Lapatinib

For research use only.

Catalog No.S2111 Synonyms: GW-572016, GSK572016

334 publications

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. Lapatinib induces ferroptosis and autophagic cell death.

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Selleck's Lapatinib has been cited by 334 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. Lapatinib induces ferroptosis and autophagic cell death.
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 NXXRSXBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XXfWlEPTB;MD6wNlU1PCEQvF2= MlvWV2FPT0WU
HCC2218 MkXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEWzNlYh|ryP M2DhWXNCVkeHUh?=
OCUB-M NXLxOHZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTBwMEW3OEDPxE1? MWXTRW5ITVJ?
ECC12 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPKN29KSzVyPUCuNFkzOzFizszN NVG3RllHW0GQR1XS
DSH1 NY\2SoZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMEmzPVYh|ryP NV;3WZJKW0GQR1XS
BT-474 NEnjfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvVTWM2OD1yLkKxN|E2KM7:TR?= MWTTRW5ITVJ?
BB30-HNC NH;heHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMkS2OVQh|ryP NEGwW5dUSU6JRWK=
EKVX NUeyc3pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvvdVR4UUN3ME2wMlQ1QDd2IN88US=> NFPnVplUSU6JRWK=
TE-12 NFzXTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwNEmwOVch|ryP M4PWOHNCVkeHUh?=
A388 M{fhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwN{KyOVgh|ryP NHnTbIVUSU6JRWK=
TE-9 NEXZdWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwN{S0OVMh|ryP MnrDV2FPT0WU
LB2241-RCC MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LEbWlEPTB;MT6xOVQxOyEQvF2= NF:2fmJUSU6JRWK=
LB996-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LQO2lEPTB;MT6zOlIzQCEQvF2= M3HSNnNCVkeHUh?=
LC-1F NE\WSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwM{iyOFQh|ryP NYjGZlBjW0GQR1XS
TE-6 NX65fVBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3pbIxwUUN3ME2xMlU2OjBzIN88US=> NGXaUHJUSU6JRWK=
A253 NV3YN4E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHraZXNKSzVyPUGuPVc{OzVizszN MVfTRW5ITVJ?
OS-RC-2 NX\ib3lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlruTWM2OD1zLkm5NVk6KM7:TR?= MWfTRW5ITVJ?
TE-1 NHvK[XNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJwMES4N{DPxE1? MV;TRW5ITVJ?
RL95-2 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f3ZWlEPTB;Mz6xOVY4KM7:TR?= M1j5RXNCVkeHUh?=
LS-513 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq5NnpKSzVyPUOuOFAxPDFizszN NYPmXod1W0GQR1XS
DJM-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn5W45KSzVyPUOuOFY6PzVizszN NVnudY5IW0GQR1XS
NMC-G1 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\ZR2lEPTB;Mz61OFUxOSEQvF2= MoXlV2FPT0WU
TE-10 M4Lm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTNwNUWzOVYh|ryP M3KxcHNCVkeHUh?=
TE-5 NFXTXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTF[2JQUUN3ME20MlA{PzNizszN MVzTRW5ITVJ?
TK10 MmXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTRwMU[1NlIh|ryP NIPIcW1USU6JRWK=
UACC-812 NF7ycFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjaVphlUUN3ME20MlU3OTV|IN88US=> MlHvV2FPT0WU
SW962 NXHETWt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1njfWlEPTB;NT6wNlE2QSEQvF2= NXLxZVhKW0GQR1XS
SW954 NFzoPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTVwM{myOFUh|ryP MYnTRW5ITVJ?
COLO-668 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTVwN{K2Olch|ryP Mof2V2FPT0WU
LB1047-RCC Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvsTWM2OD13LkiwNFQ3KM7:TR?= NXLtOJd3W0GQR1XS
NB5 NIe3RpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfUT4IyUUN3ME22MlIyODBzIN88US=> M1z5UnNCVkeHUh?=
NTERA-S-cl-D1 Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D3U2lEPTB;Nj6yOlU3OSEQvF2= M{XifHNCVkeHUh?=
IST-MEL1 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ReGNjUUN3ME22MlQ{Pjl2IN88US=> MoDsV2FPT0WU
GI-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\Oc2lEPTB;Nj61NVY5OiEQvF2= Mn\sV2FPT0WU
TGBC1TKB NVXQVXpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LUfmlEPTB;Nz6wO|E5OyEQvF2= M3i5NnNCVkeHUh?=
GT3TKB MmW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTdwMkK3OFQh|ryP NXvmU4hWW0GQR1XS
EVSA-T NYfVUWV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33HRmlEPTB;Nz60NlgyOSEQvF2= M2H6OHNCVkeHUh?=
D-502MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1m2RWlEPTB;Nz60PFg6PCEQvF2= NWrQUVFIW0GQR1XS
TE-8 NWHTVXkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3flbmlEPTB;Nz63OlE2QSEQvF2= MXTTRW5ITVJ?
OVCAR-4 NVLjW4JmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ezRWlEPTB;OT6xNVY4PSEQvF2= NInJd|FUSU6JRWK=
D-336MG NWH2VGlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXETWM2OD17LkS3N|k2KM7:TR?= Mkf1V2FPT0WU
GCIY M{S4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC4WJY6UUN3ME25MlU4PDJizszN NYDMNVdKW0GQR1XS
KS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvNb2JKSzVyPUmuOlYzQDdizszN NHXQW29USU6JRWK=
HCC2998 NUjLUWFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTlwOU[zNFch|ryP NVvm[2s6W0GQR1XS
D-247MG M4rRUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPDTWM2OD17Lkm4NlkyKM7:TR?= NXPpeWpiW0GQR1XS
TE-15 NVrzRYxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFyLkK0OUDPxE1? NVvYRoFrW0GQR1XS
IST-MES1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PscGlEPTB;MUCuNlU3PSEQvF2= M{jnfXNCVkeHUh?=
ETK-1 NGPkUFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfETWM2OD1zMD62NlMh|ryP Mnr3V2FPT0WU
RCC10RGB M4HYXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nB[mlEPTB;MUCuPVYyKM7:TR?= Ml7QV2FPT0WU
KNS-42 NHzhSpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFzLkeyOVUh|ryP MYrTRW5ITVJ?
LB771-HNC M3PLR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjTdolKSzVyPUGyMlE4OTJizszN NV;MNHVYW0GQR1XS
SR MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPKTWM2OD1zMj6yNFY1KM7:TR?= MWLTRW5ITVJ?
NCI-H1355 NVPIVYtHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjPRXdKSzVyPUGyMlg6QDVizszN MmfsV2FPT0WU
ES6 M2DiVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\RTWM2OD1zMz6wO|gh|ryP MYHTRW5ITVJ?
SK-NEP-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfPUoZKSzVyPUGzMlI2PzdizszN MX\TRW5ITVJ?
D-392MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\4eVY6UUN3ME2xN{43PDJ6IN88US=> MnnZV2FPT0WU
NB7 M1PGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTF2LkKzO|Qh|ryP MojzV2FPT0WU
SK-LMS-1 MkTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjpSFcyUUN3ME2xOE42OTR3IN88US=> MkDiV2FPT0WU
SK-UT-1 NGCzOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrSeG9XUUN3ME2xOE44QDh7IN88US=> MUTTRW5ITVJ?
CA46 NYfQcGc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF3LkC1PFYh|ryP MVfTRW5ITVJ?
IST-SL2 MkH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLJTWM2OD1zNT6xPVAyKM7:TR?= NEHsWIVUSU6JRWK=
BC-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET3bGtKSzVyPUG1MlM{OTRizszN MYXTRW5ITVJ?
LS-123 NVLw[YFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF3LkixO|Mh|ryP NGjW[GFUSU6JRWK=
Ramos-2G6-4C10 M3zsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjDVIZKSzVyPUG2MlA6OjRizszN MUfTRW5ITVJ?
MZ1-PC NV\4UVg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WzWmlEPTB;MU[uO|MyOyEQvF2= M3fj[XNCVkeHUh?=
LB647-SCLC M1LXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnOzTWM2OD1zNj65N|czKM7:TR?= Mn7ZV2FPT0WU
NCI-H1694 Mk\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ETWM2OD1zNz6xOVI6KM7:TR?= Ml\sV2FPT0WU
NCI-H322M MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PxVWlEPTB;MUeuOFM3PiEQvF2= NWfrbmpiW0GQR1XS
ES7 NGTRNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\RdFNzUUN3ME2xPE4{QTF2IN88US=> NEDJZY1USU6JRWK=
LC-2-ad MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTkUGVKSzVyPUG4MlQ{QDZizszN MU\TRW5ITVJ?
SF268 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTVbpJDUUN3ME2xPE44PDB7IN88US=> NIPm[|VUSU6JRWK=
RPMI-8402 NWra[|hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF7LkC3OFIh|ryP MoLEV2FPT0WU
HCE-T MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:5TWM2OD1{MD6yN|Q1KM7:TR?= MVjTRW5ITVJ?
A101D NUDtVoZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLnNodtUUN3ME2yNE45PTh5IN88US=> M1fhe3NCVkeHUh?=
MRK-nu-1 NU\kdHd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJyLkmxN{DPxE1? NFH3b5RUSU6JRWK=
LXF-289 NITBVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DSfGlEPTB;MkGuNFM5KM7:TR?= MUXTRW5ITVJ?
NALM-6 NVXC[2tUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLtfnZLUUN3ME2yNU4yQTZ5IN88US=> NH3seG5USU6JRWK=
DOHH-2 MkPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Pa[WlEPTB;MkGuOFgyOyEQvF2= MVzTRW5ITVJ?
EW-16 NUfSelZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ{LkG0NFIh|ryP M3fzeXNCVkeHUh?=
A4-Fuk M2Tz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nGU2lEPTB;MkKuNlE1QSEQvF2= M{TaVnNCVkeHUh?=
HD-MY-Z MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXMdpdKSzVyPUKyMlM6PjVizszN NV7QSGx5W0GQR1XS
SKM-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fKXGlEPTB;MkKuO|M2OSEQvF2= NXPuRnlrW0GQR1XS
DMS-153 M3\vfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3ZU4VxUUN3ME2yN{41OjB2IN88US=> NETvcJdUSU6JRWK=
LB373-MEL-D NI\4S4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHqxRXNKSzVyPUKzMlU1PTJizszN M1fKfXNCVkeHUh?=
LP-1 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HwOGlEPTB;MkOuPFA6PyEQvF2= MnH3V2FPT0WU
GI-ME-N M2PvSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfYcJlKSzVyPUK0MlI6OiEQvF2= M1jDcnNCVkeHUh?=
MPP-89 M1THSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fpRWlEPTB;MkWuNlA{PiEQvF2= MmLLV2FPT0WU
U-698-M MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7DXZhXUUN3ME2yOU4zPTB|IN88US=> M{TsSnNCVkeHUh?=
HC-1 MmHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjJR5FXUUN3ME2yOU43PDF6IN88US=> NGnGZY1USU6JRWK=
HCC2157 NH3ZeIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjSTWM2OD1{NT62O|Mh|ryP M4POR3NCVkeHUh?=
MOLT-4 M2OyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK1TWM2OD1{Nj6yO|Mh|ryP MkTyV2FPT0WU
LS-411N MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELYbo5KSzVyPUK2MlM{PjlizszN MXTTRW5ITVJ?
Becker MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJ4LkWxPFEh|ryP M4K2UHNCVkeHUh?=
NCI-H23 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPJO5BKSzVyPUK2Mlc2PzVizszN MX3TRW5ITVJ?
IST-SL1 NXO2UoJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHjdnJKSzVyPUK3MlM5PjdizszN M{O2UHNCVkeHUh?=
MZ2-MEL MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHXTWM2OD1{Nz60OVY3KM7:TR?= MXnTRW5ITVJ?
RKO M4nVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTJ6LkG0OFYh|ryP NIrsZ2dUSU6JRWK=
TE-441-T M4G4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7mWGRWUUN3ME2yPE44QDlizszN MY\TRW5ITVJ?
EW-24 NGjnZo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHKTWM2OD1{OT6xNlU6KM7:TR?= MWHTRW5ITVJ?
no-10 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJ7LkG2N|Eh|ryP MYfTRW5ITVJ?
D-542MG NUHvNFlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M360cmlEPTB;MkmuPVIzOSEQvF2= MVTTRW5ITVJ?
ST486 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXER5ZTUUN3ME2zNE43PDVzIN88US=> MVTTRW5ITVJ?
KURAMOCHI MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7RTWM2OD1|MD64NFU4KM7:TR?= MVXTRW5ITVJ?
ES8 MnzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3HTWM2OD1|MT61PVczKM7:TR?= MnvSV2FPT0WU
BL-41 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXFNFFnUUN3ME2zNk4yODV2IN88US=> MmXtV2FPT0WU
NB6 MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILTUYZKSzVyPUOyMlM5PTVizszN MkHWV2FPT0WU
NCI-H1304 NFy2W|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTN{LkS5Olch|ryP NEThb4tUSU6JRWK=
MS-1 MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HVO2lEPTB;M{KuO|c2OSEQvF2= NHz3[21USU6JRWK=
MFH-ino M1voOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzRbGhKSzVyPUO0MlMzOjRizszN M1jqSXNCVkeHUh?=
NOS-1 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvzTWM2OD1|ND62O|Q5KM7:TR?= Ml;mV2FPT0WU
HUTU-80 NILCPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjyWZFKSzVyPUO1MlM3PjdizszN MnHGV2FPT0WU
EB2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LQPGlEPTB;M{[uOlE5QSEQvF2= MX;TRW5ITVJ?
L-540 NIrTeFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTN5LkKzNFgh|ryP NVzMPHNsW0GQR1XS
NCI-H747 NGqxW4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3RWW1KSzVyPUO4Mlg5PDZizszN MYTTRW5ITVJ?
NCI-H446 NHPSe|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M370WWlEPTB;M{muPVY2OSEQvF2= NHHlRnZUSU6JRWK=
MOLT-16 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{eyfmlEPTB;NEKuOFE2KM7:TR?= MlzOV2FPT0WU
BC-3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrmeo5KSzVyPUS1MlQ5QTZizszN Ml:wV2FPT0WU
SJSA-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTR3LkW0O|Qh|ryP NFHoeHRUSU6JRWK=
BB65-RCC NV;3emxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPzU3NKSzVyPUS1MlY3PiEQvF2= MWHTRW5ITVJ?
SNB75 MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fke2lEPTB;NE[uNFE5KM7:TR?= NEi3dmRUSU6JRWK=

... 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
  • 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
Smiles CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

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
    Volume
    Molecular Weight

*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
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 Completed 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.

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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