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 112 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 MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rJNmlEPTB;MD6wNlU1PCEQvF2= NELWPZpUSU6JRWK=
HCC2218 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMEWzNlYh|ryP NFLpfldUSU6JRWK=
OCUB-M MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2izcmlEPTB;MD6wOVc1KM7:TR?= M1rUUXNCVkeHUh?=
ECC12 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTQTWM2OD1yLkC5NlMyKM7:TR?= MmjDV2FPT0WU
DSH1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwMEmzPVYh|ryP NVHKO3JzW0GQR1XS
BT-474 MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DQV2lEPTB;MD6yNVMyPSEQvF2= M1jlfXNCVkeHUh?=
BB30-HNC Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnUeXFsUUN3ME2wMlI1PjV2IN88US=> NYTxTpJCW0GQR1XS
EKVX MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq2bGxKSzVyPUCuOFQ5PzRizszN MY\TRW5ITVJ?
TE-12 Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ztSGlEPTB;MD60PVA2PyEQvF2= MkPJV2FPT0WU
A388 NHX0N2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLQTWM2OD1yLkeyNlU5KM7:TR?= NWO3SppXW0GQR1XS
TE-9 NYPQNnU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\4ZnFKSzVyPUCuO|Q1PTNizszN MkfrV2FPT0WU
LB2241-RCC NHj2fHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\BXmlEPTB;MT6xOVQxOyEQvF2= M4H2e3NCVkeHUh?=
LB996-RCC NVzBNVdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTkTWM2OD1zLkO2NlI5KM7:TR?= NVzJV2ljW0GQR1XS
LC-1F NFHoPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELDS2pKSzVyPUGuN|gzPDRizszN M1TiPXNCVkeHUh?=
TE-6 M1K3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFwNUWyNFEh|ryP NITkXYhUSU6JRWK=
A253 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfSNZJKSzVyPUGuPVc{OzVizszN M3zHSHNCVkeHUh?=
OS-RC-2 NEj5VmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrDVmhKSzVyPUGuPVkyQTlizszN MVjTRW5ITVJ?
TE-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwMES4N{DPxE1? NWHmfZUyW0GQR1XS
RL95-2 NYXJ[IVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGmydXhKSzVyPUOuNVU3PyEQvF2= NXPCS2pqW0GQR1XS
LS-513 NG\Hd4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\iTXNKSzVyPUOuOFAxPDFizszN MorDV2FPT0WU
DJM-1 M4XtPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITwN|VKSzVyPUOuOFY6PzVizszN NX7N[JBXW0GQR1XS
NMC-G1 NX3ES4Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHHU5pKSzVyPUOuOVQ2ODFizszN M4Lte3NCVkeHUh?=
TE-10 NHHpTZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr4TWM2OD1|LkW1N|U3KM7:TR?= NVTJeopCW0GQR1XS
TE-5 NFHjNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7mR5pKSzVyPUSuNFM4OyEQvF2= MnTOV2FPT0WU
TK10 Mly3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PMbmlEPTB;ND6xOlUzOiEQvF2= NY\FT2VYW0GQR1XS
UACC-812 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTRwNU[xOVMh|ryP NGPBe2pUSU6JRWK=
SW962 NX72eIN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXvTWM2OD13LkCyNVU6KM7:TR?= Mn7ZV2FPT0WU
SW954 NFPCdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTVwM{myOFUh|ryP M1zGVHNCVkeHUh?=
COLO-668 NYHKXpNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTVwN{K2Olch|ryP MoHYV2FPT0WU
LB1047-RCC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTVwOECwOFYh|ryP MYLTRW5ITVJ?
NB5 MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjNToNIUUN3ME22MlIyODBzIN88US=> NF7IdYlUSU6JRWK=
NTERA-S-cl-D1 NV3GeHRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ryWGlEPTB;Nj6yOlU3OSEQvF2= MXnTRW5ITVJ?
IST-MEL1 NF\XcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTZwNEO2PVQh|ryP Mn3qV2FPT0WU
GI-1 NEDDfnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXkVlZoUUN3ME22MlUyPjh{IN88US=> M{jyN3NCVkeHUh?=
TGBC1TKB M3\Uemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HUT2lEPTB;Nz6wO|E5OyEQvF2= M3HYO3NCVkeHUh?=
GT3TKB MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSx[4NKSzVyPUeuNlI4PDRizszN NVXDNIZGW0GQR1XS
EVSA-T MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHvU3hZUUN3ME23MlQzQDFzIN88US=> MYrTRW5ITVJ?
D-502MG NVOyUXRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXRXJBKSzVyPUeuOFg5QTRizszN MX\TRW5ITVJ?
TE-8 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTRTWM2OD15Lke2NVU6KM7:TR?= NVu5N2R5W0GQR1XS
OVCAR-4 NXX3N|JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[1dZZKSzVyPUmuNVE3PzVizszN Mmj3V2FPT0WU
D-336MG NV65fmFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7nVnRjUUN3ME25MlQ4Ozl3IN88US=> NED1R4pUSU6JRWK=
GCIY Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LqUmlEPTB;OT61O|QzKM7:TR?= NIrNbG5USU6JRWK=
KS-1 MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTlwNk[yPFch|ryP M{\uNXNCVkeHUh?=
HCC2998 NHvvcmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTlwOU[zNFch|ryP NHriTFRUSU6JRWK=
D-247MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfwdWNKSzVyPUmuPVgzQTFizszN NXm1d49YW0GQR1XS
TE-15 MmHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFyLkK0OUDPxE1? NUDzSW9{W0GQR1XS
IST-MES1 NFu0WlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1T4TmlEPTB;MUCuNlU3PSEQvF2= MWDTRW5ITVJ?
ETK-1 NE\OPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTFyLk[yN{DPxE1? NWS3b4s5W0GQR1XS
RCC10RGB NV[1eGtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLOTWM2OD1zMD65OlEh|ryP NX;JTG1qW0GQR1XS
KNS-42 NFHVfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDtN2pKSzVyPUGxMlczPTVizszN NXvnNHZbW0GQR1XS
LB771-HNC NYn0PZV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrz[WNKSzVyPUGyMlE4OTJizszN NEGwUXBUSU6JRWK=
SR MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe2TWM2OD1zMj6yNFY1KM7:TR?= Ml\NV2FPT0WU
NCI-H1355 M3rTdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HtVWlEPTB;MUKuPFk5PSEQvF2= MW\TRW5ITVJ?
ES6 NEXBNHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjZWnNqUUN3ME2xN{4xPzhizszN NVzjWFdkW0GQR1XS
SK-NEP-1 M2LHbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7CfGhKSzVyPUGzMlI2PzdizszN MWDTRW5ITVJ?
D-392MG NIPxSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7XTWM2OD1zMz62OFI5KM7:TR?= NFz1WI5USU6JRWK=
NB7 M1XTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PiSmlEPTB;MUSuNlM4PCEQvF2= M2XmS3NCVkeHUh?=
SK-LMS-1 Mn3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDyc2xxUUN3ME2xOE42OTR3IN88US=> NGXGRXJUSU6JRWK=
SK-UT-1 NUP4PYhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfuU4pKSzVyPUG0Mlc5QDlizszN NFTsWVBUSU6JRWK=
CA46 NXOyWYxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTBTWM2OD1zNT6wOVg3KM7:TR?= MWjTRW5ITVJ?
IST-SL2 NG\xfnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTF3LkG5NFEh|ryP MlSyV2FPT0WU
BC-1 NF\WU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn0fZVKSzVyPUG1MlM{OTRizszN NWnmeJY5W0GQR1XS
LS-123 M{\vfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF3LkixO|Mh|ryP MnnsV2FPT0WU
Ramos-2G6-4C10 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF4LkC5NlQh|ryP MXTTRW5ITVJ?
MZ1-PC NX3jeo5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[5WmlEPTB;MU[uO|MyOyEQvF2= MUXTRW5ITVJ?
LB647-SCLC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXrVXRKSzVyPUG2Mlk{PzJizszN M{jYRnNCVkeHUh?=
NCI-H1694 NWf1[Yw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHnTWM2OD1zNz6xOVI6KM7:TR?= NFH0emVUSU6JRWK=
NCI-H322M NVHwdm1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF5LkSzOlYh|ryP NV3CWoRXW0GQR1XS
ES7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF6LkO5NVQh|ryP MX7TRW5ITVJ?
LC-2-ad NVfHUnZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PnOGlEPTB;MUiuOFM5PiEQvF2= M2iwVnNCVkeHUh?=
SF268 M4jpW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjWeVdKSzVyPUG4Mlc1ODlizszN NXz0XYt[W0GQR1XS
RPMI-8402 Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF7LkC3OFIh|ryP NELqNIlUSU6JRWK=
HCE-T MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\qc|JUUUN3ME2yNE4zOzR2IN88US=> MYLTRW5ITVJ?
A101D MoHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJyLki1PFch|ryP M3rLbHNCVkeHUh?=
MRK-nu-1 NH6wbJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7TZ2xWUUN3ME2yNE46OTNizszN NHTPWJRUSU6JRWK=
LXF-289 NETCb|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[2TWM2OD1{MT6wN|gh|ryP MWXTRW5ITVJ?
NALM-6 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\oNGlEPTB;MkGuNVk3PyEQvF2= M37a[nNCVkeHUh?=
DOHH-2 NWrGUolvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PsdmlEPTB;MkGuOFgyOyEQvF2= M4T0[HNCVkeHUh?=
EW-16 NF;4SlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDrW2Y{UUN3ME2yNk4yPDB{IN88US=> NV3ucoZnW0GQR1XS
A4-Fuk MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXySGhKSzVyPUKyMlIyPDlizszN NGC0eJpUSU6JRWK=
HD-MY-Z Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJ{LkO5OlUh|ryP NX3nXmh2W0GQR1XS
SKM-1 M{fLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Hwc2lEPTB;MkKuO|M2OSEQvF2= MVzTRW5ITVJ?
DMS-153 M3fqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2OwdGlEPTB;MkOuOFIxPCEQvF2= NVvzU|d1W0GQR1XS
LB373-MEL-D M1K3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLUZplKSzVyPUKzMlU1PTJizszN M1TlS3NCVkeHUh?=
LP-1 NETaR3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ|LkiwPVch|ryP NGT3fnlUSU6JRWK=
GI-ME-N M{LpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITIbYdKSzVyPUK0MlI6OiEQvF2= NVvLSVJvW0GQR1XS
MPP-89 NHHndJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJ3LkKwN|Yh|ryP NHPYeVBUSU6JRWK=
U-698-M NX3Q[oFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDdolTUUN3ME2yOU4zPTB|IN88US=> NX;qTVJUW0GQR1XS
HC-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzoTWM2OD1{NT62OFE5KM7:TR?= MorFV2FPT0WU
HCC2157 M{jYNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ3Lk[3N{DPxE1? M4rne3NCVkeHUh?=
MOLT-4 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\LNVNKSzVyPUK2MlI4OyEQvF2= NYP5[WF1W0GQR1XS
LS-411N NFf3OotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nyT2lEPTB;Mk[uN|M3QSEQvF2= MnfTV2FPT0WU
Becker MoDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknpTWM2OD1{Nj61NVgyKM7:TR?= MYnTRW5ITVJ?
NCI-H23 M3n0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ4Lke1O|Uh|ryP NIn2VXlUSU6JRWK=
IST-SL1 MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ncJRKSzVyPUK3MlM5PjdizszN NGWyUo5USU6JRWK=
MZ2-MEL Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon6TWM2OD1{Nz60OVY3KM7:TR?= NV3iVYJiW0GQR1XS
RKO NGfROIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ6LkG0OFYh|ryP MX;TRW5ITVJ?
TE-441-T NUnaZpB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzFN25KSzVyPUK4Mlc5QSEQvF2= MWXTRW5ITVJ?
EW-24 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHmTWM2OD1{OT6xNlU6KM7:TR?= MmX5V2FPT0WU
no-10 MljiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnTPJVKSzVyPUK5MlE3OzFizszN NGXtTZJUSU6JRWK=
D-542MG NE\VNXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;6TGlEPTB;MkmuPVIzOSEQvF2= M4Xj[HNCVkeHUh?=
ST486 NU\CZlNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTNyLk[0OVEh|ryP NXP3dYo2W0GQR1XS
KURAMOCHI NGLNfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfjTWM2OD1|MD64NFU4KM7:TR?= M1zQdXNCVkeHUh?=
ES8 NHPL[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELjNZZKSzVyPUOxMlU6PzJizszN NHPFfJNUSU6JRWK=
BL-41 NXW4[HJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN{LkGwOVQh|ryP Mm\jV2FPT0WU
NB6 NIe4bo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTo[5lKUUN3ME2zNk4{QDV3IN88US=> M3;ZOnNCVkeHUh?=
NCI-H1304 NGG1NZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;tfYpMUUN3ME2zNk41QTZ5IN88US=> M4LuXnNCVkeHUh?=
MS-1 M2G0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn1NJpKSzVyPUOyMlc4PTFizszN MU\TRW5ITVJ?
MFH-ino NFO3NGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TifmlEPTB;M{SuN|IzPCEQvF2= MUXTRW5ITVJ?
NOS-1 NFnJVYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPZTWM2OD1|ND62O|Q5KM7:TR?= NF7xTZpUSU6JRWK=
HUTU-80 NF7FU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTN3LkO2Olch|ryP NGnyeGpUSU6JRWK=
EB2 NGLIR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\ON2lEPTB;M{[uOlE5QSEQvF2= MWPTRW5ITVJ?
L-540 NI\3fmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;reo5KSzVyPUO3MlI{ODhizszN M2jjXHNCVkeHUh?=
NCI-H747 NXfP[5BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN6Lki4OFYh|ryP NFfucYFUSU6JRWK=
NCI-H446 NEXDWFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTN7Lkm2OVEh|ryP Mlm3V2FPT0WU
MOLT-16 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\yTWM2OD12Mj60NVUh|ryP MoHuV2FPT0WU
BC-3 M1frNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3aUJYxUUN3ME20OU41QDl4IN88US=> Mk\HV2FPT0WU
SJSA-1 MlLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTR3LkW0O|Qh|ryP M4XqbXNCVkeHUh?=
BB65-RCC NVT4[ppvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR3Lk[2OkDPxE1? NEfO[|NUSU6JRWK=
SNB75 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz5TWM2OD12Nj6wNVgh|ryP Mn7MV2FPT0WU

... 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]
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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]
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  • 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]
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  • 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 (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 )

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    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):
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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
NCT03075995 Unknown status Other: hight-fat breakfast Breast Cancer Sun Yat-sen University April 12 2017 Not Applicable
NCT02338245 Completed Drug: ASLAN001|Drug: Lapatinib|Drug: Capecitabine Metastatic Breast Cancer Aslan Pharmaceuticals December 29 2014 Phase 2
NCT02294786 Terminated Drug: Lapatinib|Drug: Capecitabine|Drug: Octreotide Cancer Novartis Pharmaceuticals|Novartis December 17 2014 Phase 2
NCT02213042 Active not recruiting Drug: Lapatinib|Biological: Trastuzumab Neoplasms Breast Novartis Pharmaceuticals|Novartis October 24 2014 Phase 2
NCT01782651 Completed Drug: Lapatinib plus capecitabine Neoplasms Breast GlaxoSmithKline August 2014 --
NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie July 2014 Not Applicable

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