Afatinib (BIBW2992)

Catalog No.S1011

Afatinib (BIBW2992) Chemical Structure

Molecular Weight(MW): 485.94

Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively.

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In DMSO USD 240 In stock
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USD 210 In stock
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Cited by 38 Publications

4 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively.
Targets
EGFR (L858R) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
ErbB4 [2]
(Cell-free assay)
EGFR (L858R/T790M) [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
0.4 nM 0.5 nM 1 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 Mn3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\UTWM2OD1yLkCwOVczKM7:TR?= MorxV2FPT0WU
KASUMI-1 NWr5VFg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwMEC5NVEh|ryP NH\obFVUSU6JRWK=
HCC2218 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzSW3NKSzVyPUCuNFA6QDdizszN NHHMV|NUSU6JRWK=
KARPAS-45 NFLKfnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjLTWM2OD1yLkCxOlcyKM7:TR?= NF:xZm9USU6JRWK=
HSC-4 NYf1OHJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrFTWM2OD1yLkCxO|Q5KM7:TR?= NF[zPXZUSU6JRWK=
CHL-1 NEi0R4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TyfGlEPTB;MD6wNVg{QSEQvF2= NWD6VW54W0GQR1XS
KY821 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXneppJUUN3ME2wMlAzODZizszN NXTxOWxrW0GQR1XS
NCI-N87 NUjqNoNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTBwMEK3O|Mh|ryP MXPTRW5ITVJ?
DOK NF3he2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMEOxPVQh|ryP M{LSUnNCVkeHUh?=
DSH1 Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLYXIhoUUN3ME2wMlA{OzF2IN88US=> M2fwXXNCVkeHUh?=
MDA-MB-175-VII MlHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7rWIc3UUN3ME2wMlA{PDF4IN88US=> NUTwNlFCW0GQR1XS
NCI-H2170 M{D6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TmcWlEPTB;MD6wN|czQCEQvF2= Mmq0V2FPT0WU
BT-474 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwMES5PFYh|ryP NF3i[plUSU6JRWK=
EFO-27 MnXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMEWxPFIh|ryP M2K1RnNCVkeHUh?=
NCI-H720 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwMEWzNlUh|ryP NYTGXVdiW0GQR1XS
PC-14 MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPhRY0yUUN3ME2wMlA2PjZ6IN88US=> NHKwcolUSU6JRWK=
EC-GI-10 M{nmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXwVXByUUN3ME2wMlA2QTF{IN88US=> MmnJV2FPT0WU
KYSE-450 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\4TWM2OD1yLkC1PVc5KM7:TR?= MYDTRW5ITVJ?
BPH-1 MlG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG0SWpKSzVyPUCuNFU6QDhizszN MmDkV2FPT0WU
NCI-H292 MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkX1TWM2OD1yLkC2NFkh|ryP NITBeWxUSU6JRWK=
H9 NHjvV|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrwTWM2OD1yLkC3NVMzKM7:TR?= MXXTRW5ITVJ?
NCI-H526 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TwcmlEPTB;MD6wO|gzOyEQvF2= M2nnTXNCVkeHUh?=
NCI-H1623 M13Qbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLnTWM2OD1yLkC4NFI2KM7:TR?= M{jmbnNCVkeHUh?=
KYSE-140 NUf4W2k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3zOmh4UUN3ME2wMlA5OzNizszN NYPkRm1UW0GQR1XS
Ca9-22 M2nrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwMEizOVMh|ryP M33TenNCVkeHUh?=
AU565 NGLVcZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwMEi1NFQh|ryP M1\wXXNCVkeHUh?=
ZR-75-30 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\2cXNHUUN3ME2wMlA6PTR3IN88US=> MXPTRW5ITVJ?
NCI-H1770 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzpTWM2OD1yLkGwNlgh|ryP M3XtdHNCVkeHUh?=
LB2241-RCC M{LP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMUC4PFQh|ryP M4\0cXNCVkeHUh?=
CAL-39 NYL4U|U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjITWM2OD1yLkGxO|kzKM7:TR?= M4DJc3NCVkeHUh?=
UACC-893 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXToTGY6UUN3ME2wMlEyQDh3IN88US=> Mk\aV2FPT0WU
LU-65 NV7v[VdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH3TWM2OD1yLkGyOlM{KM7:TR?= MmnQV2FPT0WU
HN MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HtZWlEPTB;MD6xN|A4PyEQvF2= MkjEV2FPT0WU
TI-73 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3kV5dKSzVyPUCuNVQ4OTVizszN M2XCPXNCVkeHUh?=
KU812 NIH4WVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rlW2lEPTB;MD6xOVQ2PiEQvF2= M1\rW3NCVkeHUh?=
SW13 NVvJ[W9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1WwZ2lEPTB;MD6xOlIyPiEQvF2= M1ziUXNCVkeHUh?=
BB30-HNC Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnobWN2UUN3ME2wMlE3PTd4IN88US=> M3jNO3NCVkeHUh?=
HSC-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMU[4N|ch|ryP NETUPY5USU6JRWK=
BV-173 NUGzPHhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwMUe1PVYh|ryP MkXrV2FPT0WU
CAL-27 M2\rZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17ue2lEPTB;MD6xO|Y{PiEQvF2= NIWzemdUSU6JRWK=
SBC-1 NFv2VmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;FTWM2OD1yLkG4PVU6KM7:TR?= MXvTRW5ITVJ?
CAL-33 Ml;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMkCxPFQh|ryP NHLIemFUSU6JRWK=
NCI-H209 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{noO2lEPTB;MD6yNFQ3KM7:TR?= NWXNNJJiW0GQR1XS
COR-L105 NW\GeW5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMkGwPFQh|ryP M3rNdHNCVkeHUh?=
HSC-3 NXzyVmh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fifWlEPTB;MD6yNVE6QCEQvF2= M3PtTHNCVkeHUh?=
NCI-H69 M{HlTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17IT2lEPTB;MD6yNVQ2OSEQvF2= MkC2V2FPT0WU
MOLT-13 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMkO5O|Uh|ryP Ml\NV2FPT0WU
ML-2 NYjW[3JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrhRohvUUN3ME2wMlI1QDB{IN88US=> MULTRW5ITVJ?
IGROV-1 MkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXscpdjUUN3ME2wMlI2QTV{IN88US=> NXL5XYVSW0GQR1XS
TK10 M1PrRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K3c2lEPTB;MD6yOlc{QCEQvF2= MnjsV2FPT0WU
EoL-1-cell MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfmTWM2OD1yLkK2PFkzKM7:TR?= MmXNV2FPT0WU
HO-1-N-1 NHTZUYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrTTWM2OD1yLkK3PFU{KM7:TR?= M2XSfHNCVkeHUh?=
BHY NWPpNmg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXDNFRsUUN3ME2wMlI5PjV3IN88US=> NVnPZXNmW0GQR1XS
LU-139 Mni4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwM{C1NUDPxE1? MWjTRW5ITVJ?
23132-87 NIP4OVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHpdphxUUN3ME2wMlMyQTJ|IN88US=> M2fwWnNCVkeHUh?=
ACHN M3\qfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTaemNKSzVyPUCuN|E6QTRizszN NXzCfW5IW0GQR1XS
DoTc2-4510 NGnxOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnEXmIxUUN3ME2wMlMzOjF7IN88US=> Mnq3V2FPT0WU
BB65-RCC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjaclhKSzVyPUCuN|Q2QTNizszN NIDiWIRUSU6JRWK=
HLE NEXxcotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L2bmlEPTB;MD6zOVA1PiEQvF2= NVvHeVlrW0GQR1XS
HCC1419 M3zLcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDZfGp5UUN3ME2wMlM3PDB6IN88US=> MXjTRW5ITVJ?
A388 NF;VToFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnPboduUUN3ME2wMlM3QDV5IN88US=> MWrTRW5ITVJ?
NUGC-3 NG\JWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwM{izO|Mh|ryP M321e3NCVkeHUh?=
KYSE-180 NUO5Spc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrpZ|VJUUN3ME2wMlM6ODh7IN88US=> M3jh[XNCVkeHUh?=
TE-6 NH\Oe2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXVUphKSzVyPUCuOFAzPDZizszN M{HaUXNCVkeHUh?=
A498 NVHLfZFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwNEC2O|Qh|ryP NIDjTXRUSU6JRWK=
NCI-H1648 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvsTWM2OD1yLkS0NVgzKM7:TR?= NXnlbGtDW0GQR1XS
DU-145 M3zxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHK5Z2NKSzVyPUCuOFQ5OzNizszN MmrBV2FPT0WU
CW-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWwTWM2OD1yLkS2PVE1KM7:TR?= NXvJeYtZW0GQR1XS
A431 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjMXodKSzVyPUCuOFgzOzNizszN MX3TRW5ITVJ?
SAS MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH4SFZKSzVyPUCuOFg{QThizszN MX;TRW5ITVJ?
NCI-H2126 NFj5ZpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPtN3lqUUN3ME2wMlUyQTJ4IN88US=> MX;TRW5ITVJ?
NCI-H358 MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwNUOyNUDPxE1? MorPV2FPT0WU
FADU NHXDOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHxe2lKSzVyPUCuOVQ1ODRizszN MmmwV2FPT0WU
ACN NXzYTFI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIC1T4xKSzVyPUCuOVUxQTRizszN MUjTRW5ITVJ?
HCC70 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorYTWM2OD1yLkW3OlYyKM7:TR?= M4rESXNCVkeHUh?=
NCI-H1838 NXrl[GI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXreG5KSzVyPUCuOlAzQTlizszN NWnEWG91W0GQR1XS
CAL-54 M4nzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLHb|l5UUN3ME2wMlYyPjJzIN88US=> MWHTRW5ITVJ?
NCI-H1975 M4fOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwNkG3Nlgh|ryP NXfkdld3W0GQR1XS
COR-L88 NX\JW2pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:5OGlEPTB;MD62OFEyOyEQvF2= MWTTRW5ITVJ?
CTV-1 NIK5U4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrTTWM2OD1yLk[0N|kzKM7:TR?= Mn7RV2FPT0WU
EW-18 NYrIfmdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwNki2PVgh|ryP NWewU2ZWW0GQR1XS
HCC1806 NFXp[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS5U5VKSzVyPUCuOlk3PjZizszN NIHGWlNUSU6JRWK=
HuP-T4 NUniUpBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwNkm3OkDPxE1? MnvGV2FPT0WU
MDA-MB-361 NYPhUlhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYmwfVEzUUN3ME2wMlczPjZ{IN88US=> NEDTWYlUSU6JRWK=
NCI-H1573 NHfJd|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHVTWM2OD1yLkezOlMh|ryP NYnnWWpkW0GQR1XS
KU-19-19 M4ToXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7a[WNiUUN3ME2wMlc4PDZ2IN88US=> NWHYbZY1W0GQR1XS
COLO-678 M3fhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjpSpZKSzVyPUCuPFA5OzRizszN NV[3WGRIW0GQR1XS
C-33-A M13NeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwOEGyPVch|ryP Ml3OV2FPT0WU
Calu-3 NEjFXnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\xOGlKSzVyPUCuPFE1OzRizszN MYHTRW5ITVJ?
AGS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fxRmlEPTB;MD64N|Y1QCEQvF2= NIflXFNUSU6JRWK=
SCC-25 M1fubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rIVWlEPTB;MD64OFE4OSEQvF2= NVj0[YRxW0GQR1XS
JVM-2 NVHsW3BDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[0O2VKSzVyPUCuPFgzQTlizszN NVjZdG1YW0GQR1XS
HCE-T Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm1bY1KSzVyPUCuPFg1OjhizszN MXjTRW5ITVJ?
ES4 NUTpT5FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HtNGlEPTB;MD65O|g{PiEQvF2= MV7TRW5ITVJ?
EKVX NVjw[nR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jv[2lEPTB;MT6wNVA3PCEQvF2= NYC3OWtYW0GQR1XS
D-542MG NYDMdVRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDITWM2OD1zLkCxNFY1KM7:TR?= MXfTRW5ITVJ?
SW1116 MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPVXHZRUUN3ME2xMlAyOjh5IN88US=> NUnuU5h{W0GQR1XS
5637 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFwMEG1NUDPxE1? NVj4blVuW0GQR1XS
HT-1376 NV31b4dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K0NGlEPTB;MT6wNVUyOyEQvF2= NWHLNWdXW0GQR1XS
NB69 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4foOWlEPTB;MT6wNlk1PSEQvF2= MoCxV2FPT0WU
YKG-1 M{nsW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDzWnFKSzVyPUGuNFU1OTlizszN NVq1TZhUW0GQR1XS
EW-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwMEe4PFMh|ryP MUDTRW5ITVJ?
GCIY NUDBXFhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r1bGlEPTB;MT6wPFExPCEQvF2= MlTFV2FPT0WU
SK-MES-1 M13sZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjJTWM2OD1zLkGxOFg4KM7:TR?= M{PtcHNCVkeHUh?=
PANC-08-13 M2[wdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnuOZRKSzVyPUGuNVY1OTZizszN MUnTRW5ITVJ?
SK-NEP-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTFwMUe1NVMh|ryP Mn\BV2FPT0WU
SW954 M2e5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXITWM2OD1zLkKwNlE1KM7:TR?= MXLTRW5ITVJ?
NCI-SNU-5 NY\UfY1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTFwMkO5JO69VQ>? MoDhV2FPT0WU
SW48 M3;LWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwMkW0N|Ih|ryP M1\BeXNCVkeHUh?=
HT-3 MkD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrDTWM2OD1zLkK4O|U{KM7:TR?= NXzIeXdpW0GQR1XS
ETK-1 MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjncWZ{UUN3ME2xMlM4PDV4IN88US=> NEDTT2hUSU6JRWK=
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KM-H2 MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTN2LkG3O|kh|ryP MUfTRW5ITVJ?
NCI-H2122 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCTWM2OD1|ND6zOFcyKM7:TR?= NXvRdmJUW0GQR1XS
ABC-1 M3P5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDtfIlUUUN3ME2zOE4{Pjl|IN88US=> MW\TRW5ITVJ?
NCI-H1355 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\EZWlEPTB;M{SuN|g5QSEQvF2= NWT6c2Q1W0GQR1XS
NOMO-1 M{e5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D5ZmlEPTB;M{SuOVcxOyEQvF2= MWnTRW5ITVJ?
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NCI-H810 NFGwU5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLRTWM2OD1|ND63Nlc5KM7:TR?= NGPTVVZUSU6JRWK=
D-392MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfwXpRZUUN3ME2zOU4xPTZ3IN88US=> NIHxUYNUSU6JRWK=
LB771-HNC NXi4WWJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTN3LkG2OVgh|ryP NV;pV5hiW0GQR1XS
COLO-679 MoXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nsNmlEPTB;M{WuN|g5KM7:TR?= NIPWfoVUSU6JRWK=
SK-PN-DW M2S4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm2V|BEUUN3ME2zOU41OzZ7IN88US=> M{P0T3NCVkeHUh?=
VA-ES-BJ MnrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTN3LkS2OFkh|ryP NGTucotUSU6JRWK=
KNS-42 M1W4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnHVpJOUUN3ME2zOU42QDJ4IN88US=> NGO2bXJUSU6JRWK=
RVH-421 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTmN5kyUUN3ME2zOU44PjR3IN88US=> NEK0R5JUSU6JRWK=
P30-OHK M4rpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvCS|hJUUN3ME2zOU45PzV{IN88US=> M2Huc3NCVkeHUh?=
G-402 NVXPe3lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXoWWJ5UUN3ME2zOU46QDZ5IN88US=> M{XIbXNCVkeHUh?=
S-117 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTN4LkOwNFgh|ryP NF;tbVFUSU6JRWK=
RXF393 M2HqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELRfIdKSzVyPUO2MlM4QDVizszN NH;IZYdUSU6JRWK=
LCLC-103H NYPZZ3E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[3TWM2OD1|Nj63PFA{KM7:TR?= M4LYO3NCVkeHUh?=
U-118-MG M4K1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHQSYtKSzVyPUO2Mlg5PDdizszN NYDkVpFYW0GQR1XS
8-MG-BA MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHJW5U1UUN3ME2zOk46PDh|IN88US=> MWrTRW5ITVJ?
MFH-ino MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[3OZJrUUN3ME2zO{4{OzdzIN88US=> NHvibJVUSU6JRWK=
NCI-H23 NEHtOmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGxO5lKSzVyPUO3MlQyQTZizszN NHq4ZnpUSU6JRWK=
NCI-H446 M2f6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTN5LkS4OlIh|ryP M2XOTXNCVkeHUh?=
LU-99A NXfPclZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H3XGlEPTB;M{euOVc{OSEQvF2= NUT4XlM6W0GQR1XS
KP-N-YN M4XpZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XBT2lEPTB;M{euOlE6PSEQvF2= M37hN3NCVkeHUh?=
SCC-9 NHvxXZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPUT49KSzVyPUO3Mlc5OzhizszN MWfTRW5ITVJ?
EFM-19 MlXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTqTWM2OD1|Nz63PVY4KM7:TR?= NIPu[45USU6JRWK=
A427 NFTu[|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37LVmlEPTB;M{euPVExPyEQvF2= Ml;zV2FPT0WU
LB831-BLC NIftOY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnniTWM2OD1|OD62NFM6KM7:TR?= MXzTRW5ITVJ?
HOS NWewRWt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTN7Lk[yO|Mh|ryP NVrwOXIzW0GQR1XS
LAN-6 M1uySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrmRnEzUUN3ME20NE4xOTF{IN88US=> M1LkT3NCVkeHUh?=
U251 NWHGfZFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXPeYJKSzVyPUSwMlQxPTRizszN M1rEV3NCVkeHUh?=
SNU-387 NI\XN4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37FV2lEPTB;NECuOFU2OyEQvF2= MX3TRW5ITVJ?
DMS-79 M164[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX1cm1KSzVyPUSwMlU5QDlizszN MXTTRW5ITVJ?
SK-LU-1 M1zYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTRyLk[1Olgh|ryP MWPTRW5ITVJ?
HT NVjzWIR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTkXmNyUUN3ME20NE43PjN7IN88US=> NUf4R|RrW0GQR1XS
KP-N-YS MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPSdmN6UUN3ME20NE43PzZ6IN88US=> NUHNe41EW0GQR1XS
DMS-114 NXXoS|d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTRyLkizO|Qh|ryP NVPpdFdlW0GQR1XS
HUTU-80 NF;jPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXDTWM2OD12MT6wOVY6KM7:TR?= MVHTRW5ITVJ?
ONS-76 NEPiSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X2WmlEPTB;NEGuOFcxQSEQvF2= NGTJe4xUSU6JRWK=
A673 M4LZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnW3TWM2OD12MT61NVU4KM7:TR?= MWDTRW5ITVJ?
HPAF-II M{fHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTRzLk[3NFkh|ryP NGWzc4NUSU6JRWK=
UACC-257 Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqwTWM2OD12MT63N|Y6KM7:TR?= MV;TRW5ITVJ?
EW-22 M1jifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjoVXlKSzVyPUSxMlg3QTdizszN MVHTRW5ITVJ?
NCI-H1755 NIru[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTRzLki3NlUh|ryP M1:wPXNCVkeHUh?=
KYSE-150 NWjwWmdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn3TWM2OD12Mj6xO|gzKM7:TR?= Mn[xV2FPT0WU
CGTH-W-1 NYjpbHBKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR{LkS5OVUh|ryP MVLTRW5ITVJ?
NB13 M{XoU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrPT5pKSzVyPUSyMlYzOTdizszN NELURnBUSU6JRWK=
SW872 MonqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTR{Lk[zN|Eh|ryP MU\TRW5ITVJ?
KP-4 NIOz[nJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zDR2lEPTB;NEKuPFg{OiEQvF2= M{fBTHNCVkeHUh?=
HCC38 Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTYc41YUUN3ME20Nk46PjF6IN88US=> NW\pVHdvW0GQR1XS
BB49-HNC NXfMUGpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7ZXnpKSzVyPUSzMlI{PTZizszN NY\3cYlnW0GQR1XS
CAL-62 NEP4bVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvi[nJ{UUN3ME20N{41ODJ6IN88US=> MmPrV2FPT0WU
NCI-H2029 NYXYWmhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrKNlBwUUN3ME20N{42PThzIN88US=> NGLzNpNUSU6JRWK=
M14 NXS4Tnp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrFTWM2OD12ND6xN|MzKM7:TR?= NGjNWZpUSU6JRWK=
COLO-680N NH\zfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[wTWM2OD12ND6zN|kh|ryP MVTTRW5ITVJ?
Hs-578-T NXPoPXdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLQfJJsUUN3ME20OU4xOjl2IN88US=> M{OybnNCVkeHUh?=
MSTO-211H MkjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\YTWM2OD12NT65OFgzKM7:TR?= MlnEV2FPT0WU
EW-1 M335c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C3W2lEPTB;NEWuPVY5QSEQvF2= MnXwV2FPT0WU
SW948 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2iwcGlEPTB;NE[uOFQ3OiEQvF2= NWXjUJJMW0GQR1XS
NCI-H460 NUDofpNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTR4LkWyN{DPxE1? NYTqc3U6W0GQR1XS
CAS-1 M4CzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvCTWM2OD12Nj63O|AyKM7:TR?= MknqV2FPT0WU
TGBC11TKB NHzTeZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR5LkG3O|ch|ryP M1viU3NCVkeHUh?=
HD-MY-Z NVfyTWVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle3TWM2OD12OD63PFYh|ryP M1jpXnNCVkeHUh?=
NCI-H226 M2D1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjxSIJKSzVyPUS5Mlc4QDVizszN M{Pj[nNCVkeHUh?=
PA-1 NUOzempMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vpdWlEPTB;NEmuPFM{PSEQvF2= NVfKXmZkW0GQR1XS
LB2518-MEL M3u2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[5XYlKSzVyPUS5Mlg4OjNizszN NUDZ[mxIW0GQR1XS
A101D NV3lOZJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jFWmlEPTB;NEmuPVQzPSEQvF2= NUPMO2lYW0GQR1XS
NCI-H2087 NGnsc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nud2lEPTB;NEmuPVY5OiEQvF2= MYfTRW5ITVJ?

... 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:

[1]

+ Expand

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:

[1]

+ Expand
  • 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:

[1]

+ Expand
  • 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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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

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  • 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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03727724 Not yet recruiting Carcinoma Non-Small-Cell Lung The Netherlands Cancer Institute|Boehringer Ingelheim|Merck Serono International SA November 2018 Phase 2
NCT03695510 Not yet recruiting Head and Neck Neoplasms National Taiwan University Hospital November 2018 Phase 2
NCT03652233 Not yet recruiting Recurrent Squamous Cell Carcinoma of the Head or Neck|Platinum- and Cetuximab-Refractory Squamous Cell Carcinoma of the Head or Neck|Metastatic Squamous Cell Carcinoma of the Head or Neck|Squamous Cell Carcinoma Vanderbilt-Ingram Cancer Center|National Comprehensive Cancer Network|Boehringer Ingelheim November 2018 Phase 1
NCT03711422 Not yet recruiting Non-small Cell Lung Cancer|Leptomeningeal Disease|Central Nervous System Metastases National Cancer Centre Singapore October 2018 Phase 1
NCT03574402 Not yet recruiting Carcinoma Non-Small-Cell Lung Guangdong Association of Clinical Trials July 1 2018 Phase 2
NCT03083678 Recruiting Chordoma Leiden University Medical Center|Chordoma Foundation|Boehringer Ingelheim June 21 2018 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.

  • * Indicates a Required Field

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