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

文献中の引用(35)

カスタマーフィードバック(3)

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 NVfuXGFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPD[JdUUUN3ME2wMlAxPTd{IN88US=> MW\TRW5ITVJ?
KASUMI-1 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMEC5NVEh|ryP MknjV2FPT0WU
HCC2218 NXrpbm4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXRdnlnUUN3ME2wMlAxQTh5IN88US=> MVXTRW5ITVJ?
KARPAS-45 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH2TWM2OD1yLkCxOlcyKM7:TR?= M3rYSHNCVkeHUh?=
HSC-4 M4nwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;aUopKSzVyPUCuNFE4PDhizszN MUDTRW5ITVJ?
CHL-1 M2TyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKzTWM2OD1yLkCxPFM6KM7:TR?= M2PaWXNCVkeHUh?=
KY821 M3rDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zBUWlEPTB;MD6wNlA3KM7:TR?= MlfHV2FPT0WU
NCI-N87 NVn1WXNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXWe|dKSzVyPUCuNFI4PzNizszN NFjWd|FUSU6JRWK=
DOK NW\xPVl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Tw[GlEPTB;MD6wN|E6PCEQvF2= MoDBV2FPT0WU
DSH1 M2D0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLDU3loUUN3ME2wMlA{OzF2IN88US=> NFrhPWtUSU6JRWK=
MDA-MB-175-VII MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr3W|kxUUN3ME2wMlA{PDF4IN88US=> M3rrVHNCVkeHUh?=
NCI-H2170 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLDRmtKSzVyPUCuNFM4OjhizszN MYDTRW5ITVJ?
BT-474 MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3jcWpZUUN3ME2wMlA1QTh4IN88US=> MmTBV2FPT0WU
EFO-27 NGrDTlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy2flBKSzVyPUCuNFUyQDJizszN M2rEO3NCVkeHUh?=
NCI-H720 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnhTWM2OD1yLkC1N|I2KM7:TR?= MYrTRW5ITVJ?
PC-14 NWHFfI1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7VfXZCUUN3ME2wMlA2PjZ6IN88US=> M{LMUXNCVkeHUh?=
EC-GI-10 NH2x[lBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TXdmlEPTB;MD6wOVkyOiEQvF2= Mk[0V2FPT0WU
KYSE-450 M3XFOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXviW4J7UUN3ME2wMlA2QTd6IN88US=> NWXUVpY1W0GQR1XS
BPH-1 NVWySIV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTiOGhKSzVyPUCuNFU6QDhizszN NHnPUJBUSU6JRWK=
NCI-H292 M1LqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH4OJJKSzVyPUCuNFYxQSEQvF2= NHXsd3lUSU6JRWK=
H9 NF\QTllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;rfph1UUN3ME2wMlA4OTN{IN88US=> NHz0UnRUSU6JRWK=
NCI-H526 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwMEe4NlMh|ryP MnW4V2FPT0WU
NCI-H1623 NHvrTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzFRoxKSzVyPUCuNFgxOjVizszN MXrTRW5ITVJ?
KYSE-140 NXqye|l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPIO5BEUUN3ME2wMlA5OzNizszN M1KzfnNCVkeHUh?=
Ca9-22 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO3eoRiUUN3ME2wMlA5OzV|IN88US=> MnjBV2FPT0WU
AU565 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XwRWlEPTB;MD6wPFUxPCEQvF2= M33G[XNCVkeHUh?=
ZR-75-30 MoLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLwUJlyUUN3ME2wMlA6PTR3IN88US=> NFjMXY9USU6JRWK=
NCI-H1770 MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXETZdKSzVyPUCuNVAzQCEQvF2= MVfTRW5ITVJ?
LB2241-RCC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHaTpVKSzVyPUCuNVA5QDRizszN M2ftcnNCVkeHUh?=
CAL-39 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfOTW1KSzVyPUCuNVE4QTJizszN NUOwTHRIW0GQR1XS
UACC-893 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;KdFVKSzVyPUCuNVE5QDVizszN NF74bW5USU6JRWK=
LU-65 MlnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HWfWlEPTB;MD6xNlY{OyEQvF2= M2\OS3NCVkeHUh?=
HN MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37XOGlEPTB;MD6xN|A4PyEQvF2= MWDTRW5ITVJ?
TI-73 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPXTWM2OD1yLkG0O|E2KM7:TR?= MoLqV2FPT0WU
KU812 NYHQTpF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPJTWM2OD1yLkG1OFU3KM7:TR?= MlX1V2FPT0WU
SW13 NETDSJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7Dd5RKSzVyPUCuNVYzOTZizszN Ml3VV2FPT0WU
BB30-HNC NVLVSZdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzH[ldtUUN3ME2wMlE3PTd4IN88US=> NYHZOlg2W0GQR1XS
HSC-2 M4jQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PONWlEPTB;MD6xOlg{PyEQvF2= M2PNVXNCVkeHUh?=
BV-173 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HJXWlEPTB;MD6xO|U6PiEQvF2= MXnTRW5ITVJ?
CAL-27 NUn6WoR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq4W2tbUUN3ME2wMlE4PjN4IN88US=> NUXpZXV2W0GQR1XS
SBC-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwMUi5OVkh|ryP MoO0V2FPT0WU
CAL-33 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHjTWM2OD1yLkKwNVg1KM7:TR?= NYH2XXBvW0GQR1XS
NCI-H209 NFvQSW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn6OIFKSzVyPUCuNlA1PiEQvF2= NIX4fmpUSU6JRWK=
COR-L105 NX3mUHZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjVVnpPUUN3ME2wMlIyODh2IN88US=> NHLN[4RUSU6JRWK=
HSC-3 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofKTWM2OD1yLkKxNVk5KM7:TR?= NX:1boJvW0GQR1XS
NCI-H69 NUi3[WlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrjbJRKSzVyPUCuNlE1PTFizszN MUXTRW5ITVJ?
MOLT-13 NEm1V3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwMkO5O|Uh|ryP MUnTRW5ITVJ?
ML-2 NWWxO29ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjwT|F5UUN3ME2wMlI1QDB{IN88US=> MXTTRW5ITVJ?
IGROV-1 M4e5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvaTWM2OD1yLkK1PVUzKM7:TR?= NIjJRo1USU6JRWK=
TK10 NV3KVodmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TyUmlEPTB;MD6yOlc{QCEQvF2= MkO3V2FPT0WU
EoL-1-cell MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrWR5hKSzVyPUCuNlY5QTJizszN NYnTe5l5W0GQR1XS
HO-1-N-1 M2fDPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlixTWM2OD1yLkK3PFU{KM7:TR?= M2e1THNCVkeHUh?=
BHY Mn[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX5b2VUUUN3ME2wMlI5PjV3IN88US=> NXGzZ|ZXW0GQR1XS
LU-139 NXzrcmtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH6TWM2OD1yLkOwOVEh|ryP M1\CR3NCVkeHUh?=
23132-87 M3;Kb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS2TWM2OD1yLkOxPVI{KM7:TR?= M2PROHNCVkeHUh?=
ACHN Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nDeGlEPTB;MD6zNVk6PCEQvF2= NUP4bW5JW0GQR1XS
DoTc2-4510 NH7ufVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwM{KyNVkh|ryP MVzTRW5ITVJ?
BB65-RCC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfuTWM2OD1yLkO0OVk{KM7:TR?= MmHaV2FPT0WU
HLE MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHD[WtEUUN3ME2wMlM2ODR4IN88US=> NIWxeopUSU6JRWK=
HCC1419 M{i1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfLWGhKSzVyPUCuN|Y1ODhizszN M1ztTXNCVkeHUh?=
A388 NVHUepV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPPbJBKSzVyPUCuN|Y5PTdizszN M1e4NXNCVkeHUh?=
NUGC-3 NVu1bnJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwM{izO|Mh|ryP MWrTRW5ITVJ?
KYSE-180 NUHwU2R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfpN3hIUUN3ME2wMlM6ODh7IN88US=> MUHTRW5ITVJ?
TE-6 M1LIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwNECyOFYh|ryP MYjTRW5ITVJ?
A498 NUnreIxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DkSGlEPTB;MD60NFY4PCEQvF2= MYDTRW5ITVJ?
NCI-H1648 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwNESxPFIh|ryP MnS3V2FPT0WU
DU-145 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD0VpFQUUN3ME2wMlQ1QDN|IN88US=> NGDlbXJUSU6JRWK=
CW-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi0ZpQxUUN3ME2wMlQ3QTF2IN88US=> MkHsV2FPT0WU
A431 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rDU2lEPTB;MD60PFI{OyEQvF2= NX\mNldwW0GQR1XS
SAS M4DZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwNEizPVgh|ryP MmXiV2FPT0WU
NCI-H2126 NWL1d|JIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jSWmlEPTB;MD61NVkzPiEQvF2= NH3D[WNUSU6JRWK=
NCI-H358 M4nNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjreHZuUUN3ME2wMlU{OjFizszN Mn;OV2FPT0WU
FADU MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUWyToV2UUN3ME2wMlU1PDB2IN88US=> NULPdWxHW0GQR1XS
ACN NVG4U5RzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwNUWwPVQh|ryP MV3TRW5ITVJ?
HCC70 MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwNUe2OlEh|ryP NYG5PJBLW0GQR1XS
NCI-H1838 NHLkUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrDTZpKSzVyPUCuOlAzQTlizszN NUPUNJFDW0GQR1XS
CAL-54 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\RWWlEPTB;MD62NVYzOSEQvF2= MWTTRW5ITVJ?
NCI-H1975 NGq4XHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XDd2lEPTB;MD62NVczQCEQvF2= M4ruUHNCVkeHUh?=
COR-L88 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmzZXRKSzVyPUCuOlQyOTNizszN M2PLOHNCVkeHUh?=
CTV-1 M{Kw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\hfnp1UUN3ME2wMlY1Ozl{IN88US=> MlTXV2FPT0WU
EW-18 NHLXVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjJTWM2OD1yLk[4Olk5KM7:TR?= MmjBV2FPT0WU
HCC1806 NGDWbHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX72[W9FUUN3ME2wMlY6PjZ4IN88US=> MUjTRW5ITVJ?
HuP-T4 NGLBU49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwNkm3OkDPxE1? M321bXNCVkeHUh?=
MDA-MB-361 NUPJN4dwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf0e5BKSzVyPUCuO|I3PjJizszN M{e4d3NCVkeHUh?=
NCI-H1573 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\GUpc{UUN3ME2wMlc{PjNizszN MWnTRW5ITVJ?
KU-19-19 NHPGV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU[1bGJUUUN3ME2wMlc4PDZ2IN88US=> NVfGNnB6W0GQR1XS
COLO-678 MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M16xbWlEPTB;MD64NFg{PCEQvF2= MWjTRW5ITVJ?
C-33-A NFfXd45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwOEGyPVch|ryP M{n5U3NCVkeHUh?=
Calu-3 NWj3WI5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37nbWlEPTB;MD64NVQ{PCEQvF2= NIfNS25USU6JRWK=
AGS MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv1TWM2OD1yLkizOlQ5KM7:TR?= MV3TRW5ITVJ?
SCC-25 NWXsRmlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwOESxO|Eh|ryP MUTTRW5ITVJ?
JVM-2 M1;ye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwOEiyPVkh|ryP NYPFV3JUW0GQR1XS
HCE-T M4WybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;DVlFKSzVyPUCuPFg1OjhizszN NYLGRWxPW0GQR1XS
ES4 MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX75[nR{UUN3ME2wMlk4QDN4IN88US=> MXnTRW5ITVJ?
EKVX NFXrXJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfKOJFKSzVyPUGuNFExPjRizszN NUezUpl4W0GQR1XS
D-542MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jsVWlEPTB;MT6wNVA3PCEQvF2= MkLxV2FPT0WU
SW1116 Mke1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYi2[25CUUN3ME2xMlAyOjh5IN88US=> NFLr[mZUSU6JRWK=
5637 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonJTWM2OD1zLkCxOVEh|ryP NYH2SId2W0GQR1XS
HT-1376 NYm3O3pYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnK[4VKSzVyPUGuNFE2OTNizszN NFHSWFJUSU6JRWK=
NB69 NYOwdo1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1r1d2lEPTB;MT6wNlk1PSEQvF2= MVjTRW5ITVJ?
YKG-1 NVPlZoNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwMEW0NVkh|ryP NVWzd29GW0GQR1XS
EW-3 NGPJOFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwMEe4PFMh|ryP NUL6R4NJW0GQR1XS
GCIY MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G0cWlEPTB;MT6wPFExPCEQvF2= NELac4VUSU6JRWK=
SK-MES-1 MkfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT0XpJsUUN3ME2xMlEyPDh5IN88US=> NXjEbmp3W0GQR1XS
PANC-08-13 M3\sPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjxTWM2OD1zLkG2OFE3KM7:TR?= NGTCOVdUSU6JRWK=
SK-NEP-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PuUWlEPTB;MT6xO|UyOyEQvF2= NGLDTVdUSU6JRWK=
SW954 NF\WN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMkCyNVQh|ryP MlTOV2FPT0WU
NCI-SNU-5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jY[mlEPTB;MT6yN|kh|ryP MmLWV2FPT0WU
SW48 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXaTWM2OD1zLkK1OFMzKM7:TR?= MoPUV2FPT0WU
HT-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e0b2lEPTB;MT6yPFc2OyEQvF2= Ml3hV2FPT0WU
ETK-1 NFr2VYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{mzfGlEPTB;MT6zO|Q2PiEQvF2= M1TsUHNCVkeHUh?=
SCC-15 MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHBTWM2OD1zLkO5OFUyKM7:TR?= Mk\PV2FPT0WU
DU-4475 NEXNT29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHKyS3RKSzVyPUGuOFAyOjFizszN MVXTRW5ITVJ?
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CFPAC-1 M13LU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGm5TnVKSzVyPUGuOFI1QTNizszN M3[ybXNCVkeHUh?=
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NCI-H1993 Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHETWM2OD16LkOzOlMyKM7:TR?= Mo\tV2FPT0WU
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HAL-01 M3HOdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRThwNUG5NUDPxE1? Mn7OV2FPT0WU
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BFTC-909 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHxU3B5UUN3ME25MlA3Pzl7IN88US=> M3\0enNCVkeHUh?=
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BALL-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIraWWdKSzVyPUmuNlE6ODdizszN NWHq[HVLW0GQR1XS
SF539 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XYfWlEPTB;OT6yN|U3OiEQvF2= MVXTRW5ITVJ?
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NCI-H1703 NUSzclFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLMS|c1UUN3ME25MlM1Ozd3IN88US=> M3nifnNCVkeHUh?=
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NCI-H1563 M1jmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPXe5NWUUN3ME25Mlc3ODNzIN88US=> M3\wTHNCVkeHUh?=
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DEL NV;KU5ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPQTWM2OD1zMD6zPVQ3KM7:TR?= NV[5SY5WW0GQR1XS
HuCCT1 M13GWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfufHlzUUN3ME2xNE43ODN|IN88US=> M3X2UnNCVkeHUh?=
OVCAR-4 NF3kfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zObGlEPTB;MUCuPFg{PSEQvF2= NILDU4ZUSU6JRWK=
CAL-72 NH:yfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn5TWM2OD1zMD65N|kyKM7:TR?= NHnsbnpUSU6JRWK=
HCC1954 MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFzLkC3OVQh|ryP Mn3HV2FPT0WU
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SK-MEL-24 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1y2emlEPTB;MUGuNlM3PiEQvF2= MUPTRW5ITVJ?
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NCI-H650 M17iU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3DOIFKSzVyPUGxMlI1OThizszN NWOxcoFoW0GQR1XS
ALL-PO Mn3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\Ob2lEPTB;MUGuNlUyOiEQvF2= NX[5N5NZW0GQR1XS
T84 NH7BNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkS5TWM2OD1zMT6zPVA4KM7:TR?= NGT4[o1USU6JRWK=
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SW626 NHK4NIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LjUWlEPTB;MUGuOVc2PSEQvF2= NWnCNVFsW0GQR1XS
RPMI-2650 MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFzLkW4PFUh|ryP M{\H[nNCVkeHUh?=
MC-IXC NITERm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPzTWM2OD1zMT62O|I5KM7:TR?= NEnVNHNUSU6JRWK=
HOP-62 NUnjdWFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjZWJpKSzVyPUGxMlY4PjRizszN MoftV2FPT0WU
NOS-1 NGXLdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XXZ2lEPTB;MUGuO|ExQSEQvF2= M2[5OXNCVkeHUh?=
SW1573 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jOUmlEPTB;MUGuO|I6PSEQvF2= NH65RYZUSU6JRWK=
WM-115 M2DxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrwfWNIUUN3ME2xNU44PTh6IN88US=> MlLlV2FPT0WU
HuO9 Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXlU3dKSzVyPUGxMlg4PzRizszN Ml2xV2FPT0WU
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MDA-MB-453 M3zLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jr[mlEPTB;MUGuPVUyPSEQvF2= NYfNTXo3W0GQR1XS
NCI-H596 M4HE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[2bmlEPTB;MUKuNFM3QSEQvF2= M2DiXnNCVkeHUh?=
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RS4-11 M{HLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zGV2lEPTB;MUKuNVczPSEQvF2= MWfTRW5ITVJ?
HCC1937 MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTF{Lke1OlQh|ryP NXTRe3RCW0GQR1XS
SW837 M{TrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LDOWlEPTB;MUKuPVAzQCEQvF2= MYXTRW5ITVJ?
NMC-G1 M2jvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHNWmZKSzVyPUGyMlkzOzRizszN NWTiNZFtW0GQR1XS
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DBTRG-05MG NED5TYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGwPYc2UUN3ME2xN{4xPjN{IN88US=> M1f0RXNCVkeHUh?=
SK-UT-1 NX61[IJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPGR5pKSzVyPUGzMlExQDNizszN MVTTRW5ITVJ?
OVCAR-5 Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTId49KSzVyPUGzMlE2QTNizszN NFzIS3BUSU6JRWK=
8505C NX;HO2M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF|LkKwOlch|ryP M1vheXNCVkeHUh?=
SK-MEL-1 NX3aPGJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTK[YM1UUN3ME2xN{44OTN3IN88US=> MXXTRW5ITVJ?
LK-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\CTWM2OD1zMz63OlM6KM7:TR?= NHvGcY5USU6JRWK=
OE33 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF|Lke4OkDPxE1? MoriV2FPT0WU
Ramos-2G6-4C10 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCxTWM2OD1zND6wNlAzKM7:TR?= NETNWGNUSU6JRWK=
EW-13 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL4R453UUN3ME2xOE4xOzV{IN88US=> MnfsV2FPT0WU
NCI-H1793 NV3sbGtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfkepFKSzVyPUG0MlIxQDdizszN NHHtVYpUSU6JRWK=
BHT-101 MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfCTWM2OD1zND6yOFEh|ryP NEK5UJRUSU6JRWK=
RKO MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPGPFVoUUN3ME2xOE42ODd3IN88US=> NVrZcI4xW0GQR1XS
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NCI-H2030 Ml;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTF2Lk[0OFgh|ryP NEHtOHVUSU6JRWK=
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A2058 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF3LkC0NFkh|ryP MUfTRW5ITVJ?
SW1463 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWS3WIJPUUN3ME2xOU4xPDh3IN88US=> M{DDd3NCVkeHUh?=
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CAL-120 NVTnSpA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPzNHF[UUN3ME2xOU4yPDR5IN88US=> MVrTRW5ITVJ?
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NCI-H2405 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF5LkG5O|Qh|ryP NU\VVFhjW0GQR1XS
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RH-18 NIDIbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n3c2lEPTB;MUiuNFA{PSEQvF2= MX7TRW5ITVJ?
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COLO-320-HSR MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofRTWM2OD1zOD63OFYh|ryP NH;sUFVUSU6JRWK=
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NCI-H810 Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTN2LkeyO|gh|ryP NGni[m9USU6JRWK=
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LCLC-103H NHr6[ZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTN4Lke4NFMh|ryP M{DtTXNCVkeHUh?=
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8-MG-BA NWjmVXNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXyelBKSzVyPUO2Mlk1QDNizszN MYnTRW5ITVJ?
MFH-ino MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrnTWM2OD1|Nz6zN|cyKM7:TR?= NWK3VHhVW0GQR1XS
NCI-H23 NHzEXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TGR2lEPTB;M{euOFE6PiEQvF2= MWHTRW5ITVJ?
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KP-N-YN M1nNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTN5Lk[xPVUh|ryP MW\TRW5ITVJ?
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LB831-BLC MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN6Lk[wN|kh|ryP MXPTRW5ITVJ?
HOS M4fvSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKwTWM2OD1|OT62Nlc{KM7:TR?= M2XHN3NCVkeHUh?=
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DMS-79 NGfD[FdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInOPZNKSzVyPUSwMlU5QDlizszN MX;TRW5ITVJ?
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HT Ml;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDPUZpNUUN3ME20NE43PjN7IN88US=> NXrWZodTW0GQR1XS
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HUTU-80 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmO4TWM2OD12MT6wOVY6KM7:TR?= NYnpO2k{W0GQR1XS
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UACC-257 NXvlfpRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTRzLkezOlkh|ryP M2nkV3NCVkeHUh?=
EW-22 M{LJbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\sNocyUUN3ME20NU45Pjl5IN88US=> M4jle3NCVkeHUh?=
NCI-H1755 NWjIZ|Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfjZVN6UUN3ME20NU45PzJ3IN88US=> NHrRO|dUSU6JRWK=
KYSE-150 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTR{LkG3PFIh|ryP MVTTRW5ITVJ?
CGTH-W-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:xTWlEPTB;NEKuOFk2PSEQvF2= M{exbHNCVkeHUh?=
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HCC38 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33QTGlEPTB;NEKuPVYyQCEQvF2= M1q2OnNCVkeHUh?=
BB49-HNC NUO1NGJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPFbnBFUUN3ME20N{4zOzV4IN88US=> NGTyS3dUSU6JRWK=
CAL-62 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnewTWM2OD12Mz60NFI5KM7:TR?= MWrTRW5ITVJ?
NCI-H2029 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmizTWM2OD12Mz61OVgyKM7:TR?= NHnOVZlUSU6JRWK=
M14 NVfnW3pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPPcGtKSzVyPUS0MlE{OzJizszN NH\WXZFUSU6JRWK=
COLO-680N Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTR2LkOzPUDPxE1? NU\MTVZjW0GQR1XS
Hs-578-T M4HUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTR3LkCyPVQh|ryP M1TO[HNCVkeHUh?=
MSTO-211H M4Ozc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUm0O2JTUUN3ME20OU46PDh{IN88US=> NFn2eVhUSU6JRWK=
EW-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjtTWM2OD12NT65Olg6KM7:TR?= MkLDV2FPT0WU
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NCI-H460 NGOzc4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHT5b3lKSzVyPUS2MlUzOyEQvF2= MWfTRW5ITVJ?
CAS-1 M3nZXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL1TJBwUUN3ME20Ok44PzBzIN88US=> M4jZ[nNCVkeHUh?=
TGBC11TKB NHXmeG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR5LkG3O|ch|ryP Mnq3V2FPT0WU
HD-MY-Z NF;G[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHZPJdxUUN3ME20PE44QDZizszN MlvOV2FPT0WU
NCI-H226 MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTR7Lke3PFUh|ryP M1uwU3NCVkeHUh?=
PA-1 NVXKV|d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR7LkizN|Uh|ryP M{\xNHNCVkeHUh?=
LB2518-MEL MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR7Lki3NlMh|ryP M4P3dXNCVkeHUh?=
A101D MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu0SotKSzVyPUS5Mlk1OjVizszN M17ndnNCVkeHUh?=
NCI-H2087 NEfEWoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fIb2lEPTB;NEmuPVY5OiEQvF2= NXOzXXFZW0GQR1XS

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/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。

  • 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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