Afatinib (BIBW2992)

For research use only.

Catalog No.S1011

244 publications

Afatinib (BIBW2992) Chemical Structure

CAS No. 850140-72-6

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 244 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 M1qxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTaR3M4UUN3ME2wMlAxPTd{IN88US=> M1nSPHNCVkeHUh?=
KASUMI-1 NV;sZ4V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzRVI1KSzVyPUCuNFA6OTFizszN NWfUV3g3W0GQR1XS
HCC2218 NYHidGRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLI[nhWUUN3ME2wMlAxQTh5IN88US=> NX2yeZl[W0GQR1XS
KARPAS-45 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33sZ2lEPTB;MD6wNVY4OSEQvF2= NIn3cIxUSU6JRWK=
HSC-4 NV3n[pQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nVVmlEPTB;MD6wNVc1QCEQvF2= MnzUV2FPT0WU
CHL-1 NHrPSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2KxRWlEPTB;MD6wNVg{QSEQvF2= MmLaV2FPT0WU
KY821 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDMTWM2OD1yLkCyNFYh|ryP MnzCV2FPT0WU
NCI-N87 Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3TeZhUUUN3ME2wMlAzPzd|IN88US=> NUiySVkxW0GQR1XS
DOK M3r1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjxRoVKSzVyPUCuNFMyQTRizszN Mo\SV2FPT0WU
DSH1 MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\JTWM2OD1yLkCzN|E1KM7:TR?= Mm\WV2FPT0WU
MDA-MB-175-VII MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMEO0NVYh|ryP NW\QemZOW0GQR1XS
NCI-H2170 M4DCbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr6XY5iUUN3ME2wMlA{PzJ6IN88US=> M{juZXNCVkeHUh?=
BT-474 NVv1cJg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMES5PFYh|ryP NUHv[XFGW0GQR1XS
EFO-27 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn2TWM2OD1yLkC1NVgzKM7:TR?= NX7CUYxmW0GQR1XS
NCI-H720 M3\jSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMEWzNlUh|ryP NWK5doU5W0GQR1XS
PC-14 M3vl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHiTWM2OD1yLkC1OlY5KM7:TR?= MYPTRW5ITVJ?
EC-GI-10 NFyxO5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLSdYZHUUN3ME2wMlA2QTF{IN88US=> MVjTRW5ITVJ?
KYSE-450 NXrUTIlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTZTWM2OD1yLkC1PVc5KM7:TR?= MVfTRW5ITVJ?
BPH-1 MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX3TWM2OD1yLkC1PVg5KM7:TR?= Mm\kV2FPT0WU
NCI-H292 Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwME[wPUDPxE1? NE\JbVRUSU6JRWK=
H9 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX6TWM2OD1yLkC3NVMzKM7:TR?= M17oc3NCVkeHUh?=
NCI-H526 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7D[FhKSzVyPUCuNFc5OjNizszN MV3TRW5ITVJ?
NCI-H1623 M13qWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TCdWlEPTB;MD6wPFAzPSEQvF2= NU\oR3JGW0GQR1XS
KYSE-140 NIe3XHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMEizN{DPxE1? MoTKV2FPT0WU
Ca9-22 M3[1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonITWM2OD1yLkC4N|U{KM7:TR?= NHzxUmhUSU6JRWK=
AU565 NGDySXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjTWZlrUUN3ME2wMlA5PTB2IN88US=> Ml\oV2FPT0WU
ZR-75-30 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlntTWM2OD1yLkC5OVQ2KM7:TR?= M4TLZXNCVkeHUh?=
NCI-H1770 NI\4XHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMUCyPEDPxE1? NUfqb|RYW0GQR1XS
LB2241-RCC M2HEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljzTWM2OD1yLkGwPFg1KM7:TR?= M4m2OnNCVkeHUh?=
CAL-39 NVvtV21zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFSzUmlKSzVyPUCuNVE4QTJizszN MYPTRW5ITVJ?
UACC-893 NWXXNmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3zXG5KSzVyPUCuNVE5QDVizszN MmX6V2FPT0WU
LU-65 M1;UXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzVVHFKSzVyPUCuNVI3OzNizszN M1OydHNCVkeHUh?=
HN MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7kepBKSzVyPUCuNVMxPzdizszN MVfTRW5ITVJ?
TI-73 NFPIcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jxTmlEPTB;MD6xOFcyPSEQvF2= M4PUbnNCVkeHUh?=
KU812 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\kZXJKSzVyPUCuNVU1PTZizszN NWD3Z2pXW0GQR1XS
SW13 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMU[yNVYh|ryP NFfqVWdUSU6JRWK=
BB30-HNC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3W1V2lEPTB;MD6xOlU4PiEQvF2= NYrzTWpVW0GQR1XS
HSC-2 NHLx[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PNZ2lEPTB;MD6xOlg{PyEQvF2= MXXTRW5ITVJ?
BV-173 NYXoXI5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTBTWM2OD1yLkG3OVk3KM7:TR?= MWXTRW5ITVJ?
CAL-27 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPST2FKSzVyPUCuNVc3OzZizszN NFjBPINUSU6JRWK=
SBC-1 M3znWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O4ZmlEPTB;MD6xPFk2QSEQvF2= NUHaZ4V5W0GQR1XS
CAL-33 M{eybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwMkCxPFQh|ryP NWfwXmJsW0GQR1XS
NCI-H209 NVHlWGprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfWTWM2OD1yLkKwOFYh|ryP NUfoXpltW0GQR1XS
COR-L105 M1naemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojUTWM2OD1yLkKxNFg1KM7:TR?= M1;jOnNCVkeHUh?=
HSC-3 NV60[lJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXvRXNKSzVyPUCuNlEyQThizszN MYrTRW5ITVJ?
NCI-H69 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln5TWM2OD1yLkKxOFUyKM7:TR?= MXrTRW5ITVJ?
MOLT-13 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMkO5O|Uh|ryP NGmwUVRUSU6JRWK=
ML-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF31NG9KSzVyPUCuNlQ5ODJizszN NG\BS|hUSU6JRWK=
IGROV-1 M33wVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK0XJBKSzVyPUCuNlU6PTJizszN NF3yUIJUSU6JRWK=
TK10 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwMk[3N|gh|ryP NXPjcI02W0GQR1XS
EoL-1-cell NIm3UZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfrTWM2OD1yLkK2PFkzKM7:TR?= MYTTRW5ITVJ?
HO-1-N-1 MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDyTWM2OD1yLkK3PFU{KM7:TR?= MVzTRW5ITVJ?
BHY MkmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jibGlEPTB;MD6yPFY2PSEQvF2= NYqyRXJDW0GQR1XS
LU-139 MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrXTWM2OD1yLkOwOVEh|ryP MorEV2FPT0WU
23132-87 M3[5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTBwM{G5NlMh|ryP NUnVcIRmW0GQR1XS
ACHN M4L5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n4[WlEPTB;MD6zNVk6PCEQvF2= MXPTRW5ITVJ?
DoTc2-4510 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfrTWM2OD1yLkOyNlE6KM7:TR?= Ml6wV2FPT0WU
BB65-RCC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LZO2lEPTB;MD6zOFU6OyEQvF2= MnPCV2FPT0WU
HLE MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG2TWM2OD1yLkO1NFQ3KM7:TR?= NXfXR|A1W0GQR1XS
HCC1419 NHjjeXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTCTGxKSzVyPUCuN|Y1ODhizszN M4n3NnNCVkeHUh?=
A388 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwM{[4OVch|ryP MnqxV2FPT0WU
NUGC-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPLcpRpUUN3ME2wMlM5Ozd|IN88US=> MUDTRW5ITVJ?
KYSE-180 M1fDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvnNYpKSzVyPUCuN|kxQDlizszN NWGzdJVlW0GQR1XS
TE-6 NXPFbJF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLjXoZ{UUN3ME2wMlQxOjR4IN88US=> NGr6S|dUSU6JRWK=
A498 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwNEC2O|Qh|ryP M2jBWXNCVkeHUh?=
NCI-H1648 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn64TWM2OD1yLkS0NVgzKM7:TR?= MV;TRW5ITVJ?
DU-145 Ml25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorqTWM2OD1yLkS0PFM{KM7:TR?= M3LrbXNCVkeHUh?=
CW-2 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2flOWlEPTB;MD60OlkyPCEQvF2= NWLmfVQ6W0GQR1XS
A431 NGDnOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT5d|BEUUN3ME2wMlQ5OjN|IN88US=> NUC2Z|Q1W0GQR1XS
SAS M3i5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwNEizPVgh|ryP MnvEV2FPT0WU
NCI-H2126 M4TDWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPheZBXUUN3ME2wMlUyQTJ4IN88US=> MUTTRW5ITVJ?
NCI-H358 NUjsc5JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjuSG5KSzVyPUCuOVMzOSEQvF2= NUG1VJBJW0GQR1XS
FADU NEPWUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;XfXY5UUN3ME2wMlU1PDB2IN88US=> MVrTRW5ITVJ?
ACN M4jLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7rTWM2OD1yLkW1NFk1KM7:TR?= M{\uZ3NCVkeHUh?=
HCC70 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPKfmV6UUN3ME2wMlU4PjZzIN88US=> NGP1ZXFUSU6JRWK=
NCI-H1838 M1\QN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwNkCyPVkh|ryP NYnDfVYzW0GQR1XS
CAL-54 M3zZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwNkG2NlEh|ryP MkOyV2FPT0WU
NCI-H1975 MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwNkG3Nlgh|ryP MkPIV2FPT0WU
COR-L88 NGjMfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLlTWM2OD1yLk[0NVE{KM7:TR?= NW[zVoZkW0GQR1XS
CTV-1 NHHTfW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[xTWM2OD1yLk[0N|kzKM7:TR?= NGHzeo9USU6JRWK=
EW-18 M{G1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwNki2PVgh|ryP NXzCOlV6W0GQR1XS
HCC1806 NHXKeohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33qfWlEPTB;MD62PVY3PiEQvF2= MkXqV2FPT0WU
HuP-T4 NXfQ[WU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwNkm3OkDPxE1? MkPoV2FPT0WU
MDA-MB-361 MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z0SmlEPTB;MD63NlY3OiEQvF2= M1fXS3NCVkeHUh?=
NCI-H1573 M{i0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorwTWM2OD1yLkezOlMh|ryP NGTNT2JUSU6JRWK=
KU-19-19 NFnQ[5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqzco5KSzVyPUCuO|c1PjRizszN MkfmV2FPT0WU
COLO-678 NVj6XHE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTDTWM2OD1yLkiwPFM1KM7:TR?= MonDV2FPT0WU
C-33-A M2jaTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjJboJKSzVyPUCuPFEzQTdizszN NX\ZcpJNW0GQR1XS
Calu-3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID0bZRKSzVyPUCuPFE1OzRizszN MmLNV2FPT0WU
AGS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fM[WlEPTB;MD64N|Y1QCEQvF2= MUjTRW5ITVJ?
SCC-25 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPwVHpKSzVyPUCuPFQyPzFizszN MkK1V2FPT0WU
JVM-2 NFXj[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHCc3pRUUN3ME2wMlg5Ojl7IN88US=> M4r2W3NCVkeHUh?=
HCE-T MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rW[GlEPTB;MD64PFQzQCEQvF2= MXvTRW5ITVJ?
ES4 M{WwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7hXlBOUUN3ME2wMlk4QDN4IN88US=> M2nmSHNCVkeHUh?=
EKVX NYrkeHRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnhdplRUUN3ME2xMlAyODZ2IN88US=> NULnN2JJW0GQR1XS
D-542MG NYjU[|lKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof1TWM2OD1zLkCxNFY1KM7:TR?= MnrFV2FPT0WU
SW1116 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrYSoN[UUN3ME2xMlAyOjh5IN88US=> NEW0T4ZUSU6JRWK=
5637 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwMEG1NUDPxE1? NInJSG5USU6JRWK=
HT-1376 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFwMEG1NVMh|ryP NEjSdG5USU6JRWK=
NB69 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHVTWM2OD1zLkCyPVQ2KM7:TR?= NFPKfFVUSU6JRWK=
YKG-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTZTWM2OD1zLkC1OFE6KM7:TR?= NHLkOWpUSU6JRWK=
EW-3 NIfhT5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTFwMEe4PFMh|ryP NEnYT|RUSU6JRWK=
GCIY MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTFwMEixNFQh|ryP MkDqV2FPT0WU
SK-MES-1 NUfDe4Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTFwMUG0PFch|ryP MmfCV2FPT0WU
PANC-08-13 NWPCeZZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFwMU[0NVYh|ryP NFvuU2FUSU6JRWK=
SK-NEP-1 NVK0SnB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTFwMUe1NVMh|ryP Mn3sV2FPT0WU
SW954 NGXnWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PhemlEPTB;MT6yNFIyPCEQvF2= NELqUGZUSU6JRWK=
NCI-SNU-5 MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnKTWM2OD1zLkKzPUDPxE1? NHzOb3dUSU6JRWK=
SW48 M2XUT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknFTWM2OD1zLkK1OFMzKM7:TR?= Mlv2V2FPT0WU
HT-3 NHjsNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTFwMki3OVMh|ryP M3rFd3NCVkeHUh?=
ETK-1 M3HPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\lTWM2OD1zLkO3OFU3KM7:TR?= NXfuSVF2W0GQR1XS
SCC-15 M3u5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjWWFdKSzVyPUGuN|k1PTFizszN NUHNVlBCW0GQR1XS
DU-4475 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwNECxNlEh|ryP NFjifXRUSU6JRWK=
NB5 NFvleYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHsWWRKSzVyPUGuOFE{OTdizszN NGDQUZhUSU6JRWK=
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NCI-H810 NXjMNXZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoraTWM2OD1|ND63Nlc5KM7:TR?= NGSwTGFUSU6JRWK=
D-392MG M3XoTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTN3LkC1OlUh|ryP MlL1V2FPT0WU
LB771-HNC MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy2W|RKSzVyPUO1MlE3PThizszN M1fFZ3NCVkeHUh?=
COLO-679 NWPYcJFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqwTWM2OD1|NT6zPFgh|ryP MmLDV2FPT0WU
SK-PN-DW NFnv[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fWXGlEPTB;M{WuOFM3QSEQvF2= MWPTRW5ITVJ?
VA-ES-BJ MkK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrhTWM2OD1|NT60OlQ6KM7:TR?= M3HJNHNCVkeHUh?=
KNS-42 M2XaeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi5TWM2OD1|NT61PFI3KM7:TR?= NWHsTWFlW0GQR1XS
RVH-421 NHnL[IdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXrTWE1UUN3ME2zOU44PjR3IN88US=> M{C5T3NCVkeHUh?=
P30-OHK M1LOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zpSmlEPTB;M{WuPFc2OiEQvF2= NGm1eXFUSU6JRWK=
G-402 M361d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXnTWM2OD1|NT65PFY4KM7:TR?= MmXFV2FPT0WU
S-117 NIHhb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPa[|NKSzVyPUO2MlMxODhizszN MlHBV2FPT0WU
RXF393 NF;IRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTnbIdHUUN3ME2zOk4{Pzh3IN88US=> M1rwPHNCVkeHUh?=
LCLC-103H NG\oUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN4Lke4NFMh|ryP MVnTRW5ITVJ?
U-118-MG M1K0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;ne2lEPTB;M{[uPFg1PyEQvF2= M4HG[3NCVkeHUh?=
8-MG-BA NFPNV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfLTWM2OD1|Nj65OFg{KM7:TR?= MX7TRW5ITVJ?
MFH-ino MnjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7vRlJlUUN3ME2zO{4{OzdzIN88US=> M1f5UnNCVkeHUh?=
NCI-H23 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13GRmlEPTB;M{euOFE6PiEQvF2= M362fnNCVkeHUh?=
NCI-H446 MnLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPLTWM2OD1|Nz60PFYzKM7:TR?= MX;TRW5ITVJ?
LU-99A M2jKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1WxZ2lEPTB;M{euOVc{OSEQvF2= M2XNXnNCVkeHUh?=
KP-N-YN NVzUdVdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfPbGFKSzVyPUO3MlYyQTVizszN NVfhNYZzW0GQR1XS
SCC-9 NXntRYdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljDTWM2OD1|Nz63PFM5KM7:TR?= MYTTRW5ITVJ?
EFM-19 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHrZXdMUUN3ME2zO{44QTZ5IN88US=> MWjTRW5ITVJ?
A427 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTN5LkmxNFch|ryP NVrIepJ{W0GQR1XS
LB831-BLC NUO0ZotsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf3dpB{UUN3ME2zPE43ODN7IN88US=> NI\wdmpUSU6JRWK=
HOS M1XWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHMRYdKSzVyPUO5MlYzPzNizszN NEfqSHNUSU6JRWK=
LAN-6 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TDbGlEPTB;NECuNFEyOiEQvF2= M2Lsd3NCVkeHUh?=
U251 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPpTWM2OD12MD60NFU1KM7:TR?= MVrTRW5ITVJ?
SNU-387 MoDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC3dWJGUUN3ME20NE41PTV|IN88US=> MoHyV2FPT0WU
DMS-79 NXP1NoVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRyLkW4PFkh|ryP NX[ydWxZW0GQR1XS
SK-LU-1 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\JZ|VKSzVyPUSwMlY2PjhizszN Mn;3V2FPT0WU
HT NUf3dWV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\HW4xKSzVyPUSwMlY3OzlizszN NIjyV4tUSU6JRWK=
KP-N-YS MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYno[lJlUUN3ME20NE43PzZ6IN88US=> MWTTRW5ITVJ?
DMS-114 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTRyLkizO|Qh|ryP MULTRW5ITVJ?
HUTU-80 NGq4PXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXQWoRHUUN3ME20NU4xPTZ7IN88US=> NWPvRVU6W0GQR1XS
ONS-76 M4nkWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfwTWM2OD12MT60O|A6KM7:TR?= MUjTRW5ITVJ?
A673 NUnjOpJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTRzLkWxOVch|ryP NHe1elJUSU6JRWK=
HPAF-II NFHSc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3vdVI4UUN3ME20NU43PzB7IN88US=> M3;WcXNCVkeHUh?=
UACC-257 M3j5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj0RmpKSzVyPUSxMlc{PjlizszN M3XybXNCVkeHUh?=
EW-22 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nrfGlEPTB;NEGuPFY6PyEQvF2= MXnTRW5ITVJ?
NCI-H1755 NXH0WHFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPZWo1oUUN3ME20NU45PzJ3IN88US=> NHfHfXlUSU6JRWK=
KYSE-150 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPnTWM2OD12Mj6xO|gzKM7:TR?= M2LBO3NCVkeHUh?=
CGTH-W-1 NVnGc4RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXJfXIzUUN3ME20Nk41QTV3IN88US=> NVrITFhNW0GQR1XS
NB13 NV;5ZXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH6NodKSzVyPUSyMlYzOTdizszN M1\ObXNCVkeHUh?=
SW872 MnjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jHcGlEPTB;NEKuOlM{OSEQvF2= M1XPcHNCVkeHUh?=
KP-4 M2LmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfWcJpUUUN3ME20Nk45QDN{IN88US=> Mk\yV2FPT0WU
HCC38 NI\XSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK5eW57UUN3ME20Nk46PjF6IN88US=> MmXMV2FPT0WU
BB49-HNC NEjseW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnaeFhKSzVyPUSzMlI{PTZizszN MU\TRW5ITVJ?
CAL-62 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofITWM2OD12Mz60NFI5KM7:TR?= M3HVSXNCVkeHUh?=
NCI-H2029 MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3qwS2lEPTB;NEOuOVU5OSEQvF2= MWPTRW5ITVJ?
M14 M2roe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFu1dIJKSzVyPUS0MlE{OzJizszN MlnvV2FPT0WU
COLO-680N MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR2LkOzPUDPxE1? M2f2ZXNCVkeHUh?=
Hs-578-T MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHkWnBUUUN3ME20OU4xOjl2IN88US=> MXXTRW5ITVJ?
MSTO-211H MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR3Lkm0PFIh|ryP MojzV2FPT0WU
EW-1 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTR3Lkm2PFkh|ryP NULVcHdHW0GQR1XS
SW948 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLZTWM2OD12Nj60OFYzKM7:TR?= MUfTRW5ITVJ?
NCI-H460 NGfMOGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fLeGlEPTB;NE[uOVI{KM7:TR?= NV\lWpFrW0GQR1XS
CAS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS5TWM2OD12Nj63O|AyKM7:TR?= NH3KOIRUSU6JRWK=
TGBC11TKB M3:0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\oTWM2OD12Nz6xO|c4KM7:TR?= M1zZPXNCVkeHUh?=
HD-MY-Z M1zve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonxTWM2OD12OD63PFYh|ryP MnjhV2FPT0WU
NCI-H226 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W0[GlEPTB;NEmuO|c5PSEQvF2= MmfqV2FPT0WU
PA-1 M1rvc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TSeWlEPTB;NEmuPFM{PSEQvF2= MnXUV2FPT0WU
LB2518-MEL NXjTfmNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XET2lEPTB;NEmuPFczOyEQvF2= NVLLd3pDW0GQR1XS
A101D NELWWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj6XVNKSzVyPUS5Mlk1OjVizszN M2rGU3NCVkeHUh?=
NCI-H2087 NFnOb29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3DcHBKSzVyPUS5Mlk3QDJizszN MoTMV2FPT0WU

... 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. 850140-72-6
Storage powder
in solvent
Synonyms N/A
Smiles CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4

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 ()
% 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
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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
NCT04497584 Not yet recruiting Drug: Afatinib + Prednisone Advanced Squamous Non Small Cell Lung Cancer University of Texas Southwestern Medical Center September 1 2020 Phase 2
NCT04413201 Not yet recruiting Drug: Afatinib|Drug: Osimertinib Non-squamous NSCLC Michael Hopp|Boehringer Ingelheim|Johannes Gutenberg University Mainz June 30 2020 Phase 4
NCT04206787 Recruiting Drug: Afatinib Non-squamous Non-Small Cell Lung Cancer Boehringer Ingelheim May 20 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

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