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 302 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 M4LQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljWTWM2OD1yLkCyOVQ1KM7:TR?= NIDKN3RUSU6JRWK=
HCC2218 M3TEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInON3NKSzVyPUCuNFU{OjZizszN NVnOT483W0GQR1XS
OCUB-M M1z1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\zTWM2OD1yLkC1O|Qh|ryP NYnqZ5Z{W0GQR1XS
ECC12 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMEmyN|Eh|ryP MnXHV2FPT0WU
DSH1 MlyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvETWM2OD1yLkC5N|k3KM7:TR?= NFPQUZdUSU6JRWK=
BT-474 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMkGzNVUh|ryP NEL1bnVUSU6JRWK=
BB30-HNC NYnYU3hET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O3UGlEPTB;MD6yOFY2PCEQvF2= MnXFV2FPT0WU
EKVX NW\XbY8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jIfmlEPTB;MD60OFg4PCEQvF2= NWX0fnZbW0GQR1XS
TE-12 MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm0TWM2OD1yLkS5NFU4KM7:TR?= M4T1OHNCVkeHUh?=
A388 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwN{KyOVgh|ryP MUfTRW5ITVJ?
TE-9 NUSwbJJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm3cZBKSzVyPUCuO|Q1PTNizszN MYDTRW5ITVJ?
LB2241-RCC NILCXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XzWGlEPTB;MT6xOVQxOyEQvF2= MVvTRW5ITVJ?
LB996-RCC MmC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\4R402UUN3ME2xMlM3OjJ6IN88US=> NWjsWmx2W0GQR1XS
LC-1F NIfxbVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mor2TWM2OD1zLkO4NlQ1KM7:TR?= NGTSeXVUSU6JRWK=
TE-6 Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjMbHV{UUN3ME2xMlU2OjBzIN88US=> MWPTRW5ITVJ?
A253 NGLyRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwOUezN|Uh|ryP MVvTRW5ITVJ?
OS-RC-2 Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTkTWM2OD1zLkm5NVk6KM7:TR?= M1\VWHNCVkeHUh?=
TE-1 M37TWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nTN2lEPTB;Mj6wOFg{KM7:TR?= MkTxV2FPT0WU
RL95-2 NXXMNpF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLISXlKSzVyPUOuNVU3PyEQvF2= M3:wd3NCVkeHUh?=
LS-513 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjmTWM2OD1|LkSwNFQyKM7:TR?= M{PLUXNCVkeHUh?=
DJM-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTNwNE[5O|Uh|ryP MWjTRW5ITVJ?
NMC-G1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTNwNUS1NFEh|ryP MmjhV2FPT0WU
TE-10 MmrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTNwNUWzOVYh|ryP NEnScppUSU6JRWK=
TE-5 NVTYOFl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYj4O5lmUUN3ME20MlA{PzNizszN M4HUR3NCVkeHUh?=
TK10 M3fxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDZW2p{UUN3ME20MlE3PTJ{IN88US=> M1XNU3NCVkeHUh?=
UACC-812 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LO[WlEPTB;ND61OlE2OyEQvF2= NWPCVFJvW0GQR1XS
SW962 M2Hxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13iVmlEPTB;NT6wNlE2QSEQvF2= NIq2WlZUSU6JRWK=
SW954 NH7VWnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTVwM{myOFUh|ryP MknyV2FPT0WU
COLO-668 NE[wbJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HKNGlEPTB;NT63NlY3PyEQvF2= NGjSZZJUSU6JRWK=
LB1047-RCC Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTVwOECwOFYh|ryP MWLTRW5ITVJ?
NB5 NFfsT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPITWM2OD14LkKxNFAyKM7:TR?= NXTZR2FlW0GQR1XS
NTERA-S-cl-D1 NGrOfIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTZwMk[1OlEh|ryP NWXiZ4dsW0GQR1XS
IST-MEL1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHlXWZmUUN3ME22MlQ{Pjl2IN88US=> M3fnV3NCVkeHUh?=
GI-1 NYnKUGhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTZwNUG2PFIh|ryP NIT3R45USU6JRWK=
TGBC1TKB M3TUSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TuTGlEPTB;Nz6wO|E5OyEQvF2= NGnPUpJUSU6JRWK=
GT3TKB NIn6W3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTdwMkK3OFQh|ryP M2joO3NCVkeHUh?=
EVSA-T MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;TTWM2OD15LkSyPFEyKM7:TR?= NEfNeJhUSU6JRWK=
D-502MG NXzTSpZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknnTWM2OD15LkS4PFk1KM7:TR?= M17tdXNCVkeHUh?=
TE-8 Ml;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWewV49lUUN3ME23Mlc3OTV7IN88US=> MVXTRW5ITVJ?
OVCAR-4 NVPOZ4JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfYOoRDUUN3ME25MlEyPjd3IN88US=> MWfTRW5ITVJ?
D-336MG MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jVS2lEPTB;OT60O|M6PSEQvF2= NH3zbodUSU6JRWK=
GCIY NUizXnhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXkTWM2OD17LkW3OFIh|ryP NIHZRoxUSU6JRWK=
KS-1 NFrERoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XmUGlEPTB;OT62OlI5PyEQvF2= NWTKcGc6W0GQR1XS
HCC2998 NULnT5BQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJTWM2OD17Lkm2N|A4KM7:TR?= M2DIRnNCVkeHUh?=
D-247MG NInuTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPPVllOUUN3ME25Mlk5OjlzIN88US=> M2DkZXNCVkeHUh?=
TE-15 Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfqXFZKSzVyPUGwMlI1PSEQvF2= MVnTRW5ITVJ?
IST-MES1 M4PRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjnbml2UUN3ME2xNE4zPTZ3IN88US=> MVvTRW5ITVJ?
ETK-1 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnsfWtKSzVyPUGwMlYzOyEQvF2= M2\sXnNCVkeHUh?=
RCC10RGB NH7s[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT5TWM2OD1zMD65OlEh|ryP Mn6wV2FPT0WU
KNS-42 NVXPelV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\RTWM2OD1zMT63NlU2KM7:TR?= NUHVS2dkW0GQR1XS
LB771-HNC NGjsU|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DSOGlEPTB;MUKuNVcyOiEQvF2= MXzTRW5ITVJ?
SR NVm4[mxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULSWJI5UUN3ME2xNk4zODZ2IN88US=> NYD6bJp7W0GQR1XS
NCI-H1355 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCzTWM2OD1zMj64PVg2KM7:TR?= NHTaOZVUSU6JRWK=
ES6 MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjGTWM2OD1zMz6wO|gh|ryP Mn7PV2FPT0WU
SK-NEP-1 MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3GzemlEPTB;MUOuNlU4PyEQvF2= MnfwV2FPT0WU
D-392MG NYHkZ2Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmexTWM2OD1zMz62OFI5KM7:TR?= NYnQTHRGW0GQR1XS
NB7 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HXWWlEPTB;MUSuNlM4PCEQvF2= Mor3V2FPT0WU
SK-LMS-1 Mn;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnSeW1UUUN3ME2xOE42OTR3IN88US=> M33wTnNCVkeHUh?=
SK-UT-1 NITVS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILIT5dKSzVyPUG0Mlc5QDlizszN MYfTRW5ITVJ?
CA46 M3rZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTlTWM2OD1zNT6wOVg3KM7:TR?= NIiyTIlUSU6JRWK=
IST-SL2 NEHUNJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4r0WWlEPTB;MUWuNVkxOSEQvF2= NHfJS5lUSU6JRWK=
BC-1 M1XVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfISVlKSzVyPUG1MlM{OTRizszN MYTTRW5ITVJ?
LS-123 NYXMO2pTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr2O2lDUUN3ME2xOU45OTd|IN88US=> M{XVZXNCVkeHUh?=
Ramos-2G6-4C10 Mlf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DCN2lEPTB;MU[uNFkzPCEQvF2= M37wWHNCVkeHUh?=
MZ1-PC NUCzc5ZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T2ZmlEPTB;MU[uO|MyOyEQvF2= MoXaV2FPT0WU
LB647-SCLC M1TQcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF4LkmzO|Ih|ryP Mk[wV2FPT0WU
NCI-H1694 NXvV[5RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\vfGlEPTB;MUeuNVUzQSEQvF2= MnvPV2FPT0WU
NCI-H322M MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{mwbmlEPTB;MUeuOFM3PiEQvF2= NHzPSHJUSU6JRWK=
ES7 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULzSZliUUN3ME2xPE4{QTF2IN88US=> MoD0V2FPT0WU
LC-2-ad MnPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7UTWM2OD1zOD60N|g3KM7:TR?= NUm0b4hsW0GQR1XS
SF268 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG5eWdpUUN3ME2xPE44PDB7IN88US=> M3vydnNCVkeHUh?=
RPMI-8402 MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF7LkC3OFIh|ryP M4DndXNCVkeHUh?=
HCE-T NGSxenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XHPWlEPTB;MkCuNlM1PCEQvF2= M3j0VHNCVkeHUh?=
A101D NHzEclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJyLki1PFch|ryP NF7Se3BUSU6JRWK=
MRK-nu-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X1fGlEPTB;MkCuPVE{KM7:TR?= MWHTRW5ITVJ?
LXF-289 NGD5WY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\1cWJKSzVyPUKxMlA{QCEQvF2= NEjVPGZUSU6JRWK=
NALM-6 NF3kUGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJzLkG5Olch|ryP NYHjT|RrW0GQR1XS
DOHH-2 MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJzLkS4NVMh|ryP M3L0ZXNCVkeHUh?=
EW-16 M3rib2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJ{LkG0NFIh|ryP NW[2[WgzW0GQR1XS
A4-Fuk NI\yflZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXMTWM2OD1{Mj6yNVQ6KM7:TR?= Mnj0V2FPT0WU
HD-MY-Z M1uwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHTPGVCUUN3ME2yNk4{QTZ3IN88US=> Ml3kV2FPT0WU
SKM-1 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ{LkezOVEh|ryP NHrrbWJUSU6JRWK=
DMS-153 NYX0XFRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\TTWM2OD1{Mz60NlA1KM7:TR?= NHj0VpdUSU6JRWK=
LB373-MEL-D MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q4UGlEPTB;MkOuOVQ2OiEQvF2= MkLrV2FPT0WU
LP-1 NFG1e|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jleGlEPTB;MkOuPFA6PyEQvF2= M{jMXXNCVkeHUh?=
GI-ME-N MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHHRY1KSzVyPUK0MlI6OiEQvF2= MorDV2FPT0WU
MPP-89 NVjXSXBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ3LkKwN|Yh|ryP M3K1OnNCVkeHUh?=
U-698-M MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjUTJVKSzVyPUK1MlI2ODNizszN NYHKRm1sW0GQR1XS
HC-1 NIPqUY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJ3Lk[0NVgh|ryP MXLTRW5ITVJ?
HCC2157 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD0TWM2OD1{NT62O|Mh|ryP MVTTRW5ITVJ?
MOLT-4 M{KyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe3U294UUN3ME2yOk4zPzNizszN M2C5bHNCVkeHUh?=
LS-411N MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDpTWM2OD1{Nj6zN|Y6KM7:TR?= NWPBXHlOW0GQR1XS
Becker Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJ4LkWxPFEh|ryP MmLrV2FPT0WU
NCI-H23 NWD5WHQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJ4Lke1O|Uh|ryP NVjuZ4x4W0GQR1XS
IST-SL1 NWnhRmpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u0W2lEPTB;MkeuN|g3PyEQvF2= NVHQdlB5W0GQR1XS
MZ2-MEL Mmr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7vfJpKSzVyPUK3MlQ2PjZizszN NF;HeoxUSU6JRWK=
RKO M3P1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;0bWlEPTB;MkiuNVQ1PiEQvF2= NGezd3pUSU6JRWK=
TE-441-T NYfRT5V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInnNHRKSzVyPUK4Mlc5QSEQvF2= M13tSHNCVkeHUh?=
EW-24 Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrycIZKSzVyPUK5MlEzPTlizszN NHfxUItUSU6JRWK=
no-10 M2npSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJ7LkG2N|Eh|ryP MVfTRW5ITVJ?
D-542MG NVPqUJlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDGS2ZKSzVyPUK5MlkzOjFizszN MnrUV2FPT0WU
ST486 M4LDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjrfIRDUUN3ME2zNE43PDVzIN88US=> MlfOV2FPT0WU
KURAMOCHI MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HTR2lEPTB;M{CuPFA2PyEQvF2= NYnweGZ{W0GQR1XS
ES8 NHLT[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTBTWM2OD1|MT61PVczKM7:TR?= NHHoeXlUSU6JRWK=
BL-41 Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1e5bmlEPTB;M{KuNVA2PCEQvF2= M1HEPXNCVkeHUh?=
NB6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\zNmlEPTB;M{KuN|g2PSEQvF2= MoPuV2FPT0WU
NCI-H1304 NFXXTmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXEbnlOUUN3ME2zNk41QTZ5IN88US=> NYfCfGw3W0GQR1XS
MS-1 M4Po[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDpTWM2OD1|Mj63O|UyKM7:TR?= NGXUOZVUSU6JRWK=
MFH-ino NYjjWIJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ji[GlEPTB;M{SuN|IzPCEQvF2= NXflW5N[W0GQR1XS
NOS-1 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XZfGlEPTB;M{SuOlc1QCEQvF2= M2POT3NCVkeHUh?=
HUTU-80 NYLzNGlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\QTWM2OD1|NT6zOlY4KM7:TR?= MlrBV2FPT0WU
EB2 M1uz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDKdJAzUUN3ME2zOk43OTh7IN88US=> M13vOnNCVkeHUh?=
L-540 NEXtR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTSeVJyUUN3ME2zO{4zOzB6IN88US=> MnT3V2FPT0WU
NCI-H747 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nIWGlEPTB;M{iuPFg1PiEQvF2= Mmr4V2FPT0WU
NCI-H446 MlvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1G5SGlEPTB;M{muPVY2OSEQvF2= NH6zPWlUSU6JRWK=
MOLT-16 NXW0[W52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnpc2F{UUN3ME20Nk41OTVizszN MXnTRW5ITVJ?
BC-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTQ[mRKSzVyPUS1MlQ5QTZizszN NYGwV|FYW0GQR1XS
SJSA-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXWyXlAzUUN3ME20OU42PDd2IN88US=> NWn3dY9QW0GQR1XS
BB65-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR3Lk[2OkDPxE1? M{Xkd3NCVkeHUh?=
SNB75 NFXhfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjqTWM2OD12Nj6wNVgh|ryP NUK1ZZVLW0GQR1XS

... 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)

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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