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 175 Publications

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 M4foNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n0TWlEPTB;MD6wNFU4OiEQvF2= NXzucFA1W0GQR1XS
KASUMI-1 M13kPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[2SlBZUUN3ME2wMlAxQTFzIN88US=> NYTnRlJPW0GQR1XS
HCC2218 M3rCSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMEC5PFch|ryP NXL2Z4xbW0GQR1XS
KARPAS-45 M4HwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS5XIVRUUN3ME2wMlAyPjdzIN88US=> M4j5eHNCVkeHUh?=
HSC-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX5TWM2OD1yLkCxO|Q5KM7:TR?= MkKwV2FPT0WU
CHL-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHTd4s1UUN3ME2wMlAyQDN7IN88US=> NFvodXJUSU6JRWK=
KY821 NHTuXY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMEKwOkDPxE1? M2PVcHNCVkeHUh?=
NCI-N87 NGTIN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfINY1KSzVyPUCuNFI4PzNizszN MXLTRW5ITVJ?
DOK NGXa[YVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMEOxPVQh|ryP M1jHVnNCVkeHUh?=
DSH1 NXjNNXB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[4VGlEPTB;MD6wN|MyPCEQvF2= NIHkVWJUSU6JRWK=
MDA-MB-175-VII M1OzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj3TXM2UUN3ME2wMlA{PDF4IN88US=> M4XNdnNCVkeHUh?=
NCI-H2170 M3XETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwMEO3Nlgh|ryP MU\TRW5ITVJ?
BT-474 NITERnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluyTWM2OD1yLkC0PVg3KM7:TR?= NIO5NZRUSU6JRWK=
EFO-27 NVnjcVFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoO2TWM2OD1yLkC1NVgzKM7:TR?= NHjiW2xUSU6JRWK=
NCI-H720 Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwMEWzNlUh|ryP NU\zOINPW0GQR1XS
PC-14 NGmwXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfYTY9PUUN3ME2wMlA2PjZ6IN88US=> NICxZmJUSU6JRWK=
EC-GI-10 NYrT[FE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jzOWlEPTB;MD6wOVkyOiEQvF2= NFfLfXBUSU6JRWK=
KYSE-450 NGPk[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zrd2lEPTB;MD6wOVk4QCEQvF2= MVHTRW5ITVJ?
BPH-1 MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfzR|ZKSzVyPUCuNFU6QDhizszN NGG1TJJUSU6JRWK=
NCI-H292 NGKzflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwME[wPUDPxE1? NIL2TYpUSU6JRWK=
H9 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEexN|Ih|ryP NET6PI1USU6JRWK=
NCI-H526 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXLTWM2OD1yLkC3PFI{KM7:TR?= M3LSOHNCVkeHUh?=
NCI-H1623 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHOc5I3UUN3ME2wMlA5ODJ3IN88US=> NXTsT2J4W0GQR1XS
KYSE-140 NWDCTFZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMEizN{DPxE1? NHfnUm1USU6JRWK=
Ca9-22 MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMEizOVMh|ryP NIj2RnRUSU6JRWK=
AU565 NG[1WJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwMEi1NFQh|ryP NGLsWGRUSU6JRWK=
ZR-75-30 NHHrPHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX3TWM2OD1yLkC5OVQ2KM7:TR?= MkHBV2FPT0WU
NCI-H1770 M4GzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMUCyPEDPxE1? NXHxcYdEW0GQR1XS
LB2241-RCC M3jRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXYbmZZUUN3ME2wMlExQDh2IN88US=> MUjTRW5ITVJ?
CAL-39 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Gzd2lEPTB;MD6xNVc6OiEQvF2= MnzZV2FPT0WU
UACC-893 M3zTTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fLWWlEPTB;MD6xNVg5PSEQvF2= NEf0fZpUSU6JRWK=
LU-65 M{HC[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnXUVJKSzVyPUCuNVI3OzNizszN MVPTRW5ITVJ?
HN MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\xTWM2OD1yLkGzNFc4KM7:TR?= NUXzNHdUW0GQR1XS
TI-73 M3j2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG1PVE5UUN3ME2wMlE1PzF3IN88US=> MYDTRW5ITVJ?
KU812 NXTmfJU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrFT2RKSzVyPUCuNVU1PTZizszN NISxc4hUSU6JRWK=
SW13 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTJVWo3UUN3ME2wMlE3OjF4IN88US=> NW[zSJpRW0GQR1XS
BB30-HNC NVvlb4M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXH[otKSzVyPUCuNVY2PzZizszN MULTRW5ITVJ?
HSC-2 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWwUJNKSzVyPUCuNVY5OzdizszN MVHTRW5ITVJ?
BV-173 Ml7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvyNoN4UUN3ME2wMlE4PTl4IN88US=> MW\TRW5ITVJ?
CAL-27 M{\WTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDkZmVKSzVyPUCuNVc3OzZizszN NUfKdJJoW0GQR1XS
SBC-1 NWLnTpp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPzTWM2OD1yLkG4PVU6KM7:TR?= NUnyeG9qW0GQR1XS
CAL-33 M1zne2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrdZhKSzVyPUCuNlAyQDRizszN NU\ZPWJnW0GQR1XS
NCI-H209 M3;GVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGyOnc{UUN3ME2wMlIxPDZizszN MUjTRW5ITVJ?
COR-L105 NV7xW|NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMkGwPFQh|ryP MoL6V2FPT0WU
HSC-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWxTWM2OD1yLkKxNVk5KM7:TR?= MVvTRW5ITVJ?
NCI-H69 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ISWlEPTB;MD6yNVQ2OSEQvF2= NGjLU5BUSU6JRWK=
MOLT-13 NI\jeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwMkO5O|Uh|ryP NX\zT21NW0GQR1XS
ML-2 M2njb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFez[5dKSzVyPUCuNlQ5ODJizszN NG\pNFVUSU6JRWK=
IGROV-1 NUPDUVQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLlemdJUUN3ME2wMlI2QTV{IN88US=> M{jye3NCVkeHUh?=
TK10 M1i1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m5dGlEPTB;MD6yOlc{QCEQvF2= NVzqR3FVW0GQR1XS
EoL-1-cell NWrEW4tuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG3TWM2OD1yLkK2PFkzKM7:TR?= NGHmSmFUSU6JRWK=
HO-1-N-1 MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKxTWM2OD1yLkK3PFU{KM7:TR?= NGnCXI1USU6JRWK=
BHY NXrPOXVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPQNmV4UUN3ME2wMlI5PjV3IN88US=> MXTTRW5ITVJ?
LU-139 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\sS41FUUN3ME2wMlMxPTFizszN NH\ab4FUSU6JRWK=
23132-87 M2nGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi5OHNGUUN3ME2wMlMyQTJ|IN88US=> M3\PUnNCVkeHUh?=
ACHN NUXCfXVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwM{G5PVQh|ryP MXPTRW5ITVJ?
DoTc2-4510 NFj1S4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLDTWM2OD1yLkOyNlE6KM7:TR?= M1vzT3NCVkeHUh?=
BB65-RCC Mn30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwM{S1PVMh|ryP NIrNeXBUSU6JRWK=
HLE NH\pR3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLITWM2OD1yLkO1NFQ3KM7:TR?= M4T4c3NCVkeHUh?=
HCC1419 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ra[2lEPTB;MD6zOlQxQCEQvF2= MXfTRW5ITVJ?
A388 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHLTWM2OD1yLkO2PFU4KM7:TR?= M2LrdnNCVkeHUh?=
NUGC-3 NFPXeXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLBW2hKSzVyPUCuN|g{PzNizszN NVHNXmJbW0GQR1XS
KYSE-180 NXTYZZZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwM{mwPFkh|ryP NIXjZ5FUSU6JRWK=
TE-6 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwNECyOFYh|ryP MWPTRW5ITVJ?
A498 NV7ufodVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNEC2O|Qh|ryP NIDybFdUSU6JRWK=
NCI-H1648 NEnaSW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXYTWM2OD1yLkS0NVgzKM7:TR?= MXnTRW5ITVJ?
DU-145 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2OxU2lEPTB;MD60OFg{OyEQvF2= NVTYW4JJW0GQR1XS
CW-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmqwTWM2OD1yLkS2PVE1KM7:TR?= M4Tme3NCVkeHUh?=
A431 NH7aN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzpbmxKSzVyPUCuOFgzOzNizszN NUC3TW1PW0GQR1XS
SAS NF7KW4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwNEizPVgh|ryP NGeycYRUSU6JRWK=
NCI-H2126 NHvGcIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnXTWM2OD1yLkWxPVI3KM7:TR?= NV25ZYVvW0GQR1XS
NCI-H358 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7mTWM2OD1yLkWzNlEh|ryP MYnTRW5ITVJ?
FADU M1vnWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLkeIF2UUN3ME2wMlU1PDB2IN88US=> MmrnV2FPT0WU
ACN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXtbG5KSzVyPUCuOVUxQTRizszN MXjTRW5ITVJ?
HCC70 MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvsWGxKUUN3ME2wMlU4PjZzIN88US=> MlXhV2FPT0WU
NCI-H1838 M2TDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPETWM2OD1yLk[wNlk6KM7:TR?= Mm\VV2FPT0WU
CAL-54 M3P4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLlZ4RKSzVyPUCuOlE3OjFizszN M4\iPHNCVkeHUh?=
NCI-H1975 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwNkG3Nlgh|ryP Mli0V2FPT0WU
COR-L88 MmDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwNkSxNVMh|ryP MoXsV2FPT0WU
CTV-1 NYfJbHlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHRSpE5UUN3ME2wMlY1Ozl{IN88US=> MX7TRW5ITVJ?
EW-18 M{TMdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv1TWM2OD1yLk[4Olk5KM7:TR?= MX;TRW5ITVJ?
HCC1806 M4TLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO5N4NKSzVyPUCuOlk3PjZizszN MkDwV2FPT0WU
HuP-T4 NGXleHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLFOJJHUUN3ME2wMlY6PzZizszN MnjWV2FPT0WU
MDA-MB-361 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwN{K2OlIh|ryP NHnFV2lUSU6JRWK=
NCI-H1573 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHaeIlnUUN3ME2wMlc{PjNizszN M4C1[3NCVkeHUh?=
KU-19-19 NHPCUmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1f3OmlEPTB;MD63O|Q3PCEQvF2= NGTJe3ZUSU6JRWK=
COLO-678 MlrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HvWWlEPTB;MD64NFg{PCEQvF2= M2DWRXNCVkeHUh?=
C-33-A MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX3eJlKSzVyPUCuPFEzQTdizszN NU\oPFN3W0GQR1XS
Calu-3 M3S1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPZOoFKSzVyPUCuPFE1OzRizszN MnzPV2FPT0WU
AGS NWq5SHZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zaemlEPTB;MD64N|Y1QCEQvF2= NVTqOVM2W0GQR1XS
SCC-25 NHf4UJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fHT2lEPTB;MD64OFE4OSEQvF2= MoX6V2FPT0WU
JVM-2 NHnJUpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv6WGNKSzVyPUCuPFgzQTlizszN M2fLWnNCVkeHUh?=
HCE-T M4TaN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrZTWM2OD1yLki4OFI5KM7:TR?= NGPnPHZUSU6JRWK=
ES4 MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoWxTWM2OD1yLkm3PFM3KM7:TR?= MXTTRW5ITVJ?
EKVX MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPkTWM2OD1zLkCxNFY1KM7:TR?= MXLTRW5ITVJ?
D-542MG MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWmzcFloUUN3ME2xMlAyODZ2IN88US=> NUKyRnB7W0GQR1XS
SW1116 M{m5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLPTWM2OD1zLkCxNlg4KM7:TR?= NXHVfmxVW0GQR1XS
5637 NEXrWGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;KNG8{UUN3ME2xMlAyPTFizszN NXvYfFB{W0GQR1XS
HT-1376 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfJdIhKSzVyPUGuNFE2OTNizszN NGnsUVBUSU6JRWK=
NB69 MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nBR2lEPTB;MT6wNlk1PSEQvF2= M1nleHNCVkeHUh?=
YKG-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf2T5BKSzVyPUGuNFU1OTlizszN MXHTRW5ITVJ?
EW-3 M4H5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTFwMEe4PFMh|ryP MlLIV2FPT0WU
GCIY MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj5PVJKSzVyPUGuNFgyODRizszN M2jBbnNCVkeHUh?=
SK-MES-1 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnDRW97UUN3ME2xMlEyPDh5IN88US=> NVXQZWw6W0GQR1XS
PANC-08-13 NXHVSoNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjLdppOUUN3ME2xMlE3PDF4IN88US=> MoPHV2FPT0WU
SK-NEP-1 MnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMUe1NVMh|ryP NGfNfnJUSU6JRWK=
SW954 NYnsT21uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC3TWM2OD1zLkKwNlE1KM7:TR?= M2HTcHNCVkeHUh?=
NCI-SNU-5 NH7wRphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DUOmlEPTB;MT6yN|kh|ryP NYT5d5RXW0GQR1XS
SW48 NGDVTm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\4TWM2OD1zLkK1OFMzKM7:TR?= M1:2b3NCVkeHUh?=
HT-3 NX;IbY1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXJfFN7UUN3ME2xMlI5PzV|IN88US=> MVvTRW5ITVJ?
ETK-1 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PrW2lEPTB;MT6zO|Q2PiEQvF2= MlzVV2FPT0WU
SCC-15 NIHvcmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ZeWlEPTB;MT6zPVQ2OSEQvF2= MlL6V2FPT0WU
DU-4475 NUi5fFBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzDTWM2OD1zLkSwNVIyKM7:TR?= NGnRbnlUSU6JRWK=
NB5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnBfYtKSzVyPUGuOFE{OTdizszN NETj[IpUSU6JRWK=
CFPAC-1 MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPNWXhKSzVyPUGuOFI1QTNizszN NWnUeJQ4W0GQR1XS
NCI-H630 NX7he4ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwNEW1PFIh|ryP M3jaNHNCVkeHUh?=
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NOMO-1 Ml:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrGdmZKSzVyPUO0MlU4ODNizszN M3WwdnNCVkeHUh?=
MZ7-mel M37s[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DMbmlEPTB;M{SuOlQ5PyEQvF2= NXvpZmZ5W0GQR1XS
NCI-H810 M1\jVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH2V3drUUN3ME2zOE44Ojd6IN88US=> Mmn6V2FPT0WU
D-392MG M4XqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrpdY9KSzVyPUO1MlA2PjVizszN MYXTRW5ITVJ?
LB771-HNC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL4[GlKSzVyPUO1MlE3PThizszN NVz1d4tIW0GQR1XS
COLO-679 NUi3XFJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O3[GlEPTB;M{WuN|g5KM7:TR?= NHnZc4dUSU6JRWK=
SK-PN-DW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\YTWM2OD1|NT60N|Y6KM7:TR?= Mn2zV2FPT0WU
VA-ES-BJ M131dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnGSnRKSzVyPUO1MlQ3PDlizszN NF\s[WZUSU6JRWK=
KNS-42 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT1TWM2OD1|NT61PFI3KM7:TR?= M1fmZXNCVkeHUh?=
RVH-421 NYThdYYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTN3Lke2OFUh|ryP M1;kN3NCVkeHUh?=
P30-OHK MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:5fVlXUUN3ME2zOU45PzV{IN88US=> MYHTRW5ITVJ?
G-402 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPITWM2OD1|NT65PFY4KM7:TR?= Mnn6V2FPT0WU
S-117 M3;NTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3nTWM2OD1|Nj6zNFA5KM7:TR?= M{PoZ3NCVkeHUh?=
RXF393 M3nCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\YZWlKSzVyPUO2MlM4QDVizszN Mn7VV2FPT0WU
LCLC-103H NYTGbGZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfXTWM2OD1|Nj63PFA{KM7:TR?= MVTTRW5ITVJ?
U-118-MG MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTrRVg6UUN3ME2zOk45QDR5IN88US=> NWS3d2t5W0GQR1XS
8-MG-BA NW\uPHB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f2ZmlEPTB;M{[uPVQ5OyEQvF2= M4j1cXNCVkeHUh?=
MFH-ino MnLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{iyU2lEPTB;M{euN|M4OSEQvF2= NH3yZlJUSU6JRWK=
NCI-H23 NWq2N|JkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPrOoNKSzVyPUO3MlQyQTZizszN M12yXHNCVkeHUh?=
NCI-H446 M2DaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X2NmlEPTB;M{euOFg3OiEQvF2= MmXMV2FPT0WU
LU-99A NYTTdVBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrw[G5KSzVyPUO3MlU4OzFizszN MWTTRW5ITVJ?
KP-N-YN NWj6T2ZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LIc2lEPTB;M{euOlE6PSEQvF2= NGS1coRUSU6JRWK=
SCC-9 NGXOeVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP1PWtlUUN3ME2zO{44QDN6IN88US=> NYiybnBVW0GQR1XS
EFM-19 M17tb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zRe2lEPTB;M{euO|k3PyEQvF2= M1fXcHNCVkeHUh?=
A427 NE\TO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTTSIpRUUN3ME2zO{46OTB5IN88US=> NUjX[XRLW0GQR1XS
LB831-BLC M2LzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTN6Lk[wN|kh|ryP MnPCV2FPT0WU
HOS MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnlU|NKSzVyPUO5MlYzPzNizszN NX\qfHc4W0GQR1XS
LAN-6 NWXLfGtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y0VWlEPTB;NECuNFEyOiEQvF2= MoLXV2FPT0WU
U251 M2nPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTRyLkSwOVQh|ryP M2fGT3NCVkeHUh?=
SNU-387 M4PDd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M324cWlEPTB;NECuOFU2OyEQvF2= MXvTRW5ITVJ?
DMS-79 NGmwOpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmCxTWM2OD12MD61PFg6KM7:TR?= M3fKUnNCVkeHUh?=
SK-LU-1 NULmO2ZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnDTWM2OD12MD62OVY5KM7:TR?= MlTQV2FPT0WU
HT M{XpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvlb3RKSzVyPUSwMlY3OzlizszN NHLxZYdUSU6JRWK=
KP-N-YS MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nVdWlEPTB;NECuOlc3QCEQvF2= NUnOOm5bW0GQR1XS
DMS-114 NIK1bWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zBdWlEPTB;NECuPFM4PCEQvF2= MojEV2FPT0WU
HUTU-80 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTKTWM2OD12MT6wOVY6KM7:TR?= M1rqfnNCVkeHUh?=
ONS-76 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfHPGdKSzVyPUSxMlQ4ODlizszN NUTsRYhiW0GQR1XS
A673 NVTpWJhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi1XVRKSzVyPUSxMlUyPTdizszN M33tR3NCVkeHUh?=
HPAF-II MnTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v5OWlEPTB;NEGuOlcxQSEQvF2= NIrvR5ZUSU6JRWK=
UACC-257 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvVelFqUUN3ME20NU44OzZ7IN88US=> M2fYRXNCVkeHUh?=
EW-22 NYXjUFFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLsNo1KSzVyPUSxMlg3QTdizszN NHnk[HRUSU6JRWK=
NCI-H1755 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17rR2lEPTB;NEGuPFczPSEQvF2= NG\GVm9USU6JRWK=
KYSE-150 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR{LkG3PFIh|ryP MWjTRW5ITVJ?
CGTH-W-1 Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP6R4tSUUN3ME20Nk41QTV3IN88US=> MlLHV2FPT0WU
NB13 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR{Lk[yNVch|ryP MmTDV2FPT0WU
SW872 M1:w[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH6TWM2OD12Mj62N|MyKM7:TR?= M13NTXNCVkeHUh?=
KP-4 M3Xxfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTR{Lki4N|Ih|ryP M4\qUnNCVkeHUh?=
HCC38 NX;sd4VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjm[2NKSzVyPUSyMlk3OThizszN NHmyXoJUSU6JRWK=
BB49-HNC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDMb4JKSzVyPUSzMlI{PTZizszN MlryV2FPT0WU
CAL-62 MoHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fDdWlEPTB;NEOuOFAzQCEQvF2= Mnv6V2FPT0WU
NCI-H2029 MmX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR|LkW1PFEh|ryP M4DnenNCVkeHUh?=
M14 NXu1XmxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HkVmlEPTB;NESuNVM{OiEQvF2= M3\oTnNCVkeHUh?=
COLO-680N MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFKweYlKSzVyPUS0MlM{QSEQvF2= Mn62V2FPT0WU
Hs-578-T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrrcIdKSzVyPUS1MlAzQTRizszN MlS0V2FPT0WU
MSTO-211H MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXX6[4Y2UUN3ME20OU46PDh{IN88US=> MVzTRW5ITVJ?
EW-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3OTWM2OD12NT65Olg6KM7:TR?= NFHVWYxUSU6JRWK=
SW948 NVHzWJlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIeyco5KSzVyPUS2MlQ1PjJizszN MoK2V2FPT0WU
NCI-H460 NVSzWFV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml21TWM2OD12Nj61NlMh|ryP NW\VTZZZW0GQR1XS
CAS-1 Mn;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLJT4lKSzVyPUS2Mlc4ODFizszN M4LnSnNCVkeHUh?=
TGBC11TKB NHn2Z3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrVWZFKSzVyPUS3MlE4PzdizszN NISwWHdUSU6JRWK=
HD-MY-Z MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37FPWlEPTB;NEiuO|g3KM7:TR?= NIP4UWxUSU6JRWK=
NCI-H226 Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzRfVhKSzVyPUS5Mlc4QDVizszN MYHTRW5ITVJ?
PA-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r5dmlEPTB;NEmuPFM{PSEQvF2= NHXMbGJUSU6JRWK=
LB2518-MEL NIPXNFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTR7Lki3NlMh|ryP MnnHV2FPT0WU
A101D MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzyO4VKSzVyPUS5Mlk1OjVizszN MWLTRW5ITVJ?
NCI-H2087 M37EdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LzdmlEPTB;NEmuPVY5OiEQvF2= M2jhdHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CIP2A / p-AKT / AKT / PARP; 

PubMed: 25537503     


Time-dependent effects of afatinib on CIP2A, p-AKT and apoptosis-related proteins in the sensitive H358 and resistant H460 cells. Cells were exposed to 10 μM afatinib for up to 48 hours. Immunoblots were scanned and quantitated to determine the ratio of the level of CIP2A to actin. Data are mean ± SD. n = 3 for the different time intervals.

p-EGFR / p-IGF1R / p-ERK / p-AKT; 

PubMed: 26052929     


Effects of afatinib on EGFR and IGF1R Signaling Pathways. H1975 cells were treated with afatinib with various doses and cell lysates were subjected to Western blot analysis. Afatinib effectively inhibits p-EGFR and p-ERK while p-AKT was partially inhibited. IGF1R phosphorylation was increased upon afatinib treatment in H1975 cells.

p-VEGFR2 / VEGFR2 / JAG1 / DLL4 / NICD1 ; 

PubMed: 28533486     


HUVECs were cultured in the presence of Vatalanib (100 nM) or DBZ (10 nM) for 1 h and then treated for 15 min with rhgal-3 (37 nM) and cultured for additional 6 hrs. After this period, the total protein was isolated and the protein levels of galectin-3, NICD1, DLL4, JAG1, VEGFR2 and VEGFR2-p were assessed by Western blot. β-actin was used as a loading control.

25537503 26052929 28533486
Growth inhibition assay
Cell apoptosis; 

PubMed: 25537503     


Dose-dependent effects of afatinib on apoptosis. Data are mean ± SD. n = 3 for each concentration. *, p < 0.05, **, p < 0.01, vs. no afatinib. 

Cell viability; 

PubMed: 26515464     


A. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion and L858R. The proportional cell viability is shown. B. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion+T790M and L858R+T790M. The proportional cell viability is shown. C. MTS assay for Ba/F3 cells harboring wild type EGFR. The proportional cell viability is shown. Erlotinib, afatinib, osimertinib, and rociletinib were used as EGFR-TKIs. Error bars indicate standard deviation.

25537503 26515464
Immunofluorescence
p65; 

PubMed: 26317651     


Effects of different treatments on the nuclear translocation of the NF-κB subunit p65. A2780T cells were treated with 2.5 μM afatinib for 48 hours, or 10 μM PDTC for 2 hours. Subsequently, the NF-κB subunit p65 (red) was localized by immunofluorescence and a confocal microscopy. Nuclei were stained with DAPI (blue). Scale bar = 10 μM.

vacuoles; 

PubMed: 29713246     


Autophagy activation upon treatment with Afatinib and Sorafenib was validated using immunofluorescence in order to visualize a creation of autophagosomes; ×60 magnification. DMSO treatment was used as control. Green—autophagy vacuoles; Blue—Hoechst, nuclear staining. 

26317651 29713246
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]

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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:

[1]

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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:

[1]

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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 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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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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 )

  • C1
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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):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03711422 Not yet recruiting Drug: Afatinib Non-small Cell Lung Cancer|Leptomeningeal Disease|Central Nervous System Metastases National Cancer Centre Singapore October 2018 Phase 1
NCT03083678 Recruiting Drug: Afatinib Chordoma Leiden University Medical Center|Chordoma Foundation|Boehringer Ingelheim June 21 2018 Phase 2
NCT03370770 Active not recruiting Drug: Afatinib|Drug: Osimertinib Carcinoma Non-Small-Cell Lung Boehringer Ingelheim December 28 2017 --
NCT02423525 Recruiting Drug: Afatinib Brain Cancer Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute December 2016 Phase 1
NCT02695290 Terminated Drug: Afatinib Carcinoma Non-Small-Cell Lung|ErbB Receptors Boehringer Ingelheim March 17 2016 Phase 4
NCT02171741 Completed Drug: BIBW 2992|Drug: Docetaxel Neoplasms Boehringer Ingelheim April 2005 Phase 1

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