Afatinib (BIBW2992)

Catalog No.S1011

Afatinib (BIBW2992) Chemical Structure

Molecular Weight(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.

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In DMSO USD 240 In stock
USD 120 In stock
USD 210 In stock
USD 570 In stock

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Cited by 35 Publications

3 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective EGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
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
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v1cGlEPTB;MD6wNFU4OiEQvF2= MmnwV2FPT0WU
KASUMI-1 M3Lv[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;tbW1KSzVyPUCuNFA6OTFizszN NFrOeVNUSU6JRWK=
HCC2218 M3HwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwMEC5PFch|ryP MYHTRW5ITVJ?
KARPAS-45 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMEG2O|Eh|ryP NVnBUmNFW0GQR1XS
HSC-4 MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GwW2lEPTB;MD6wNVc1QCEQvF2= NGjZNllUSU6JRWK=
CHL-1 NHXLWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXZTWM2OD1yLkCxPFM6KM7:TR?= NI\wdFRUSU6JRWK=
KY821 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXMUHFUUUN3ME2wMlAzODZizszN NVn3SXVlW0GQR1XS
NCI-N87 NEHzOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGwNWdKSzVyPUCuNFI4PzNizszN MYnTRW5ITVJ?
DOK NUX5TpNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PPdmlEPTB;MD6wN|E6PCEQvF2= MnzSV2FPT0WU
DSH1 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:yTWM2OD1yLkCzN|E1KM7:TR?= MlXMV2FPT0WU
MDA-MB-175-VII NI[3ZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvSXGJWUUN3ME2wMlA{PDF4IN88US=> M2DLV3NCVkeHUh?=
NCI-H2170 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3ITWM2OD1yLkCzO|I5KM7:TR?= NInwfYxUSU6JRWK=
BT-474 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjVcm5KSzVyPUCuNFQ6QDZizszN NX3Z[I5jW0GQR1XS
EFO-27 M3HtUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWzTWM2OD1yLkC1NVgzKM7:TR?= NX;XNINXW0GQR1XS
NCI-H720 M2rObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMEWzNlUh|ryP M4\qXnNCVkeHUh?=
PC-14 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwMEW2Olgh|ryP MnHIV2FPT0WU
EC-GI-10 MmXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXVTWM2OD1yLkC1PVEzKM7:TR?= NF:5cpFUSU6JRWK=
KYSE-450 M1faOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTGPFNQUUN3ME2wMlA2QTd6IN88US=> NHXEeIhUSU6JRWK=
BPH-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPb4JKSzVyPUCuNFU6QDhizszN MVjTRW5ITVJ?
NCI-H292 NX7WT3dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofqTWM2OD1yLkC2NFkh|ryP NYnrSGxzW0GQR1XS
H9 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHiTVI3UUN3ME2wMlA4OTN{IN88US=> MUHTRW5ITVJ?
NCI-H526 NIfLXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMEe4NlMh|ryP M1uxWHNCVkeHUh?=
NCI-H1623 NFPUeJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe5[FdKSzVyPUCuNFgxOjVizszN M1XlXXNCVkeHUh?=
KYSE-140 M3nQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXmT3VKSzVyPUCuNFg{OyEQvF2= MlLqV2FPT0WU
Ca9-22 MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknwTWM2OD1yLkC4N|U{KM7:TR?= NUn6OIVkW0GQR1XS
AU565 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2raOGlEPTB;MD6wPFUxPCEQvF2= M1XzS3NCVkeHUh?=
ZR-75-30 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXsTWM2OD1yLkC5OVQ2KM7:TR?= MUfTRW5ITVJ?
NCI-H1770 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXYTWM2OD1yLkGwNlgh|ryP NVzkcIV3W0GQR1XS
LB2241-RCC NF:5XI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMUC4PFQh|ryP NYW4bowzW0GQR1XS
CAL-39 M2DYdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHy5dHdKSzVyPUCuNVE4QTJizszN NFvOboxUSU6JRWK=
UACC-893 NY[wTGhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Xvb2lEPTB;MD6xNVg5PSEQvF2= M{ezTHNCVkeHUh?=
LU-65 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\wdZRKSzVyPUCuNVI3OzNizszN NH7YPW9USU6JRWK=
HN M3frZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TYPWlEPTB;MD6xN|A4PyEQvF2= NF7tWI9USU6JRWK=
TI-73 NGXLdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3JcZBTUUN3ME2wMlE1PzF3IN88US=> NVf6UXB3W0GQR1XS
KU812 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMUW0OVYh|ryP MkXsV2FPT0WU
SW13 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETZTYJKSzVyPUCuNVYzOTZizszN MlvLV2FPT0WU
BB30-HNC NXH0WoEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMU[1O|Yh|ryP Mn7qV2FPT0WU
HSC-2 NYPxWlhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjRUJFjUUN3ME2wMlE3QDN5IN88US=> NYe5VXlXW0GQR1XS
BV-173 M{LXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[zb|JKSzVyPUCuNVc2QTZizszN MULTRW5ITVJ?
CAL-27 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zqfmlEPTB;MD6xO|Y{PiEQvF2= M3XSeXNCVkeHUh?=
SBC-1 NUnRUXhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwMUi5OVkh|ryP M{jCOXNCVkeHUh?=
CAL-33 NFfWe|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULPb5RSUUN3ME2wMlIxOTh2IN88US=> NHS0XlBUSU6JRWK=
NCI-H209 M1m3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u3S2lEPTB;MD6yNFQ3KM7:TR?= M4LmS3NCVkeHUh?=
COR-L105 NYjGV4JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwMkGwPFQh|ryP MnXMV2FPT0WU
HSC-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j5OGlEPTB;MD6yNVE6QCEQvF2= M4jwS3NCVkeHUh?=
NCI-H69 M{HzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMkG0OVEh|ryP NYXrRpczW0GQR1XS
MOLT-13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\sOYh5UUN3ME2wMlI{QTd3IN88US=> NFHQTpVUSU6JRWK=
ML-2 MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHDTWM2OD1yLkK0PFAzKM7:TR?= M3rGNXNCVkeHUh?=
IGROV-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMkW5OVIh|ryP Ml36V2FPT0WU
TK10 NECyfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPMUFVKSzVyPUCuNlY4OzhizszN MXjTRW5ITVJ?
EoL-1-cell NXXRfGcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7rTWM2OD1yLkK2PFkzKM7:TR?= NV2wSW43W0GQR1XS
HO-1-N-1 NXTDd|d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITlSHBKSzVyPUCuNlc5PTNizszN MUDTRW5ITVJ?
BHY M37jNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XQZ2lEPTB;MD6yPFY2PSEQvF2= MVnTRW5ITVJ?
LU-139 NWXlPZpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfuT5J7UUN3ME2wMlMxPTFizszN MVXTRW5ITVJ?
23132-87 NUDJb3NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LP[mlEPTB;MD6zNVkzOyEQvF2= MX\TRW5ITVJ?
ACHN M4Xsfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrFZo1KSzVyPUCuN|E6QTRizszN NELM[4hUSU6JRWK=
DoTc2-4510 MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkCyTWM2OD1yLkOyNlE6KM7:TR?= NWHKR3lLW0GQR1XS
BB65-RCC MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV60OoJKUUN3ME2wMlM1PTl|IN88US=> NEPYdYtUSU6JRWK=
HLE NIqwOG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwM{WwOFYh|ryP MWrTRW5ITVJ?
HCC1419 NVLhZ5JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TQNGlEPTB;MD6zOlQxQCEQvF2= MYjTRW5ITVJ?
A388 NXPiPZVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LjSmlEPTB;MD6zOlg2PyEQvF2= NYPnZXdPW0GQR1XS
NUGC-3 M3\EUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3EVFJKSzVyPUCuN|g{PzNizszN MXfTRW5ITVJ?
KYSE-180 M3yzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\ne|BKSzVyPUCuN|kxQDlizszN NX7mUnUxW0GQR1XS
TE-6 NVLYOI0xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm1[lJvUUN3ME2wMlQxOjR4IN88US=> NH[0VJhUSU6JRWK=
A498 MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDQTWM2OD1yLkSwOlc1KM7:TR?= NVzRfJhIW0GQR1XS
NCI-H1648 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rDemlEPTB;MD60OFE5OiEQvF2= MmTOV2FPT0WU
DU-145 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLlRpRKSzVyPUCuOFQ5OzNizszN MXvTRW5ITVJ?
CW-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nuPGlEPTB;MD60OlkyPCEQvF2= MWHTRW5ITVJ?
A431 Mny4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i2OGlEPTB;MD60PFI{OyEQvF2= M1rJRXNCVkeHUh?=
SAS M{L6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HJfGlEPTB;MD60PFM6QCEQvF2= Mnr6V2FPT0WU
NCI-H2126 NFW2e3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwNUG5NlYh|ryP MWfTRW5ITVJ?
NCI-H358 NWLidopFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwNUOyNUDPxE1? M33jT3NCVkeHUh?=
FADU MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXaTWM2OD1yLkW0OFA1KM7:TR?= MVfTRW5ITVJ?
ACN Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7PNJVmUUN3ME2wMlU2ODl2IN88US=> M1zSXHNCVkeHUh?=
HCC70 NFGxTmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HnWWlEPTB;MD61O|Y3OSEQvF2= MXfTRW5ITVJ?
NCI-H1838 MkLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzmTWM2OD1yLk[wNlk6KM7:TR?= NYXy[VlpW0GQR1XS
CAL-54 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjiWpFKSzVyPUCuOlE3OjFizszN NUjIXWtZW0GQR1XS
NCI-H1975 MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwNkG3Nlgh|ryP NYi1PIY1W0GQR1XS
COR-L88 Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G1d2lEPTB;MD62OFEyOyEQvF2= NVzaeJpzW0GQR1XS
CTV-1 NVrVTlRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDuOpNPUUN3ME2wMlY1Ozl{IN88US=> M2nmZ3NCVkeHUh?=
EW-18 MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXPZoVKSzVyPUCuOlg3QThizszN M4rPSHNCVkeHUh?=
HCC1806 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jPeWlEPTB;MD62PVY3PiEQvF2= MVrTRW5ITVJ?
HuP-T4 M1TiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX4TZlKSzVyPUCuOlk4PiEQvF2= MkHBV2FPT0WU
MDA-MB-361 Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nwVWlEPTB;MD63NlY3OiEQvF2= NYfvW4ZIW0GQR1XS
NCI-H1573 NVL5WYFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXYfGZKSzVyPUCuO|M3OyEQvF2= NFHwT5ZUSU6JRWK=
KU-19-19 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rndWlEPTB;MD63O|Q3PCEQvF2= NVnZfZh1W0GQR1XS
COLO-678 NHPqbJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwOEC4N|Qh|ryP MV;TRW5ITVJ?
C-33-A NICwN2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jxemlEPTB;MD64NVI6PyEQvF2= M{S0WHNCVkeHUh?=
Calu-3 M2jXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwOEG0N|Qh|ryP Mn;GV2FPT0WU
AGS NF3PVXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrNUJVKSzVyPUCuPFM3PDhizszN MUnTRW5ITVJ?
SCC-25 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXzTXlbUUN3ME2wMlg1OTdzIN88US=> MlnnV2FPT0WU
JVM-2 NXzXeo4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwOEiyPVkh|ryP NGnPXXFUSU6JRWK=
HCE-T MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HNdGlEPTB;MD64PFQzQCEQvF2= NHu3cXJUSU6JRWK=
ES4 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYn6bWRkUUN3ME2wMlk4QDN4IN88US=> MlzQV2FPT0WU
EKVX NFryTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTFwMEGwOlQh|ryP Mn7UV2FPT0WU
D-542MG NGD2T5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHi4cnJKSzVyPUGuNFExPjRizszN Ml7JV2FPT0WU
SW1116 NHzoWG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjOV4Q5UUN3ME2xMlAyOjh5IN88US=> NHf6XZNUSU6JRWK=
5637 NF2w[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j5UGlEPTB;MT6wNVUyKM7:TR?= NFLCXWpUSU6JRWK=
HT-1376 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDIOXhQUUN3ME2xMlAyPTF|IN88US=> NWOxPI9DW0GQR1XS
NB69 MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHlTWM2OD1zLkCyPVQ2KM7:TR?= MnLnV2FPT0WU
YKG-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD5TWM2OD1zLkC1OFE6KM7:TR?= MkjwV2FPT0WU
EW-3 NVP3[4d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;tTWM2OD1zLkC3PFg{KM7:TR?= MVnTRW5ITVJ?
GCIY NWnDOox3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13pVGlEPTB;MT6wPFExPCEQvF2= MXHTRW5ITVJ?
SK-MES-1 MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPXcotXUUN3ME2xMlEyPDh5IN88US=> Mk\4V2FPT0WU
PANC-08-13 NX21fXNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTaTWM2OD1zLkG2OFE3KM7:TR?= NW\t[Y1oW0GQR1XS
SK-NEP-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nBVGlEPTB;MT6xO|UyOyEQvF2= MlfzV2FPT0WU
SW954 NEG2do1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK2SotyUUN3ME2xMlIxOjF2IN88US=> MonhV2FPT0WU
NCI-SNU-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HDZWlEPTB;MT6yN|kh|ryP NEHmZ|ZUSU6JRWK=
SW48 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXLfpNKSzVyPUGuNlU1OzJizszN MlPjV2FPT0WU
HT-3 NFjEeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTXcnNKSzVyPUGuNlg4PTNizszN M4jWV3NCVkeHUh?=
ETK-1 NGPBTYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrhNWRuUUN3ME2xMlM4PDV4IN88US=> MVLTRW5ITVJ?
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OE33 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF|Lke4OkDPxE1? MnXHV2FPT0WU
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SK-HEP-1 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LuN2lEPTB;M{CuOlMzPiEQvF2= M3XKSHNCVkeHUh?=
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KM-H2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN2LkG3O|kh|ryP MVLTRW5ITVJ?
NCI-H2122 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\5cpJKSzVyPUO0MlM1PzFizszN MnTHV2FPT0WU
ABC-1 M3S3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m3fWlEPTB;M{SuN|Y6OyEQvF2= MX\TRW5ITVJ?
NCI-H1355 Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTN2LkO4PFkh|ryP MYLTRW5ITVJ?
NOMO-1 Ml7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTN2LkW3NFMh|ryP MmTjV2FPT0WU
MZ7-mel MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInKdplKSzVyPUO0MlY1QDdizszN MmfIV2FPT0WU
NCI-H810 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TQTWlEPTB;M{SuO|I4QCEQvF2= MV3TRW5ITVJ?
D-392MG NGq3T4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PhdmlEPTB;M{WuNFU3PSEQvF2= MkCyV2FPT0WU
LB771-HNC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTmZnd6UUN3ME2zOU4yPjV6IN88US=> NGnQR5hUSU6JRWK=
COLO-679 NI\JTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWySZhKSzVyPUO1MlM5QCEQvF2= MnnPV2FPT0WU
SK-PN-DW M2G5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPESnhKSzVyPUO1MlQ{PjlizszN NYC3R5dSW0GQR1XS
VA-ES-BJ MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XndGlEPTB;M{WuOFY1QSEQvF2= M{nNS3NCVkeHUh?=
KNS-42 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7QTWM2OD1|NT61PFI3KM7:TR?= MW\TRW5ITVJ?
RVH-421 NHjRbZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTN3Lke2OFUh|ryP Mk[4V2FPT0WU
P30-OHK NX75bo96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPqTWM2OD1|NT64O|UzKM7:TR?= MYHTRW5ITVJ?
G-402 NEHo[mdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHZNlk5UUN3ME2zOU46QDZ5IN88US=> MUfTRW5ITVJ?
S-117 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN4LkOwNFgh|ryP NVzieYkxW0GQR1XS
RXF393 NX7a[4R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTN4LkO3PFUh|ryP MYPTRW5ITVJ?
LCLC-103H NXH0OphUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P3SmlEPTB;M{[uO|gxOyEQvF2= NW\UOFlmW0GQR1XS
U-118-MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7McoJKSzVyPUO2Mlg5PDdizszN M3nzUnNCVkeHUh?=
8-MG-BA MnTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fzd2lEPTB;M{[uPVQ5OyEQvF2= NWWz[ZB3W0GQR1XS
MFH-ino MmXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfBXZd[UUN3ME2zO{4{OzdzIN88US=> MVvTRW5ITVJ?
NCI-H23 NIfyW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXX[YlQUUN3ME2zO{41OTl4IN88US=> Moi4V2FPT0WU
NCI-H446 Mle0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjFTWM2OD1|Nz60PFYzKM7:TR?= NV3tO5Q5W0GQR1XS
LU-99A NUXQZ3JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXsTWM2OD1|Nz61O|MyKM7:TR?= NWLXPYl{W0GQR1XS
KP-N-YN NHrk[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnoRWluUUN3ME2zO{43OTl3IN88US=> NXvvVFlGW0GQR1XS
SCC-9 MmXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHxTWM2OD1|Nz63PFM5KM7:TR?= M{fYV3NCVkeHUh?=
EFM-19 M37XcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK5PGFKSzVyPUO3Mlc6PjdizszN NUn6Z2l4W0GQR1XS
A427 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTN5LkmxNFch|ryP NYTKZo5bW0GQR1XS
LB831-BLC NVXVe3FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPNTWM2OD1|OD62NFM6KM7:TR?= M4q4VnNCVkeHUh?=
HOS MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjINGZnUUN3ME2zPU43Ojd|IN88US=> MlfVV2FPT0WU
LAN-6 M3LwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLmTWM2OD12MD6wNVEzKM7:TR?= NFTFOoNUSU6JRWK=
U251 NWDsV3ZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33NbmlEPTB;NECuOFA2PCEQvF2= M{mw[HNCVkeHUh?=
SNU-387 NXH4dXhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XQcWlEPTB;NECuOFU2OyEQvF2= MnXMV2FPT0WU
DMS-79 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjIPFBKSzVyPUSwMlU5QDlizszN MlXtV2FPT0WU
SK-LU-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PXNWlEPTB;NECuOlU3QCEQvF2= MV7TRW5ITVJ?
HT MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRyLk[2N|kh|ryP NHXn[pZUSU6JRWK=
KP-N-YS NWfU[2lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTRyLk[3Olgh|ryP Ml;RV2FPT0WU
DMS-114 NGrLUIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTRyLkizO|Qh|ryP NX;SWZJNW0GQR1XS
HUTU-80 NWfIbm5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vJW2lEPTB;NEGuNFU3QSEQvF2= NFL4SlhUSU6JRWK=
ONS-76 NIe3c2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPrUllKSzVyPUSxMlQ4ODlizszN MleyV2FPT0WU
A673 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rLRWlEPTB;NEGuOVE2PyEQvF2= NUPTTJZqW0GQR1XS
HPAF-II M1W0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jlOWlEPTB;NEGuOlcxQSEQvF2= M{TlUHNCVkeHUh?=
UACC-257 MlLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknHTWM2OD12MT63N|Y6KM7:TR?= M{\hdHNCVkeHUh?=
EW-22 M{fZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3IfpJKSzVyPUSxMlg3QTdizszN NYPRNFh3W0GQR1XS
NCI-H1755 NVvHflZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTke|NGUUN3ME20NU45PzJ3IN88US=> M2\HVXNCVkeHUh?=
KYSE-150 NIPH[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i2cWlEPTB;NEKuNVc5OiEQvF2= NFjVfmVUSU6JRWK=
CGTH-W-1 NEP5W|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnyRpk5UUN3ME20Nk41QTV3IN88US=> NWT4SHdYW0GQR1XS
NB13 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fKZWlEPTB;NEKuOlIyPyEQvF2= M2PYdnNCVkeHUh?=
SW872 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;HNHdKSzVyPUSyMlY{OzFizszN NF\tbm1USU6JRWK=
KP-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3LTWM2OD12Mj64PFMzKM7:TR?= MlP1V2FPT0WU
HCC38 NF7BdndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TRW2lEPTB;NEKuPVYyQCEQvF2= M2nmc3NCVkeHUh?=
BB49-HNC M{PnUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1y1U2lEPTB;NEOuNlM2PiEQvF2= MoLCV2FPT0WU
CAL-62 NWG5TnV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTR|LkSwNlgh|ryP NI\rVJFUSU6JRWK=
NCI-H2029 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nCZWlEPTB;NEOuOVU5OSEQvF2= M1XPfnNCVkeHUh?=
M14 M2fQRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPWSnpKSzVyPUS0MlE{OzJizszN M2HRc3NCVkeHUh?=
COLO-680N NULXc4pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq4S5lDUUN3ME20OE4{OzlizszN MYfTRW5ITVJ?
Hs-578-T NXTjNXc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfvTWM2OD12NT6wNlk1KM7:TR?= M175OHNCVkeHUh?=
MSTO-211H NG\heZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\QN4FKSzVyPUS1Mlk1QDJizszN M13Bb3NCVkeHUh?=
EW-1 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTR3Lkm2PFkh|ryP MWTTRW5ITVJ?
SW948 M3fl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnpNVdGUUN3ME20Ok41PDZ{IN88US=> M{TFd3NCVkeHUh?=
NCI-H460 NXzvPFJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYThNYt3UUN3ME20Ok42OjNizszN NEK2PFZUSU6JRWK=
CAS-1 NFfoWXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrQS2pKSzVyPUS2Mlc4ODFizszN MWjTRW5ITVJ?
TGBC11TKB M2DIcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2SxXmlEPTB;NEeuNVc4PyEQvF2= NHjz[WxUSU6JRWK=
HD-MY-Z NYrwc|lwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f4bmlEPTB;NEiuO|g3KM7:TR?= M3rKPXNCVkeHUh?=
NCI-H226 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17zO2lEPTB;NEmuO|c5PSEQvF2= M{X6VXNCVkeHUh?=
PA-1 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR7LkizN|Uh|ryP MnyyV2FPT0WU
LB2518-MEL M1HGRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjiTXJwUUN3ME20PU45PzJ|IN88US=> NHS3fYdUSU6JRWK=
A101D M4myfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTR7Lkm0NlUh|ryP NF60d3lUSU6JRWK=
NCI-H2087 MlXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfXZ2xHUUN3ME20PU46Pjh{IN88US=> NVLieWpXW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay
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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.
Cell Research
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  • Cell lines: NSCLC cells
  • Concentrations: 0-10 μM
  • Incubation Time: 1 hour
  • Method:

    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.


    (Only for Reference)
Animal Research
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  • Animal Models: Athymic NMRI-nu/nu female mice
  • Formulation: In 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
  • Dosages: 20 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (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.

Chemical Information

Molecular Weight 485.94
Formula

C24H25ClFN5O3

CAS No. 439081-18-2
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02501603 Recruiting Gastric Cancer|Gastroesophageal Junction Cancer Yonsei University July 2016 Phase 2
NCT02795156 Not yet 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 July 2016 Phase 2
NCT02780687 Recruiting Urologic Neoplasms Boehringer Ingelheim June 2016 Phase 2
NCT02183883 Not yet recruiting Non-small Cell Lung Cancer University College, London|Boehringer Ingelheim May 2016 Phase 2
NCT02716311 Not yet recruiting Non Small Cell Lung Cancer Intergroupe Francophone de Cancerologie Thoracique April 2016 Phase 2
NCT02629523 Not yet recruiting Lung Neoplasms|EGFR Gene Mutation Chonnam National University Hospital March 2016 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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.

EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID