY5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PRfmlEPTB;MT6wNlk1PSEQvF2= M1HmNHNCVkeHUh?=
YKG-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTFwMEW0NVkh|ryP MlPrV2FPT0WU
EW-3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwMEe4PFMh|ryP NVrIS4tIW0GQR1XS
GCIY NXHKV5N5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn0XWFKSzVyPUGuNFgyODRizszN NWjtVGt4W0GQR1XS
SK-MES-1 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jIWWlEPTB;MT6xNVQ5PyEQvF2= NVm2eG14W0GQR1XS
PANC-08-13 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\KT5JKSzVyPUGuNVY1OTZizszN MmjMV2FPT0WU
SK-NEP-1 NFL4e21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rlcWlEPTB;MT6xO|UyOyEQvF2= MnP6V2FPT0WU
SW954 NVfINopsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS5WYF5UUN3ME2xMlIxOjF2IN88US=> NHy0WVdUSU6JRWK=
NCI-SNU-5 NYDGdJYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDSVpFDUUN3ME2xMlI{QSEQvF2= MWHTRW5ITVJ?
SW48 MkDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjrdYJHUUN3ME2xMlI2PDN{IN88US=> MYPTRW5ITVJ?
HT-3 NIrRZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnnTWM2OD1zLkK4O|U{KM7:TR?= MoHhV2FPT0WU
ETK-1 NFywb2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnYdHdEUUN3ME2xMlM4PDV4IN88US=> NVjodpYxW0GQR1XS
SCC-15 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXvWGVKSzVyPUGuN|k1PTFizszN NXnJNJVzW0GQR1XS
DU-4475 NYjRXYhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r5[GlEPTB;MT60NFEzOSEQvF2= M4HKZnNCVkeHUh?=
NB5 NY\3So1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTFwNEGzNVch|ryP MV3TRW5ITVJ?
CFPAC-1 NFrWeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTqTWM2OD1zLkSyOFk{KM7:TR?= M3HQdnNCVkeHUh?=
NCI-H630 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTvTWM2OD1zLkS1OVgzKM7:TR?= MljuV2FPT0WU
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D-502MG M1LSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PvT2lEPTB;OD6yPVI5OiEQvF2= MUDTRW5ITVJ?
NCI-H1993 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjSfWNKSzVyPUiuN|M3OzFizszN M1nWdnNCVkeHUh?=
SCC-4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[4UmlEPTB;OD60OFA2QSEQvF2= M4H5NHNCVkeHUh?=
HAL-01 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2i1RWlEPTB;OD61NVkyKM7:TR?= NVLq[oJGW0GQR1XS
GT3TKB Mk\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrNTWM2OD16Lk[3PVY1KM7:TR?= M1zUXXNCVkeHUh?=
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COLO-829 NED4dWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrNPWozUUN3ME24MlgxQTd4IN88US=> MmjEV2FPT0WU
OCI-AML2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnYVIkyUUN3ME24Mlk2PDhzIN88US=> M3\PTHNCVkeHUh?=
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BFTC-909 NXLmNmozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS3eVNHUUN3ME25MlA3Pzl7IN88US=> NVfIOVhkW0GQR1XS
EW-11 NHvGNJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LqVGlEPTB;OT6xO|Y2OyEQvF2= NHvnO5lUSU6JRWK=
HCE-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLtN|FuUUN3ME25MlIyPTV6IN88US=> Mny0V2FPT0WU
BALL-1 NH\yOJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzHbJNLUUN3ME25MlIyQTB5IN88US=> Ml\zV2FPT0WU
SF539 M2Ljfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHuTWM2OD17LkKzOVYzKM7:TR?= MWDTRW5ITVJ?
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C32 MmjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nub2lEPTB;OT6zN|A3PCEQvF2= MYTTRW5ITVJ?
NCI-H1703 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DzNWlEPTB;OT6zOFM4PSEQvF2= MlryV2FPT0WU
NCI-H1650 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzSfGhwUUN3ME25MlYxQTR4IN88US=> MVvTRW5ITVJ?
NCI-H1563 M3[2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TlcWlEPTB;OT63OlA{OSEQvF2= NHrOSoFUSU6JRWK=
CAL-85-1 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfVbHZNUUN3ME25Mlg4Ozh|IN88US=> NX7hc|RYW0GQR1XS
UM-UC-3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[zXGlEPTB;OT65OVA{KM7:TR?= Ml7FV2FPT0WU
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HuCCT1 NVXJS5NpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3wTWM2OD1zMD62NFM{KM7:TR?= MXPTRW5ITVJ?
OVCAR-4 MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ReWlEPTB;MUCuPFg{PSEQvF2= M3yyOHNCVkeHUh?=
CAL-72 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17zXmlEPTB;MUCuPVM6OSEQvF2= NHjmVXBUSU6JRWK=
HCC1954 NVzNNYZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInOTXFKSzVyPUGxMlA4PTRizszN MYPTRW5ITVJ?
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FTC-133 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVOwWlVIUUN3ME2xNU4yPDB5IN88US=> M1ztTnNCVkeHUh?=
SK-MEL-24 NH7ETFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\Ud2lKSzVyPUGxMlI{PjZizszN NGWzcGNUSU6JRWK=
UACC-62 MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W0RmlEPTB;MUGuNlM3QCEQvF2= MYjTRW5ITVJ?
NCI-H650 NXXIO41NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTFzLkK0NVgh|ryP M3LRdnNCVkeHUh?=
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RPMI-2650 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\kTWM2OD1zMT61PFg2KM7:TR?= NEO0[IFUSU6JRWK=
MC-IXC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;1[3RWUUN3ME2xNU43PzJ6IN88US=> M1nOSXNCVkeHUh?=
HOP-62 NWDzTnhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFzLk[3OlQh|ryP MUTTRW5ITVJ?
NOS-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fVU2lEPTB;MUGuO|ExQSEQvF2= M{G1bnNCVkeHUh?=
SW1573 NVz4eXVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW2TWM2OD1zMT63Nlk2KM7:TR?= NFzxeldUSU6JRWK=
WM-115 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n2b2lEPTB;MUGuO|U5QCEQvF2= MVjTRW5ITVJ?
HuO9 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvOXY1KSzVyPUGxMlg4PzRizszN NEXjTWFUSU6JRWK=
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NCI-H596 Ml7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDEO4FDUUN3ME2xNk4xOzZ7IN88US=> M2CyfXNCVkeHUh?=
A172 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[xTWM2OD1zMj6wO|k5KM7:TR?= M2DUPXNCVkeHUh?=
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SW837 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF{LkmwNlgh|ryP Mom4V2FPT0WU
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PFSK-1 NIXQflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF|LkC2JO69VQ>? MWfTRW5ITVJ?
DBTRG-05MG NV\VNnpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fqeWlEPTB;MUOuNFY{OiEQvF2= M1vJcXNCVkeHUh?=
SK-UT-1 NITBOpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF|LkGwPFMh|ryP M2\ESHNCVkeHUh?=
OVCAR-5 MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTF|LkG1PVMh|ryP M2i0TXNCVkeHUh?=
8505C MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOwOIlOUUN3ME2xN{4zODZ5IN88US=> NXqwUpI6W0GQR1XS
SK-MEL-1 M1q5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLKfGZKSzVyPUGzMlcyOzVizszN M1jOcnNCVkeHUh?=
LK-2 M{P4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7CTWM2OD1zMz63OlM6KM7:TR?= MX;TRW5ITVJ?
OE33 NFfFZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF|Lke4OkDPxE1? NV3yW2ZuW0GQR1XS
Ramos-2G6-4C10 NFnHc29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv4UVk{UUN3ME2xOE4xOjB{IN88US=> MV7TRW5ITVJ?
EW-13 NE\sV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF2LkCzOVIh|ryP NFj6ZmxUSU6JRWK=
NCI-H1793 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXtemJKSzVyPUG0MlIxQDdizszN M3HEOnNCVkeHUh?=
BHT-101 M2X0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HRSmlEPTB;MUSuNlQyKM7:TR?= NXzyWG5[W0GQR1XS
RKO M17Kbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTyWVRyUUN3ME2xOE42ODd3IN88US=> NGrzWItUSU6JRWK=
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PANC-10-05 NF;vNWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHFTWM2OD1zND62NlQ4KM7:TR?= NXrhfo9nW0GQR1XS
NCI-H2030 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fjbGlEPTB;MUSuOlQ1QCEQvF2= NGTaWYlUSU6JRWK=
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NCI-H1092 NWPGSIdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BeIdSUUN3ME2xOk45OzF4IN88US=> MlnrV2FPT0WU
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NCI-H2405 MmHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFuxeHpKSzVyPUG3MlE6PzRizszN MVrTRW5ITVJ?
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NCI-H2342 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF33WmdKSzVyPUG3MlU2PyEQvF2= MmnoV2FPT0WU
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D-283MED MnPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF6LkCwPFgh|ryP M{fR[3NCVkeHUh?=
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NCI-H1437 NXzFfJR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X4UWlEPTB;MUiuNVY1OSEQvF2= NXqyPXc1W0GQR1XS
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A704 NE\CfFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF6LkS3OVMh|ryP NVm1dFFWW0GQR1XS
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COLO-320-HSR M{nyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;MdmlEPTB;MUiuO|Q3KM7:TR?= MWTTRW5ITVJ?
Mo-T MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfBUFg2UUN3ME2xPE45OjB2IN88US=> NWH4SYNWW0GQR1XS
Saos-2 M4\vWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ftWmlEPTB;MUmuNVE3OiEQvF2= MVfTRW5ITVJ?
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KMOE-2 NFjhV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPj[ldTUUN3ME2xPU4zOjR{IN88US=> Mln5V2FPT0WU
MMAC-SF MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2j6SmlEPTB;MUmuNlYxPyEQvF2= Mmn2V2FPT0WU
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SK-MEL-28 NGm3[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\QXWlEPTB;MUmuN|M3OyEQvF2= NFvO[ZBUSU6JRWK=
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... 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

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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* 必須

Related EGFR 阻害剤

  • Erlotinib

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

  • Afatinib (BIBW2992) Dimaleate

    Afatinib (BIBW2992) Dimaleate 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, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Poziotinib (HM781-36B)

    Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.

  • AZ5104

    AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor. Phase 1.

  • 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.

  • Erlotinib HCl (OSI-744)

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

  • Osimertinib (AZD9291)

    AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. Phase 3.

  • 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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