Lapatinib

Catalog No.S2111 Synonyms: GW-572016, GSK572016

Lapatinib Chemical Structure

Molecular Weight(MW): 581.06

Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

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Cited by 54 Publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Targets
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM
In vitro

Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1648 NILrZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fIemlEPTB;MD6wNlU1PCEQvF2= MYjTRW5ITVJ?
HCC2218 NXe0NmdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPqTlBvUUN3ME2wMlA2OzJ4IN88US=> NF7NS2xUSU6JRWK=
OCUB-M MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H6PGlEPTB;MD6wOVc1KM7:TR?= Ml;OV2FPT0WU
ECC12 M2rJNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfnTWM2OD1yLkC5NlMyKM7:TR?= NE[2XpVUSU6JRWK=
DSH1 M1vNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwMEmzPVYh|ryP NEPoNZJUSU6JRWK=
BT-474 M2HyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPlXIJKSzVyPUCuNlE{OTVizszN NFLIUZhUSU6JRWK=
BB30-HNC M2DpVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMkS2OVQh|ryP MVLTRW5ITVJ?
EKVX NE\XV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zvVWlEPTB;MD60OFg4PCEQvF2= MkTWV2FPT0WU
TE-12 NH:yN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f3SGlEPTB;MD60PVA2PyEQvF2= NYL6PWtbW0GQR1XS
A388 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C1RWlEPTB;MD63NlI2QCEQvF2= NXrRSIJQW0GQR1XS
TE-9 M2fRe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWNJVKSzVyPUCuO|Q1PTNizszN NFniT4tUSU6JRWK=
LB2241-RCC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXJU4xSUUN3ME2xMlE2PDB|IN88US=> NHTCXlNUSU6JRWK=
LB996-RCC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;TTWM2OD1zLkO2NlI5KM7:TR?= MX3TRW5ITVJ?
LC-1F NVHzTI9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nuOGlEPTB;MT6zPFI1PCEQvF2= MkLCV2FPT0WU
TE-6 Mk\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jBZ2lEPTB;MT61OVIxOSEQvF2= M2\tN3NCVkeHUh?=
A253 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTFwOUezN|Uh|ryP MnHlV2FPT0WU
OS-RC-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXXb4tKSzVyPUGuPVkyQTlizszN Moi1V2FPT0WU
TE-1 NGHjSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJwMES4N{DPxE1? MWjTRW5ITVJ?
RL95-2 Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTNwMUW2O{DPxE1? NETFR2FUSU6JRWK=
LS-513 NYPBUZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYH6OlIxUUN3ME2zMlQxODRzIN88US=> MWjTRW5ITVJ?
DJM-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7PTWM2OD1|LkS2PVc2KM7:TR?= NEfxbGxUSU6JRWK=
NMC-G1 M2q1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\P[JpjUUN3ME2zMlU1PTBzIN88US=> MoH4V2FPT0WU
TE-10 NXvkV4tOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3DfJZlUUN3ME2zMlU2OzV4IN88US=> MljjV2FPT0WU
TE-5 NHLldYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPJTWM2OD12LkCzO|Mh|ryP MVTTRW5ITVJ?
TK10 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HzZWlEPTB;ND6xOlUzOiEQvF2= M1vhcXNCVkeHUh?=
UACC-812 M4nWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTRwNU[xOVMh|ryP NXHBW2lKW0GQR1XS
SW962 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13EfWlEPTB;NT6wNlE2QSEQvF2= NVjXPGtGW0GQR1XS
SW954 MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTVwM{myOFUh|ryP MlO1V2FPT0WU
COLO-668 MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3lVGZ6UUN3ME21MlczPjZ5IN88US=> M{S3enNCVkeHUh?=
LB1047-RCC NHe3ZoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLZbIVKSzVyPUWuPFAxPDZizszN NVnOZ3ZrW0GQR1XS
NB5 NHrTbmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TKTmlEPTB;Nj6yNVAxOSEQvF2= MX3TRW5ITVJ?
NTERA-S-cl-D1 NFzhUWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTZwMk[1OlEh|ryP NGHsSYhUSU6JRWK=
IST-MEL1 NILJclFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWzTWM2OD14LkSzOlk1KM7:TR?= NGDTWGFUSU6JRWK=
GI-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDQTWM2OD14LkWxOlgzKM7:TR?= NGe0e4RUSU6JRWK=
TGBC1TKB NWHhU|VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTSTWM2OD15LkC3NVg{KM7:TR?= M4rDbHNCVkeHUh?=
GT3TKB Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3FTWM2OD15LkKyO|Q1KM7:TR?= NXn3VYt{W0GQR1XS
EVSA-T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnEOpNKSzVyPUeuOFI5OTFizszN NFTSVJVUSU6JRWK=
D-502MG NEHxblBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDiV3lCUUN3ME23MlQ5QDl2IN88US=> MonVV2FPT0WU
TE-8 Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\iOnVKSzVyPUeuO|YyPTlizszN MWPTRW5ITVJ?
OVCAR-4 NUX2SGk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O5emlEPTB;OT6xNVY4PSEQvF2= NG[2clZUSU6JRWK=
D-336MG MnXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf6RnJKSzVyPUmuOFc{QTVizszN NY[wWm9jW0GQR1XS
GCIY M1LQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTlwNUe0NkDPxE1? NGnYbZpUSU6JRWK=
KS-1 MljVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPvTWM2OD17Lk[2Nlg4KM7:TR?= MXTTRW5ITVJ?
HCC2998 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\JTWM2OD17Lkm2N|A4KM7:TR?= NEjNTVhUSU6JRWK=
D-247MG M4PWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTlwOUiyPVEh|ryP M1r2TXNCVkeHUh?=
TE-15 NF30PFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[0SZM3UUN3ME2xNE4zPDVizszN MVXTRW5ITVJ?
IST-MES1 M{W5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17N[GlEPTB;MUCuNlU3PSEQvF2= NIPTdmtUSU6JRWK=
ETK-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnORXBbUUN3ME2xNE43OjNizszN MVHTRW5ITVJ?
RCC10RGB NX7iWFVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3EPJBKSzVyPUGwMlk3OSEQvF2= MULTRW5ITVJ?
KNS-42 NV7tV2lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjQeYNFUUN3ME2xNU44OjV3IN88US=> NETMNW5USU6JRWK=
LB771-HNC M3nYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zJUGlEPTB;MUKuNVcyOiEQvF2= NGPxd4RUSU6JRWK=
SR M2DRbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTF{LkKwOlQh|ryP NEPkW|FUSU6JRWK=
NCI-H1355 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPycHNvUUN3ME2xNk45QTh3IN88US=> NGDJc3hUSU6JRWK=
ES6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF|LkC3PEDPxE1? Mlr2V2FPT0WU
SK-NEP-1 MkLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjW[IlKSzVyPUGzMlI2PzdizszN M{nSPXNCVkeHUh?=
D-392MG Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF|Lk[0Nlgh|ryP NYXCR2V3W0GQR1XS
NB7 M4KxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF2LkKzO|Qh|ryP M33UWHNCVkeHUh?=
SK-LMS-1 M2XlPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYX1[WFpUUN3ME2xOE42OTR3IN88US=> M1T2VnNCVkeHUh?=
SK-UT-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi4N|dKSzVyPUG0Mlc5QDlizszN M2T1Z3NCVkeHUh?=
CA46 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTxTWM2OD1zNT6wOVg3KM7:TR?= NGLFVWNUSU6JRWK=
IST-SL2 M2naPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF3LkG5NFEh|ryP NX60SXVnW0GQR1XS
BC-1 M2DSTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\zb2lEPTB;MUWuN|MyPCEQvF2= M2HPdnNCVkeHUh?=
LS-123 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vhN2lEPTB;MUWuPFE4OyEQvF2= M3\3XHNCVkeHUh?=
Ramos-2G6-4C10 MkLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTDWXJKSzVyPUG2MlA6OjRizszN MUPTRW5ITVJ?
MZ1-PC NUTkXXdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfjW|VKSzVyPUG2Mlc{OTNizszN MYnTRW5ITVJ?
LB647-SCLC MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnKbGNKSzVyPUG2Mlk{PzJizszN MkXNV2FPT0WU
NCI-H1694 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\2cWlEPTB;MUeuNVUzQSEQvF2= NWP2TVh{W0GQR1XS
NCI-H322M NITXd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPZWHpYUUN3ME2xO{41OzZ4IN88US=> M2rBVXNCVkeHUh?=
ES7 NEPIPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF6LkO5NVQh|ryP MmOyV2FPT0WU
LC-2-ad MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[0fWZsUUN3ME2xPE41Ozh4IN88US=> NFXLSFdUSU6JRWK=
SF268 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvsTWM2OD1zOD63OFA6KM7:TR?= MoKxV2FPT0WU
RPMI-8402 M4H2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF35WIZKSzVyPUG5MlA4PDJizszN M1TMN3NCVkeHUh?=
HCE-T MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJyLkKzOFQh|ryP NVK0XopJW0GQR1XS
A101D M1LJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJyLki1PFch|ryP NYLWemZ1W0GQR1XS
MRK-nu-1 M{j5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTJyLkmxN{DPxE1? NFXEbJRUSU6JRWK=
LXF-289 M1jNbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXni[npnUUN3ME2yNU4xOzhizszN MlHmV2FPT0WU
NALM-6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:wWmlEPTB;MkGuNVk3PyEQvF2= NVXz[2Y{W0GQR1XS
DOHH-2 M1;JcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDYR5NKSzVyPUKxMlQ5OTNizszN NVfHW5k2W0GQR1XS
EW-16 NYXk[mJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnObFNKSzVyPUKyMlE1ODJizszN MmjXV2FPT0WU
A4-Fuk NFPqZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\5WnZKSzVyPUKyMlIyPDlizszN MlewV2FPT0WU
HD-MY-Z Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPjXplxUUN3ME2yNk4{QTZ3IN88US=> MmiwV2FPT0WU
SKM-1 MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzq[4RtUUN3ME2yNk44OzVzIN88US=> M2DVbHNCVkeHUh?=
DMS-153 NHrxenBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LVc2lEPTB;MkOuOFIxPCEQvF2= NHjLPIdUSU6JRWK=
LB373-MEL-D NHHyUWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ|LkW0OVIh|ryP MVjTRW5ITVJ?
LP-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zhUmlEPTB;MkOuPFA6PyEQvF2= M2DsdHNCVkeHUh?=
GI-ME-N Mn\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO1foVqUUN3ME2yOE4zQTJizszN NFTCV|hUSU6JRWK=
MPP-89 NFK5eo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13WO2lEPTB;MkWuNlA{PiEQvF2= MYDTRW5ITVJ?
U-698-M MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\OdmlEPTB;MkWuNlUxOyEQvF2= MYTTRW5ITVJ?
HC-1 MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3jSHhKSzVyPUK1MlY1OThizszN Mn7NV2FPT0WU
HCC2157 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj3TWM2OD1{NT62O|Mh|ryP M3vQcHNCVkeHUh?=
MOLT-4 M13kUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWyT|VKSzVyPUK2MlI4OyEQvF2= MW\TRW5ITVJ?
LS-411N MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f1NWlEPTB;Mk[uN|M3QSEQvF2= M{LT[3NCVkeHUh?=
Becker MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLXNFdQUUN3ME2yOk42OThzIN88US=> NUHOcngzW0GQR1XS
NCI-H23 MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjXbIpOUUN3ME2yOk44PTd3IN88US=> NFLmc5dUSU6JRWK=
IST-SL1 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ5LkO4Olch|ryP MnTsV2FPT0WU
MZ2-MEL M{H6cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXizeWh{UUN3ME2yO{41PTZ4IN88US=> M4rYXnNCVkeHUh?=
RKO NEjUNFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFO2NXJKSzVyPUK4MlE1PDZizszN MlfMV2FPT0WU
TE-441-T NIfqZoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj5UY15UUN3ME2yPE44QDlizszN NGK4fVFUSU6JRWK=
EW-24 NVXGU5VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP6VWdKSzVyPUK5MlEzPTlizszN MUDTRW5ITVJ?
no-10 M2C4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLPTWM2OD1{OT6xOlMyKM7:TR?= MWPTRW5ITVJ?
D-542MG M3XWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDsRWZKSzVyPUK5MlkzOjFizszN MYHTRW5ITVJ?
ST486 NXLNZoRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTNyLk[0OVEh|ryP M3fuNnNCVkeHUh?=
KURAMOCHI M3LKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33mU2lEPTB;M{CuPFA2PyEQvF2= MonuV2FPT0WU
ES8 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HNNmlEPTB;M{GuOVk4OiEQvF2= MX;TRW5ITVJ?
BL-41 M2n5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLjeZR{UUN3ME2zNk4yODV2IN88US=> M1vrO3NCVkeHUh?=
NB6 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXoT2dHUUN3ME2zNk4{QDV3IN88US=> MXfTRW5ITVJ?
NCI-H1304 NHHTc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LpPWlEPTB;M{KuOFk3PyEQvF2= NXTOfIpiW0GQR1XS
MS-1 NFj5TYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TpS2lEPTB;M{KuO|c2OSEQvF2= MWPTRW5ITVJ?
MFH-ino MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe4NXozUUN3ME2zOE4{OjJ2IN88US=> NG\uUHVUSU6JRWK=
NOS-1 MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjXTWM2OD1|ND62O|Q5KM7:TR?= Ml[wV2FPT0WU
HUTU-80 NHrGb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\i[2lEPTB;M{WuN|Y3PyEQvF2= NG[zOodUSU6JRWK=
EB2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK3TWM2OD1|Nj62NVg6KM7:TR?= NY\zSWR4W0GQR1XS
L-540 NVThZXVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTN5LkKzNFgh|ryP NWTncoZSW0GQR1XS
NCI-H747 NF\iPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXNTWM2OD1|OD64PFQ3KM7:TR?= MljhV2FPT0WU
NCI-H446 MnvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTN7Lkm2OVEh|ryP MYLTRW5ITVJ?
MOLT-16 NV21NG84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vhUWlEPTB;NEKuOFE2KM7:TR?= NIH6W5BUSU6JRWK=
BC-3 NFnscIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Hte2lEPTB;NEWuOFg6PiEQvF2= NXjkPVV1W0GQR1XS
SJSA-1 M2n6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWWy[JNXUUN3ME20OU42PDd2IN88US=> M{fITnNCVkeHUh?=
BB65-RCC NFXLNFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHFepBKSzVyPUS1MlY3PiEQvF2= NHn5[plUSU6JRWK=
SNB75 M1L3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLIeZV2UUN3ME20Ok4xOThizszN MnXTV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; 

PubMed: 29799521     


Downregulation of HSF1, mutp53, and Mdm2 in lapatinib-sensitive parental BT474, but not in lapatinib-resistant BT474R cells, treated with indicated lapatinib concentrations for 24 h.

pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP ; 

PubMed: 28938602     


SKBR3 and 78617 cells were treated with lapatinib as in panel A, then the expression of phospho-ErbB2 (Tyr1221/1222), ErbB2, phospho-EGFR (Tyr1068), EGFR, phospho-Akt (Ser473), Akt, phospho-Erk1/2 (Thr202/Tyr204), Erk2, phospho-mTOR (Ser2448), and mTOR were analyzed using Western blotting. 

p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1; 

PubMed: 22853430     


A panel of HER2-amplified breast cancer cells were treated with 200nM lapatinib for up to 72 hours to detect the initial downregulation and subsequent upregulation of HER2-HER3 and downstream signaling. Immunoblots were performed using the indicated antibodies.

29799521 28938602 22853430
Immunofluorescence
LC3 ; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 6 days and UACC893 GFP-LC3 cells were cultured for 7 days with 5 μM EZN3046 or EZN4150 .

Vimentin / E-cadherin; 

PubMed: 28243326     


Cells treated with lapatinib (5µM) increased the expression of E-cadherin and inhibited the expression of Vimentin by immunofluorescence. (Magnification: 1000×).

26637440 28243326
Growth inhibition assay
Cell viability (OE19); 

PubMed: 25350844     


Dose-response curves from escalated dose of lapatinib in the presence of 1 µM concentration of saracatinib. The calculated values of IC50 for lapatinib were following; 207.3 nM and 145 nM, respectively, after lapatinib alone and in the presence of saracatinib for parental OE19; >1,000 nM after lapatinib alone for LR2A and LR2B; 91.66 nM and 224.0 nM in the presence of saracatinib in LR2A and LR2B, respectively. Values were presented as relative cellular viability relative to vehicle-treated controls with the mean ± S.E. of quadruplicate from a representative experiment. The p values calculated by two-way ANOVA were <0.0001 comparing lapatinib alone with lapatinib plus saracatinib both in the LR2A and LR2B.

Cell viability (A431 cells); 

PubMed: 28243326     


The MTT assay was performed on the viability of A431 cells by lapatinib at different concentrations (0.1-50μM) and IC50 value was analyzed as indicated on the plot (t-test).

25350844 28243326
In vivo Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. [1]

Protocol

Kinase Assay:[1]
+ Expand

In vitro kinase assays:

The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.
Cell Research:[1]
+ Expand
  • Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 72 hours
  • Method: Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
  • Formulation: Formulated in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
  • Dosages: ~100 mg/kg
  • Administration: Orally twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.09 mM)
Water Insoluble
Ethanol 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 581.06
Formula

C29H26ClFN4O4S

CAS No. 231277-92-2
Storage powder
in solvent
Synonyms GW-572016, GSK572016

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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    C2
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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

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 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:

    If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

  • Answer:

    For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID