Lapatinib

For research use only. Not for use in humans.

Catalog No.S2111 Synonyms: GW-572016, GSK572016

309 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.

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Selleck's Lapatinib has been cited by 309 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 M1m0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HDS2lEPTB;MD6wNlU1PCEQvF2= NWfMTopJW0GQR1XS
HCC2218 Mn3nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX5TWM2OD1yLkC1N|I3KM7:TR?= NYT1ZotnW0GQR1XS
OCUB-M M4HiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTIWoVKSzVyPUCuNFU4PCEQvF2= NYq4dnpqW0GQR1XS
ECC12 MnOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknGTWM2OD1yLkC5NlMyKM7:TR?= NHvoO5NUSU6JRWK=
DSH1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwMEmzPVYh|ryP MlO0V2FPT0WU
BT-474 MnXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzPPZNKSzVyPUCuNlE{OTVizszN MlrsV2FPT0WU
BB30-HNC M4XMW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTY[VZYUUN3ME2wMlI1PjV2IN88US=> M2TQUXNCVkeHUh?=
EKVX NYr3WJpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnqVGdyUUN3ME2wMlQ1QDd2IN88US=> MX7TRW5ITVJ?
TE-12 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rUVWlEPTB;MD60PVA2PyEQvF2= MmSzV2FPT0WU
A388 NFrkV5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXzTWM2OD1yLkeyNlU5KM7:TR?= Ml\KV2FPT0WU
TE-9 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe4UYpKSzVyPUCuO|Q1PTNizszN M{XrPXNCVkeHUh?=
LB2241-RCC MorXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PXUWlEPTB;MT6xOVQxOyEQvF2= MWPTRW5ITVJ?
LB996-RCC MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4qwPGlEPTB;MT6zOlIzQCEQvF2= NWPsT3RQW0GQR1XS
LC-1F NH34WmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLYTWM2OD1zLkO4NlQ1KM7:TR?= Mlz2V2FPT0WU
TE-6 NWLadnhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr3TWM2OD1zLkW1NlAyKM7:TR?= MlzpV2FPT0WU
A253 NETIcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHlSIdKSzVyPUGuPVc{OzVizszN MX3TRW5ITVJ?
OS-RC-2 NVrxfnRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm1VXE6UUN3ME2xMlk6OTl7IN88US=> MoGxV2FPT0WU
TE-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vncWlEPTB;Mj6wOFg{KM7:TR?= MVXTRW5ITVJ?
RL95-2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzT[GlwUUN3ME2zMlE2PjdizszN NHfMR3ZUSU6JRWK=
LS-513 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXD[JhnUUN3ME2zMlQxODRzIN88US=> MkHzV2FPT0WU
DJM-1 NInMXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCwPGhpUUN3ME2zMlQ3QTd3IN88US=> NX64TlIzW0GQR1XS
NMC-G1 NIjTbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLhfXNKSzVyPUOuOVQ2ODFizszN NIPWUVBUSU6JRWK=
TE-10 NVPMfW16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7QeG9KSzVyPUOuOVU{PTZizszN NUDU[FM4W0GQR1XS
TE-5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;OTWM2OD12LkCzO|Mh|ryP NX;le3o4W0GQR1XS
TK10 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrwUXRKUUN3ME20MlE3PTJ{IN88US=> NUXwVHRGW0GQR1XS
UACC-812 NUnCc|BoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTQTWM2OD12LkW2NVU{KM7:TR?= NH3EXmtUSU6JRWK=
SW962 NHHSOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom4TWM2OD13LkCyNVU6KM7:TR?= MXHTRW5ITVJ?
SW954 NWS5OXl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTVwM{myOFUh|ryP NUX5c451W0GQR1XS
COLO-668 Ml[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEH0N5JKSzVyPUWuO|I3PjdizszN NITSO3RUSU6JRWK=
LB1047-RCC M37ZfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTFPJp1UUN3ME21MlgxODR4IN88US=> MlnGV2FPT0WU
NB5 MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTZwMkGwNFEh|ryP MULTRW5ITVJ?
NTERA-S-cl-D1 NV3NTGNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTGZY5OUUN3ME22MlI3PTZzIN88US=> M4ftOnNCVkeHUh?=
IST-MEL1 Mo\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HFPWlEPTB;Nj60N|Y6PCEQvF2= NGfyXG9USU6JRWK=
GI-1 NUPrZlNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nxSGlEPTB;Nj61NVY5OiEQvF2= M{LnTXNCVkeHUh?=
TGBC1TKB MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjoe3NKSzVyPUeuNFcyQDNizszN MnrRV2FPT0WU
GT3TKB NWHrPXJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyTWM2OD15LkKyO|Q1KM7:TR?= NH3kOFFUSU6JRWK=
EVSA-T Ml\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLLTmVKSzVyPUeuOFI5OTFizszN Mmr4V2FPT0WU
D-502MG M1S0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jNWWlEPTB;Nz60PFg6PCEQvF2= NHfHVGtUSU6JRWK=
TE-8 Moe2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vMOGlEPTB;Nz63OlE2QSEQvF2= NXLH[ZBrW0GQR1XS
OVCAR-4 NVf6bmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUSzT|I4UUN3ME25MlEyPjd3IN88US=> Mo\vV2FPT0WU
D-336MG NVLpN4NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTlwNEezPVUh|ryP MUnTRW5ITVJ?
GCIY NWDZd3drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7hXXJKSzVyPUmuOVc1OiEQvF2= M4G1eXNCVkeHUh?=
KS-1 M1vuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTlwNk[yPFch|ryP NEDwW3BUSU6JRWK=
HCC2998 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC2UI0zUUN3ME25Mlk3OzB5IN88US=> NYPpUXBiW0GQR1XS
D-247MG NHHNR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLTOJZpUUN3ME25Mlk5OjlzIN88US=> MXPTRW5ITVJ?
TE-15 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSyTWM2OD1zMD6yOFUh|ryP MlzaV2FPT0WU
IST-MES1 M4\sZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;hNWttUUN3ME2xNE4zPTZ3IN88US=> NVjWeVNLW0GQR1XS
ETK-1 NX\hfVBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C3bGlEPTB;MUCuOlI{KM7:TR?= MlrkV2FPT0WU
RCC10RGB NGHQ[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTFyLkm2NUDPxE1? NHThT5hUSU6JRWK=
KNS-42 M1riPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TWVmlEPTB;MUGuO|I2PSEQvF2= NWrYbFFGW0GQR1XS
LB771-HNC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfxTWM2OD1zMj6xO|EzKM7:TR?= MoLkV2FPT0WU
SR MlvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzQeXZKSzVyPUGyMlIxPjRizszN NHTpT5JUSU6JRWK=
NCI-H1355 M3mwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPPXmpKSzVyPUGyMlg6QDVizszN NVvRXIJVW0GQR1XS
ES6 NX;PRll5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF|LkC3PEDPxE1? NUDPV2M{W0GQR1XS
SK-NEP-1 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF|LkK1O|ch|ryP NFjEc25USU6JRWK=
D-392MG NEHXfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvlN3kzUUN3ME2xN{43PDJ6IN88US=> Mli3V2FPT0WU
NB7 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD0TWM2OD1zND6yN|c1KM7:TR?= NWTmSo4xW0GQR1XS
SK-LMS-1 M3zMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[xd49KSzVyPUG0MlUyPDVizszN MnLBV2FPT0WU
SK-UT-1 NXrONmhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TQOGlEPTB;MUSuO|g5QSEQvF2= NELzO2hUSU6JRWK=
CA46 NX;MdI1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfTUIdKSzVyPUG1MlA2QDZizszN NXS0dGpXW0GQR1XS
IST-SL2 NVfLZopmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHCeJRKUUN3ME2xOU4yQTBzIN88US=> MoLCV2FPT0WU
BC-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fyfGlEPTB;MUWuN|MyPCEQvF2= M{jyenNCVkeHUh?=
LS-123 NXHCWZZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPXeWxKSzVyPUG1MlgyPzNizszN MUHTRW5ITVJ?
Ramos-2G6-4C10 NILvbVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTF4LkC5NlQh|ryP NUD2Zm93W0GQR1XS
MZ1-PC NIDxVZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorHTWM2OD1zNj63N|E{KM7:TR?= NWrXVWJHW0GQR1XS
LB647-SCLC M1LHeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF4LkmzO|Ih|ryP MVnTRW5ITVJ?
NCI-H1694 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\YU2FKSzVyPUG3MlE2OjlizszN M3fCdHNCVkeHUh?=
NCI-H322M M2j3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DFdGlEPTB;MUeuOFM3PiEQvF2= NIf2WmtUSU6JRWK=
ES7 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF6LkO5NVQh|ryP MmL0V2FPT0WU
LC-2-ad NVjCXG1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF6LkSzPFYh|ryP MYHTRW5ITVJ?
SF268 NHzHPGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXQZ|FQUUN3ME2xPE44PDB7IN88US=> M1TSbnNCVkeHUh?=
RPMI-8402 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD0TWM2OD1zOT6wO|QzKM7:TR?= NYHw[YVoW0GQR1XS
HCE-T NU\k[|hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJyLkKzOFQh|ryP MVnTRW5ITVJ?
A101D MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33iVmlEPTB;MkCuPFU5PyEQvF2= MWfTRW5ITVJ?
MRK-nu-1 Mm\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXMOYNKSzVyPUKwMlkyOyEQvF2= MYrTRW5ITVJ?
LXF-289 NWT2OZNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHWXmZTUUN3ME2yNU4xOzhizszN NXTOWINEW0GQR1XS
NALM-6 NW\ZcJNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJzLkG5Olch|ryP MUTTRW5ITVJ?
DOHH-2 NUTqeGtiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3UR5JKSzVyPUKxMlQ5OTNizszN NYjwemNLW0GQR1XS
EW-16 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJ{LkG0NFIh|ryP M1PzfnNCVkeHUh?=
A4-Fuk NUDPUIprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jte2lEPTB;MkKuNlE1QSEQvF2= M2jhfXNCVkeHUh?=
HD-MY-Z MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHlelBwUUN3ME2yNk4{QTZ3IN88US=> MkTpV2FPT0WU
SKM-1 NXXCWolHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLNeYJYUUN3ME2yNk44OzVzIN88US=> M1OzOHNCVkeHUh?=
DMS-153 NUXzO3g2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJ|LkSyNFQh|ryP MknsV2FPT0WU
LB373-MEL-D MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvJ[FFKSzVyPUKzMlU1PTJizszN NEf5O4xUSU6JRWK=
LP-1 M3TLTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD5TWM2OD1{Mz64NFk4KM7:TR?= NWX5VYl3W0GQR1XS
GI-ME-N NWj1cnFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\RPXNKSzVyPUK0MlI6OiEQvF2= MUXTRW5ITVJ?
MPP-89 M1[xZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHacIFKSzVyPUK1MlIxOzZizszN MUXTRW5ITVJ?
U-698-M M2LvV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\JTWM2OD1{NT6yOVA{KM7:TR?= M1[3OnNCVkeHUh?=
HC-1 M3HQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL0fFlPUUN3ME2yOU43PDF6IN88US=> M{G0SnNCVkeHUh?=
HCC2157 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnmwTWM2OD1{NT62O|Mh|ryP NGS3fZhUSU6JRWK=
MOLT-4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJ4LkK3N{DPxE1? MoDZV2FPT0WU
LS-411N NWP1cHlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJ4LkOzOlkh|ryP MVPTRW5ITVJ?
Becker NEXJeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XM[WlEPTB;Mk[uOVE5OSEQvF2= MYPTRW5ITVJ?
NCI-H23 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2THS2lEPTB;Mk[uO|U4PSEQvF2= NGHPOXpUSU6JRWK=
IST-SL1 NY\leIJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PNU2lEPTB;MkeuN|g3PyEQvF2= M3PINnNCVkeHUh?=
MZ2-MEL NGPvVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;F[mxKSzVyPUK3MlQ2PjZizszN NUHGfolIW0GQR1XS
RKO NXHSeFhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJ6LkG0OFYh|ryP MVzTRW5ITVJ?
TE-441-T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW1V2Z1UUN3ME2yPE44QDlizszN NXj5UINbW0GQR1XS
EW-24 NVu1cWo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHFblZ[UUN3ME2yPU4yOjV7IN88US=> NYHUc5FIW0GQR1XS
no-10 M163Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjhXldKSzVyPUK5MlE3OzFizszN Mn7uV2FPT0WU
D-542MG MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjDd4FKSzVyPUK5MlkzOjFizszN MonLV2FPT0WU
ST486 NUT5cHpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTNyLk[0OVEh|ryP NH;lWmhUSU6JRWK=
KURAMOCHI NID1VHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTNyLkiwOVch|ryP NGrJXXJUSU6JRWK=
ES8 MmfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF23O2dKSzVyPUOxMlU6PzJizszN M1j4XHNCVkeHUh?=
BL-41 MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1uycGlEPTB;M{KuNVA2PCEQvF2= M1v2WnNCVkeHUh?=
NB6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf4TWM2OD1|Mj6zPFU2KM7:TR?= MUjTRW5ITVJ?
NCI-H1304 MlfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;YWpVzUUN3ME2zNk41QTZ5IN88US=> NFThToRUSU6JRWK=
MS-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[4e2lEPTB;M{KuO|c2OSEQvF2= NV3LcZVXW0GQR1XS
MFH-ino NWPNZmo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPCOGV6UUN3ME2zOE4{OjJ2IN88US=> MVXTRW5ITVJ?
NOS-1 MoTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm5eXpKSzVyPUO0MlY4PDhizszN NV;zfm9oW0GQR1XS
HUTU-80 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXntcmo3UUN3ME2zOU4{PjZ5IN88US=> MmfwV2FPT0WU
EB2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTN4Lk[xPFkh|ryP M{PXWnNCVkeHUh?=
L-540 NVPocVVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTN5LkKzNFgh|ryP Mnn5V2FPT0WU
NCI-H747 M2mzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTM[JQ6UUN3ME2zPE45QDR4IN88US=> M1fRdnNCVkeHUh?=
NCI-H446 M{nQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\6OWlEPTB;M{muPVY2OSEQvF2= NHG1[XNUSU6JRWK=
MOLT-16 MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDvTWM2OD12Mj60NVUh|ryP M{TXTXNCVkeHUh?=
BC-3 NYqxRpJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrNN|AzUUN3ME20OU41QDl4IN88US=> Mki1V2FPT0WU
SJSA-1 M3XQUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf1fYVKSzVyPUS1MlU1PzRizszN MYTTRW5ITVJ?
BB65-RCC MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e1bGlEPTB;NEWuOlY3KM7:TR?= MXPTRW5ITVJ?
SNB75 M1fE[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7ORXhEUUN3ME20Ok4xOThizszN M2rONnNCVkeHUh?=

... 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
Smiles C[S](=O)(=O)CCNCC1=CC=C(O1)C2=CC=C3N=CN=C(NC4=CC=C(OCC5=CC=CC(=C5)F)C(=C4)Cl)C3=C2

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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    Volume
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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