Afatinib (BIBW2992)

For research use only.

Catalog No.S1011

201 publications

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. Afatinib induces autophagy.

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Selleck's Afatinib (BIBW2992) has been cited by 201 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. Afatinib induces autophagy.
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 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEX3TFNKSzVyPUCuNFA2PzJizszN NF3LTotUSU6JRWK=
KASUMI-1 NH7qXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwMEC5NVEh|ryP NF;KfVJUSU6JRWK=
HCC2218 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiw[2NEUUN3ME2wMlAxQTh5IN88US=> MUPTRW5ITVJ?
KARPAS-45 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwMEG2O|Eh|ryP M1G5XXNCVkeHUh?=
HSC-4 M3zV[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHnXItFUUN3ME2wMlAyPzR6IN88US=> NHLF[|FUSU6JRWK=
CHL-1 MlnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3ZTpJFUUN3ME2wMlAyQDN7IN88US=> MX7TRW5ITVJ?
KY821 NYrUXIRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMEKwOkDPxE1? MlPGV2FPT0WU
NCI-N87 MnGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTmTWM2OD1yLkCyO|c{KM7:TR?= MWXTRW5ITVJ?
DOK MoDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PIXmlEPTB;MD6wN|E6PCEQvF2= MUXTRW5ITVJ?
DSH1 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwMEOzNVQh|ryP NVTodZZRW0GQR1XS
MDA-MB-175-VII M134bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG4TWM2OD1yLkCzOFE3KM7:TR?= MlG1V2FPT0WU
NCI-H2170 NXLDdndLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnGRYg6UUN3ME2wMlA{PzJ6IN88US=> NIfNXIJUSU6JRWK=
BT-474 MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwMES5PFYh|ryP MYXTRW5ITVJ?
EFO-27 NW\Ge4FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme4TWM2OD1yLkC1NVgzKM7:TR?= NYHqTY1VW0GQR1XS
NCI-H720 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;sOGI4UUN3ME2wMlA2OzJ3IN88US=> NGrYZlhUSU6JRWK=
PC-14 NV;I[VBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwMEW2Olgh|ryP M2OyZnNCVkeHUh?=
EC-GI-10 NVXa[opRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEG2[lJKSzVyPUCuNFU6OTJizszN M4XSbHNCVkeHUh?=
KYSE-450 NFnwWoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXZeo5rUUN3ME2wMlA2QTd6IN88US=> NUnBW4FkW0GQR1XS
BPH-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfJVXJuUUN3ME2wMlA2QTh6IN88US=> NHvvRZhUSU6JRWK=
NCI-H292 M37nZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyxXXg3UUN3ME2wMlA3ODlizszN M{DNdXNCVkeHUh?=
H9 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrIbXpzUUN3ME2wMlA4OTN{IN88US=> M1TGSnNCVkeHUh?=
NCI-H526 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vxTWlEPTB;MD6wO|gzOyEQvF2= NHm5bZZUSU6JRWK=
NCI-H1623 NUe5SppuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP4cJkzUUN3ME2wMlA5ODJ3IN88US=> MUXTRW5ITVJ?
KYSE-140 NIfzN29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMEizN{DPxE1? NVLsfVF1W0GQR1XS
Ca9-22 Mo\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWxSodKSzVyPUCuNFg{PTNizszN NFvMS|NUSU6JRWK=
AU565 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H3S2lEPTB;MD6wPFUxPCEQvF2= MXjTRW5ITVJ?
ZR-75-30 NWTyPJA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwMEm1OFUh|ryP NUfqcldVW0GQR1XS
NCI-H1770 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnOwTWM2OD1yLkGwNlgh|ryP NUHPcIkxW0GQR1XS
LB2241-RCC NIjsSYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2npVmlEPTB;MD6xNFg5PCEQvF2= NIfWVoxUSU6JRWK=
CAL-39 M3PqNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTkTWM2OD1yLkGxO|kzKM7:TR?= Mn;LV2FPT0WU
UACC-893 NETXVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMUG4PFUh|ryP Mn3SV2FPT0WU
LU-65 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;kW|NKSzVyPUCuNVI3OzNizszN MkHZV2FPT0WU
HN MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHMTWM2OD1yLkGzNFc4KM7:TR?= MmLBV2FPT0WU
TI-73 M3;GVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX60[JVRUUN3ME2wMlE1PzF3IN88US=> M4HxenNCVkeHUh?=
KU812 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3wTWM2OD1yLkG1OFU3KM7:TR?= MmrwV2FPT0WU
SW13 NGH6[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml74TWM2OD1yLkG2NlE3KM7:TR?= NHHJ[|NUSU6JRWK=
BB30-HNC NHXEdYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\XN4hKSzVyPUCuNVY2PzZizszN MUjTRW5ITVJ?
HSC-2 MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknBTWM2OD1yLkG2PFM4KM7:TR?= MWrTRW5ITVJ?
BV-173 NUP2VVFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\iTWM2OD1yLkG3OVk3KM7:TR?= MknPV2FPT0WU
CAL-27 M2TpNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPiS3F{UUN3ME2wMlE4PjN4IN88US=> NF;zSJpUSU6JRWK=
SBC-1 M{\vXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[wTWM2OD1yLkG4PVU6KM7:TR?= M3ewbXNCVkeHUh?=
CAL-33 NVLvVGU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\KeHlMUUN3ME2wMlIxOTh2IN88US=> MV\TRW5ITVJ?
NCI-H209 NWHwcJhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTOTWM2OD1yLkKwOFYh|ryP MnPDV2FPT0WU
COR-L105 NYLYNVhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHXTWM2OD1yLkKxNFg1KM7:TR?= MkLqV2FPT0WU
HSC-3 NWL0NItsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHCTWM2OD1yLkKxNVk5KM7:TR?= NF[wdZVUSU6JRWK=
NCI-H69 M4X3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnobJhyUUN3ME2wMlIyPDVzIN88US=> M2LxOXNCVkeHUh?=
MOLT-13 NX3ZUoVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTBwMkO5O|Uh|ryP M{nucHNCVkeHUh?=
ML-2 NXKxboNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTzTWM2OD1yLkK0PFAzKM7:TR?= Mn3PV2FPT0WU
IGROV-1 M1jWdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[0TWM2OD1yLkK1PVUzKM7:TR?= MknXV2FPT0WU
TK10 NYryUo9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMk[3N|gh|ryP M4OyUXNCVkeHUh?=
EoL-1-cell NFzPSndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16yeGlEPTB;MD6yOlg6OiEQvF2= NXXwUJZ6W0GQR1XS
HO-1-N-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLTTWM2OD1yLkK3PFU{KM7:TR?= M2PUXnNCVkeHUh?=
BHY MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPITWM2OD1yLkK4OlU2KM7:TR?= Ml7ZV2FPT0WU
LU-139 NWDJcnZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHz[JZCUUN3ME2wMlMxPTFizszN M{HHcHNCVkeHUh?=
23132-87 MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz6Z4NKSzVyPUCuN|E6OjNizszN MmXFV2FPT0WU
ACHN NF\xSHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX2dIxKUUN3ME2wMlMyQTl2IN88US=> M{HQPXNCVkeHUh?=
DoTc2-4510 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnFUlBKSzVyPUCuN|IzOTlizszN MVvTRW5ITVJ?
BB65-RCC NIewVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrPZ3k{UUN3ME2wMlM1PTl|IN88US=> MVXTRW5ITVJ?
HLE MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwM{WwOFYh|ryP NWTDb5VmW0GQR1XS
HCC1419 NHmwWnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL2TphKSzVyPUCuN|Y1ODhizszN NYPac2NOW0GQR1XS
A388 MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkK3TWM2OD1yLkO2PFU4KM7:TR?= NYPpc25RW0GQR1XS
NUGC-3 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jOUWlEPTB;MD6zPFM4OyEQvF2= NV7QeZc5W0GQR1XS
KYSE-180 NFS1SIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TZNWlEPTB;MD6zPVA5QSEQvF2= NHns[ItUSU6JRWK=
TE-6 NH:0eZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz3UJNIUUN3ME2wMlQxOjR4IN88US=> NWKxTnRVW0GQR1XS
A498 Mm\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn30TWM2OD1yLkSwOlc1KM7:TR?= M3j5fHNCVkeHUh?=
NCI-H1648 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwNESxPFIh|ryP NV61Now4W0GQR1XS
DU-145 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\qW5RKSzVyPUCuOFQ5OzNizszN NWLvdGt5W0GQR1XS
CW-2 NYK1OHJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j3b2lEPTB;MD60OlkyPCEQvF2= MonpV2FPT0WU
A431 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjjXIVlUUN3ME2wMlQ5OjN|IN88US=> MWfTRW5ITVJ?
SAS NWnydHJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;3ZVhKSzVyPUCuOFg{QThizszN NF;HVZpUSU6JRWK=
NCI-H2126 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;iSZhKSzVyPUCuOVE6OjZizszN M1vWWXNCVkeHUh?=
NCI-H358 NHPvZ|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH6zWHRKSzVyPUCuOVMzOSEQvF2= NG\0ToVUSU6JRWK=
FADU MkHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm2TWM2OD1yLkW0OFA1KM7:TR?= MWHTRW5ITVJ?
ACN MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHqx[m5KSzVyPUCuOVUxQTRizszN Ml3kV2FPT0WU
HCC70 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXwepNNUUN3ME2wMlU4PjZzIN88US=> NUPXU2pPW0GQR1XS
NCI-H1838 M{TGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\iUoxKSzVyPUCuOlAzQTlizszN NH62cmVUSU6JRWK=
CAL-54 M1:zXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfyTYhoUUN3ME2wMlYyPjJzIN88US=> MWfTRW5ITVJ?
NCI-H1975 MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHVc4N7UUN3ME2wMlYyPzJ6IN88US=> NVfOW5JKW0GQR1XS
COR-L88 NE\mWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnveFVqUUN3ME2wMlY1OTF|IN88US=> NFKxTHRUSU6JRWK=
CTV-1 NFGxSoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LIbmlEPTB;MD62OFM6OiEQvF2= MlXYV2FPT0WU
EW-18 NHLuVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwNki2PVgh|ryP NFT2OY1USU6JRWK=
HCC1806 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwNkm2OlYh|ryP NVHkdGQyW0GQR1XS
HuP-T4 NVHt[ItJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP1TWM2OD1yLk[5O|Yh|ryP NXLQNIFiW0GQR1XS
MDA-MB-361 MlHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITnToZKSzVyPUCuO|I3PjJizszN MnPHV2FPT0WU
NCI-H1573 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe2UFVFUUN3ME2wMlc{PjNizszN M4XFXXNCVkeHUh?=
KU-19-19 NIXFc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrnWHVKSzVyPUCuO|c1PjRizszN NYfNRXVJW0GQR1XS
COLO-678 NFjSU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S5eGlEPTB;MD64NFg{PCEQvF2= NH3MRnRUSU6JRWK=
C-33-A NXXsNHdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorYTWM2OD1yLkixNlk4KM7:TR?= NUXYd2JFW0GQR1XS
Calu-3 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXR2lEPTB;MD64NVQ{PCEQvF2= NFPKfZJUSU6JRWK=
AGS MmjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPmd|I5UUN3ME2wMlg{PjR6IN88US=> NWHDZot2W0GQR1XS
SCC-25 NIjWb|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLXb29bUUN3ME2wMlg1OTdzIN88US=> NFvZdGJUSU6JRWK=
JVM-2 NYj6R4dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHhT4tKSzVyPUCuPFgzQTlizszN M4nabnNCVkeHUh?=
HCE-T M3z1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPqfoZKSzVyPUCuPFg1OjhizszN NX\1TY5TW0GQR1XS
ES4 NUfxO4s2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfQTWM2OD1yLkm3PFM3KM7:TR?= MoDyV2FPT0WU
EKVX M1yxfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfTO4FKSzVyPUGuNFExPjRizszN MnP0V2FPT0WU
D-542MG NV:3RZEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDnR2xyUUN3ME2xMlAyODZ2IN88US=> Moj6V2FPT0WU
SW1116 NWf0bWNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFwMEGyPFch|ryP NGCwWFhUSU6JRWK=
5637 NWDadY41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjuO215UUN3ME2xMlAyPTFizszN MX;TRW5ITVJ?
HT-1376 NV\GRWdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\td|BKSzVyPUGuNFE2OTNizszN M4i0XXNCVkeHUh?=
NB69 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPkWJJKSzVyPUGuNFI6PDVizszN M13J[nNCVkeHUh?=
YKG-1 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjH[JpSUUN3ME2xMlA2PDF7IN88US=> MVPTRW5ITVJ?
EW-3 NEHidZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnzTIFKUUN3ME2xMlA4QDh|IN88US=> M{PQNnNCVkeHUh?=
GCIY NVy3PFJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jFTGlEPTB;MT6wPFExPCEQvF2= M{DZWXNCVkeHUh?=
SK-MES-1 NG\ucYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHxTWM2OD1zLkGxOFg4KM7:TR?= M{TsZ3NCVkeHUh?=
PANC-08-13 NV;FNYdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL6TWM2OD1zLkG2OFE3KM7:TR?= NF\ueFRUSU6JRWK=
SK-NEP-1 NFfRWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nGSWlEPTB;MT6xO|UyOyEQvF2= NHyxfYhUSU6JRWK=
SW954 NHP2cXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrHNXJRUUN3ME2xMlIxOjF2IN88US=> NVvBbnpZW0GQR1XS
NCI-SNU-5 NFPjOHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFwMkO5JO69VQ>? MmTSV2FPT0WU
SW48 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfHTWM2OD1zLkK1OFMzKM7:TR?= MVPTRW5ITVJ?
HT-3 NGm1V3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFwMki3OVMh|ryP NIfKT21USU6JRWK=
ETK-1 NVHscFNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn6TWM2OD1zLkO3OFU3KM7:TR?= M{\FR3NCVkeHUh?=
SCC-15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zGdGlEPTB;MT6zPVQ2OSEQvF2= M1;JZnNCVkeHUh?=
DU-4475 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYizcFNrUUN3ME2xMlQxOTJzIN88US=> NFr5eFJUSU6JRWK=
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CFPAC-1 M4nVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\ZTWM2OD1zLkSyOFk{KM7:TR?= M{CyWXNCVkeHUh?=
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NCI-H1703 NGju[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTlwM{SzO|Uh|ryP MofzV2FPT0WU
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CAL-72 NWTrbW5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3FVYZ[UUN3ME2xNE46OzlzIN88US=> NHz2VlRUSU6JRWK=
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MDA-MB-453 NHTSbJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T1XGlEPTB;MUGuPVUyPSEQvF2= NFTlXmdUSU6JRWK=
NCI-H596 NYizSnQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm2ZVVqUUN3ME2xNk4xOzZ7IN88US=> NXT0ZppJW0GQR1XS
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DBTRG-05MG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnNTWM2OD1zMz6wOlMzKM7:TR?= NGP6[|JUSU6JRWK=
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OVCAR-5 M1nZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX6TldGUUN3ME2xN{4yPTl|IN88US=> NYrQUINmW0GQR1XS
8505C M2fQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLjTWM2OD1zMz6yNFY4KM7:TR?= M2\MRXNCVkeHUh?=
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EW-13 M2jhcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknVTWM2OD1zND6wN|UzKM7:TR?= M3OzZ3NCVkeHUh?=
NCI-H1793 MnHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXjN4hKSzVyPUG0MlIxQDdizszN NVTxS4NQW0GQR1XS
BHT-101 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjHSmpPUUN3ME2xOE4zPDFizszN NFPhVolUSU6JRWK=
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NEC8 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS5[JQ3UUN3ME2xOE42PDd{IN88US=> MY\TRW5ITVJ?
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NCI-H2030 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2racWlEPTB;MUSuOlQ1QCEQvF2= NHnkSm9USU6JRWK=
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SW1463 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rVfWlEPTB;MUWuNFQ5PSEQvF2= MYrTRW5ITVJ?
J82 NH7G[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHFOZpKSzVyPUG1MlA2PyEQvF2= MVvTRW5ITVJ?
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NCI-H1092 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP4fHVKSzVyPUG2Mlg{OTZizszN MUPTRW5ITVJ?
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RH-18 M{fuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn4SpRKSzVyPUG4MlAxOzVizszN NHjZR5ZUSU6JRWK=
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SCH NV;PXYtsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLX[YIyUUN3ME2xPE43PDV4IN88US=> M1HyOnNCVkeHUh?=
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ABC-1 NWnZZ40xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4j4WmlEPTB;M{SuN|Y6OyEQvF2= NXfTNY5OW0GQR1XS
NCI-H1355 NYnFXnF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN2LkO4PFkh|ryP NIr4PVBUSU6JRWK=
NOMO-1 M3PsWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnoTWM2OD1|ND61O|A{KM7:TR?= M2fNUnNCVkeHUh?=
MZ7-mel NHqxcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTN2Lk[0PFch|ryP MWTTRW5ITVJ?
NCI-H810 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{mx[2lEPTB;M{SuO|I4QCEQvF2= M3TCe3NCVkeHUh?=
D-392MG NGe2SFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2H4NmlEPTB;M{WuNFU3PSEQvF2= MUHTRW5ITVJ?
LB771-HNC MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTN3LkG2OVgh|ryP M3HWbXNCVkeHUh?=
COLO-679 M1z0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ToeGlEPTB;M{WuN|g5KM7:TR?= M1LaS3NCVkeHUh?=
SK-PN-DW NXL1OXJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfhco5KSzVyPUO1MlQ{PjlizszN NUHEOVlRW0GQR1XS
VA-ES-BJ MkHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XnR2lEPTB;M{WuOFY1QSEQvF2= MUjTRW5ITVJ?
KNS-42 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPCPGZCUUN3ME2zOU42QDJ4IN88US=> M2LZV3NCVkeHUh?=
RVH-421 NIrCeVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXQO4tKSzVyPUO1Mlc3PDVizszN MkXaV2FPT0WU
P30-OHK NGXUWGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTN3Lki3OVIh|ryP M1yxdXNCVkeHUh?=
G-402 NEDCenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTN3Lkm4Olch|ryP MYHTRW5ITVJ?
S-117 NFLqbYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN4LkOwNFgh|ryP NGrSW|hUSU6JRWK=
RXF393 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvHXnVKSzVyPUO2MlM4QDVizszN M3vYbnNCVkeHUh?=
LCLC-103H MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPsVpRKSzVyPUO2Mlc5ODNizszN NYnCbpBjW0GQR1XS
U-118-MG MnjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTN4Lki4OFch|ryP MVvTRW5ITVJ?
8-MG-BA NHrpUZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTN4Lkm0PFMh|ryP NYrVR4R[W0GQR1XS
MFH-ino NWDQXIJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTN5LkOzO|Eh|ryP MnvrV2FPT0WU
NCI-H23 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrxTZdsUUN3ME2zO{41OTl4IN88US=> NUjV[3lxW0GQR1XS
NCI-H446 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG0[I8xUUN3ME2zO{41QDZ{IN88US=> MlfNV2FPT0WU
LU-99A MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm3TWM2OD1|Nz61O|MyKM7:TR?= MmfjV2FPT0WU
KP-N-YN NUXqO5lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrFZ2ZYUUN3ME2zO{43OTl3IN88US=> MWjTRW5ITVJ?
SCC-9 M3[wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTN5Lke4N|gh|ryP MXnTRW5ITVJ?
EFM-19 M3PDSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:5bFlKSzVyPUO3Mlc6PjdizszN MlfTV2FPT0WU
A427 M{nVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\ndWRKSzVyPUO3MlkyODdizszN MUfTRW5ITVJ?
LB831-BLC M{Htcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvyPI1KSzVyPUO4MlYxOzlizszN NH;LTXNUSU6JRWK=
HOS NGPoO|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP2V4R1UUN3ME2zPU43Ojd|IN88US=> NEjjOHJUSU6JRWK=
LAN-6 M4DjOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHkN3pKSzVyPUSwMlAyOTJizszN MoLyV2FPT0WU
U251 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTRyLkSwOVQh|ryP MoXyV2FPT0WU
SNU-387 NUXvSnpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDBbFdKSzVyPUSwMlQ2PTNizszN MlzuV2FPT0WU
DMS-79 NYn5R2RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXKTWM2OD12MD61PFg6KM7:TR?= NIDSU2RUSU6JRWK=
SK-LU-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrhOJVKSzVyPUSwMlY2PjhizszN NFXSb4VUSU6JRWK=
HT M1LBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO1eFhPUUN3ME20NE43PjN7IN88US=> MnLnV2FPT0WU
KP-N-YS Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr3[3ltUUN3ME20NE43PzZ6IN88US=> NV\0V4pOW0GQR1XS
DMS-114 NHPN[2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\pbmlEPTB;NECuPFM4PCEQvF2= MoXJV2FPT0WU
HUTU-80 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7rWFF7UUN3ME20NU4xPTZ7IN88US=> M2rJfXNCVkeHUh?=
ONS-76 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DBPGlEPTB;NEGuOFcxQSEQvF2= NYDpOINUW0GQR1XS
A673 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXkNZFvUUN3ME20NU42OTV5IN88US=> MoLtV2FPT0WU
HPAF-II NHr5O5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvGTWM2OD12MT62O|A6KM7:TR?= M37iZXNCVkeHUh?=
UACC-257 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn3[JpKSzVyPUSxMlc{PjlizszN MUnTRW5ITVJ?
EW-22 NHLCWnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTRzLki2PVch|ryP NHTXbFJUSU6JRWK=
NCI-H1755 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\BTWM2OD12MT64O|I2KM7:TR?= MXHTRW5ITVJ?
KYSE-150 NG[0VW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTR{LkG3PFIh|ryP M2iy[XNCVkeHUh?=
CGTH-W-1 Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR{LkS5OVUh|ryP M13Jb3NCVkeHUh?=
NB13 NXG5d3BJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrNcYdKSzVyPUSyMlYzOTdizszN M4jvSnNCVkeHUh?=
SW872 NILCRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH0TWM2OD12Mj62N|MyKM7:TR?= M13sWnNCVkeHUh?=
KP-4 M{LvWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3iZowyUUN3ME20Nk45QDN{IN88US=> MULTRW5ITVJ?
HCC38 MmTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHwc2lKSzVyPUSyMlk3OThizszN M3W4U3NCVkeHUh?=
BB49-HNC NEPMPYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\JTGlEPTB;NEOuNlM2PiEQvF2= MVfTRW5ITVJ?
CAL-62 MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjCN4JKSzVyPUSzMlQxOjhizszN NGXhUo9USU6JRWK=
NCI-H2029 M4jzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3BTWM2OD12Mz61OVgyKM7:TR?= M{iwbXNCVkeHUh?=
M14 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKzTWM2OD12ND6xN|MzKM7:TR?= NYfqUo1{W0GQR1XS
COLO-680N M2fZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3TbnI3UUN3ME20OE4{OzlizszN NWnOU4JXW0GQR1XS
Hs-578-T NHP2eWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTR3LkCyPVQh|ryP NVLLZmZFW0GQR1XS
MSTO-211H MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zzZmlEPTB;NEWuPVQ5OiEQvF2= M4D4Z3NCVkeHUh?=
EW-1 NFXzOpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPwTWM2OD12NT65Olg6KM7:TR?= M2HSVHNCVkeHUh?=
SW948 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWr1fpBmUUN3ME20Ok41PDZ{IN88US=> MnzSV2FPT0WU
NCI-H460 M3Py[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfIfVhKSzVyPUS2MlUzOyEQvF2= M4XISnNCVkeHUh?=
CAS-1 MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn0fIFKSzVyPUS2Mlc4ODFizszN NGL4UI1USU6JRWK=
TGBC11TKB NIrkNmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml65TWM2OD12Nz6xO|c4KM7:TR?= MYHTRW5ITVJ?
HD-MY-Z MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWP1ZohCUUN3ME20PE44QDZizszN MmjtV2FPT0WU
NCI-H226 Ml7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILIRYhKSzVyPUS5Mlc4QDVizszN M132cXNCVkeHUh?=
PA-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\aZpg2UUN3ME20PU45OzN3IN88US=> NIXMbHVUSU6JRWK=
LB2518-MEL MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Hw[mlEPTB;NEmuPFczOyEQvF2= M3;2OnNCVkeHUh?=
A101D NFHaV|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLITZQ4UUN3ME20PU46PDJ3IN88US=> MV7TRW5ITVJ?
NCI-H2087 NWn1W3BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;FeWlEPTB;NEmuPVY5OiEQvF2= NXvtblBGW0GQR1XS

... 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
  • 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
Smiles CN(C)C/C=C/C(=O)NC1=CC2=C(NC3=CC=C(F)C(=C3)Cl)N=CN=C2C=C1OC4CCOC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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
    Concentration
    Volume
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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
    V1
    C2
    V2

* 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):
    C7=C6/X C7: LOG(C7):
    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
NCT04206787 Not yet recruiting Drug: Afatinib Non-squamous Non-Small Cell Lung Cancer Boehringer Ingelheim May 6 2020 --
NCT04158947 Recruiting Drug: Afatinib|Drug: T-DM1 HER2-positive Breast Cancer|Brain Metastases xuexin he|Second Affiliated Hospital School of Medicine Zhejiang University May 10 2020 Phase 2
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 Completed 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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID