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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In DMSO USD 143 In stock
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Cited by 37 Publications

7 Customer Reviews

  • Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).

    Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck.

    Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies.

    Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck.

  • Inhibition of HER2 using siRNAs show a similar response measured by induced apoptosis, decreased proliferation and decreased phospho-p70-S6K staining as Lapatinib mono-treatment and combinatorial treatment with Lapatinib and trastuzumab. Trastuzumab mono-treatment is less efficient than siHER2.

    Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck.

    Lapatinib effectively inhibits EGFR activation, leading to a reduc- tion in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 μM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck.

  •  

    Endogenous associations between STAT1, EGFR, and p-STAT3 expression in breast cancer cells. (B) Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 uM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck.

    Combination treatment with lapatinib and CZ0775 significantly induces pro-apoptotic BIM proteins in H195 cells. HCC827 (a) and H1975 (b) cells were treated with either 1 μM lapatinib alone or the combination of 1 μM lapatinib plus 1 μM AZD6244 or CZ0775 for 24 h. Cell lysates were analyzed by Western blotting using the indicated antibodies. The levels of β -actin served as a loading control

    Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck.

  •  

    EGF and TGF-α-induced CD44 expression is reduced by EGFR inhibitors in SKBR3 breast cancer cells. After serum-starvation for 24 h, the cells were pretreated with EGFR inhibitors, AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then, treated with EGF (A) or TGF-α (B) for 24 h. The level of CD44 mRNA expression was analyzed by real-time PCR. After serum-starvation for 24 h, the cells were pretreated with AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then treated with EGF for 24 h (C). The levels of CD44, EGFR, ERK, and β-actin protein expression were analyzed by Western blotting.

    Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
c-Src [1]
(Cell-free assay)
C-Raf-1 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM 3.5 μM >10 μM
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 NGH5VGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\rUW1xUUN3ME2wMlAzPTR2IN88US=> NXL5eJV[W0GQR1XS
HCC2218 M3Pn[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMEWzNlYh|ryP NXrXfVluW0GQR1XS
OCUB-M NITSPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETj[nRKSzVyPUCuNFU4PCEQvF2= NEHhWnJUSU6JRWK=
ECC12 M2XYPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITQOWpKSzVyPUCuNFkzOzFizszN MkLkV2FPT0WU
DSH1 M4LGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n3UGlEPTB;MD6wPVM6PiEQvF2= MnOzV2FPT0WU
BT-474 MkjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoCzTWM2OD1yLkKxN|E2KM7:TR?= NWDjS|JIW0GQR1XS
BB30-HNC MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPXHJKSzVyPUCuNlQ3PTRizszN MYDTRW5ITVJ?
EKVX M4LSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D1cWlEPTB;MD60OFg4PCEQvF2= M4\J[nNCVkeHUh?=
TE-12 NWL5[IwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DFRWlEPTB;MD60PVA2PyEQvF2= MnrwV2FPT0WU
A388 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwN{KyOVgh|ryP MXHTRW5ITVJ?
TE-9 NIPjW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M360e2lEPTB;MD63OFQ2OyEQvF2= M{Oxe3NCVkeHUh?=
LB2241-RCC MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHWOGlKSzVyPUGuNVU1ODNizszN NV;WNottW0GQR1XS
LB996-RCC MlPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PHNGlEPTB;MT6zOlIzQCEQvF2= M4q0THNCVkeHUh?=
LC-1F M4rVZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwM{iyOFQh|ryP NX;pXpVZW0GQR1XS
TE-6 M2\mbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLvNJFKSzVyPUGuOVUzODFizszN NYTZdZF1W0GQR1XS
A253 MoK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\MTWM2OD1zLkm3N|M2KM7:TR?= NWTER3o3W0GQR1XS
OS-RC-2 NWHLUoFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnxS|hKSzVyPUGuPVkyQTlizszN MVfTRW5ITVJ?
TE-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJwMES4N{DPxE1? NWLZbnhlW0GQR1XS
RL95-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDmflFDUUN3ME2zMlE2PjdizszN NHvad|NUSU6JRWK=
LS-513 M4\FSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPJbIRKSzVyPUOuOFAxPDFizszN MoLMV2FPT0WU
DJM-1 MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPY[YxOUUN3ME2zMlQ3QTd3IN88US=> M2nxNXNCVkeHUh?=
NMC-G1 M2PNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXQclNvUUN3ME2zMlU1PTBzIN88US=> MnzVV2FPT0WU
TE-10 Mlf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DUNmlEPTB;Mz61OVM2PiEQvF2= M1PVfnNCVkeHUh?=
TE-5 NW\UWZp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTK[3FbUUN3ME20MlA{PzNizszN NXfiO3ZsW0GQR1XS
TK10 M2nCPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwMU[1NlIh|ryP NF7afYZUSU6JRWK=
UACC-812 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTRwNU[xOVMh|ryP NIn6e29USU6JRWK=
SW962 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnvTlRKSzVyPUWuNFIyPTlizszN M1;jNXNCVkeHUh?=
SW954 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rwNWlEPTB;NT6zPVI1PSEQvF2= NX;OTWlUW0GQR1XS
COLO-668 NUjsZoRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTVwN{K2Olch|ryP NFTPbGRUSU6JRWK=
LB1047-RCC NIDMeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFntdIxKSzVyPUWuPFAxPDZizszN M2LKNnNCVkeHUh?=
NB5 M1rubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLyfnNKSzVyPU[uNlExODFizszN NG\nNJdUSU6JRWK=
NTERA-S-cl-D1 MofHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XCRWlEPTB;Nj6yOlU3OSEQvF2= Ml:0V2FPT0WU
IST-MEL1 NGfxeFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLCV5pKSzVyPU[uOFM3QTRizszN MoW2V2FPT0WU
GI-1 NUnFUW1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTZwNUG2PFIh|ryP MUfTRW5ITVJ?
TGBC1TKB NIe3Z3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jiSWlEPTB;Nz6wO|E5OyEQvF2= Ml3NV2FPT0WU
GT3TKB M3LFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXFTFFKSzVyPUeuNlI4PDRizszN MX7TRW5ITVJ?
EVSA-T M3rz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPOTWM2OD15LkSyPFEyKM7:TR?= MkTsV2FPT0WU
D-502MG NGTY[WJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTdwNEi4PVQh|ryP MmTKV2FPT0WU
TE-8 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTdwN{[xOVkh|ryP M4O2VnNCVkeHUh?=
OVCAR-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\xW2hKSzVyPUmuNVE3PzVizszN NHW2cJhUSU6JRWK=
D-336MG NEfKeFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTlwNEezPVUh|ryP NXy2UWlUW0GQR1XS
GCIY M33PcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:4WmlEPTB;OT61O|QzKM7:TR?= NVvKd|BrW0GQR1XS
KS-1 NYfLbpUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXzU4VuUUN3ME25MlY3Ojh5IN88US=> MWHTRW5ITVJ?
HCC2998 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ziVWlEPTB;OT65OlMxPyEQvF2= NV:xSGxYW0GQR1XS
D-247MG NHLTS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G2XWlEPTB;OT65PFI6OSEQvF2= M1nh[XNCVkeHUh?=
TE-15 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFyLkK0OUDPxE1? MXfTRW5ITVJ?
IST-MES1 NFjXcW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTDd3pwUUN3ME2xNE4zPTZ3IN88US=> MlfvV2FPT0WU
ETK-1 Mn3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjOfJJKUUN3ME2xNE43OjNizszN NV3zR2dmW0GQR1XS
RCC10RGB M{\yNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUntVmRqUUN3ME2xNE46PjFizszN M2HETnNCVkeHUh?=
KNS-42 NYHJSnp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFzLkeyOVUh|ryP NV2yOVlOW0GQR1XS
LB771-HNC NFiyNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXiTWM2OD1zMj6xO|EzKM7:TR?= MojGV2FPT0WU
SR NFfZO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF{LkKwOlQh|ryP NGXw[JpUSU6JRWK=
NCI-H1355 M1jSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fZOmlEPTB;MUKuPFk5PSEQvF2= NHHPc|RUSU6JRWK=
ES6 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP2fZhKSzVyPUGzMlA4QCEQvF2= NI\G[JdUSU6JRWK=
SK-NEP-1 NUPLVoNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfBZ3ZMUUN3ME2xN{4zPTd5IN88US=> NITWOmtUSU6JRWK=
D-392MG MlvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\5dpd2UUN3ME2xN{43PDJ6IN88US=> MlzkV2FPT0WU
NB7 NYj2OnVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH2TWM2OD1zND6yN|c1KM7:TR?= Mm\uV2FPT0WU
SK-LMS-1 NIXOd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXITWM2OD1zND61NVQ2KM7:TR?= M1nj[3NCVkeHUh?=
SK-UT-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjBTWM2OD1zND63PFg6KM7:TR?= MlrzV2FPT0WU
CA46 NHv5blRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF3LkC1PFYh|ryP M1jBXXNCVkeHUh?=
IST-SL2 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzRTWM2OD1zNT6xPVAyKM7:TR?= MljKV2FPT0WU
BC-1 NGXiN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfaTWM2OD1zNT6zN|E1KM7:TR?= Ml[3V2FPT0WU
LS-123 M3LL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DvUmlEPTB;MUWuPFE4OyEQvF2= Ml;KV2FPT0WU
Ramos-2G6-4C10 NUnvZ3hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVra[3RSUUN3ME2xOk4xQTJ2IN88US=> NXjQSpdNW0GQR1XS
MZ1-PC M{fNOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LBdmlEPTB;MU[uO|MyOyEQvF2= MlG2V2FPT0WU
LB647-SCLC M4PrN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r2NmlEPTB;MU[uPVM4OiEQvF2= M{jYOHNCVkeHUh?=
NCI-H1694 MnyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF5LkG1Nlkh|ryP NUfUe2FuW0GQR1XS
NCI-H322M M2jCSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF5LkSzOlYh|ryP M{DYWXNCVkeHUh?=
ES7 M{L4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILxe3VKSzVyPUG4MlM6OTRizszN M4jHTXNCVkeHUh?=
LC-2-ad MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfMUVZKSzVyPUG4MlQ{QDZizszN M2mwbHNCVkeHUh?=
SF268 NH;yTmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTF6Lke0NFkh|ryP NX\rRWdjW0GQR1XS
RPMI-8402 NXvTRpRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXCbXhGUUN3ME2xPU4xPzR{IN88US=> NGrZXXlUSU6JRWK=
HCE-T Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjoUnZ2UUN3ME2yNE4zOzR2IN88US=> Mn;YV2FPT0WU
A101D MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTJyLki1PFch|ryP M1jJT3NCVkeHUh?=
MRK-nu-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJyLkmxN{DPxE1? NEW0SpNUSU6JRWK=
LXF-289 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvLR2lKSzVyPUKxMlA{QCEQvF2= MUfTRW5ITVJ?
NALM-6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJzLkG5Olch|ryP MWfTRW5ITVJ?
DOHH-2 MkDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJzLkS4NVMh|ryP MW\TRW5ITVJ?
EW-16 NF3wfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJ{LkG0NFIh|ryP MkTpV2FPT0WU
A4-Fuk MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnqTWM2OD1{Mj6yNVQ6KM7:TR?= NXTYcnRQW0GQR1XS
HD-MY-Z MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ{LkO5OlUh|ryP NF;CVIxUSU6JRWK=
SKM-1 M{TM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;qZ2lEPTB;MkKuO|M2OSEQvF2= NVTzSFhbW0GQR1XS
DMS-153 NWDjc4xXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfoZpdKSzVyPUKzMlQzODRizszN MWLTRW5ITVJ?
LB373-MEL-D Moq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fRN2lEPTB;MkOuOVQ2OiEQvF2= M{eybHNCVkeHUh?=
LP-1 MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXIVHdiUUN3ME2yN{45ODl5IN88US=> NF7YfIZUSU6JRWK=
GI-ME-N NH3nOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ2LkK5NkDPxE1? NVzwN3JEW0GQR1XS
MPP-89 NFyzR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXCTlhmUUN3ME2yOU4zODN4IN88US=> NIjHZXpUSU6JRWK=
U-698-M NHXIPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJ3LkK1NFMh|ryP MUfTRW5ITVJ?
HC-1 M1e5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T2Z2lEPTB;MkWuOlQyQCEQvF2= M2DoSXNCVkeHUh?=
HCC2157 NXzQO5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPTfGRqUUN3ME2yOU43PzNizszN M4\j[nNCVkeHUh?=
MOLT-4 M2rFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfsVItkUUN3ME2yOk4zPzNizszN MoX4V2FPT0WU
LS-411N M3\kcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG4R4lsUUN3ME2yOk4{OzZ7IN88US=> MUPTRW5ITVJ?
Becker NYPpbWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\DPGlEPTB;Mk[uOVE5OSEQvF2= NILmWJBUSU6JRWK=
NCI-H23 NUjMPWNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[ze2lEPTB;Mk[uO|U4PSEQvF2= NX\iS2l6W0GQR1XS
IST-SL1 NHv2[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHDUYFDUUN3ME2yO{4{QDZ5IN88US=> MoOwV2FPT0WU
MZ2-MEL MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjOeW1KSzVyPUK3MlQ2PjZizszN M{\3V3NCVkeHUh?=
RKO Ml7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XXbWlEPTB;MkiuNVQ1PiEQvF2= NUXCSYdGW0GQR1XS
TE-441-T MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:1U2VKSzVyPUK4Mlc5QSEQvF2= M4m1U3NCVkeHUh?=
EW-24 NHrV[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4qybGlEPTB;MkmuNVI2QSEQvF2= MVXTRW5ITVJ?
no-10 Mn;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3HTWM2OD1{OT6xOlMyKM7:TR?= Mn:yV2FPT0WU
D-542MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K3fGlEPTB;MkmuPVIzOSEQvF2= MlvSV2FPT0WU
ST486 NICxbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO2TWM2OD1|MD62OFUyKM7:TR?= M{HZZnNCVkeHUh?=
KURAMOCHI MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\pNWlEPTB;M{CuPFA2PyEQvF2= NGryW2xUSU6JRWK=
ES8 MoS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fOV2lEPTB;M{GuOVk4OiEQvF2= MnTsV2FPT0WU
BL-41 Mnr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fKW2lEPTB;M{KuNVA2PCEQvF2= MVnTRW5ITVJ?
NB6 M3fpeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjQNmQyUUN3ME2zNk4{QDV3IN88US=> NF7k[VVUSU6JRWK=
NCI-H1304 MknYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXSTWM2OD1|Mj60PVY4KM7:TR?= MkG0V2FPT0WU
MS-1 M37FOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4e1emlEPTB;M{KuO|c2OSEQvF2= MXHTRW5ITVJ?
MFH-ino NF;sSmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTN2LkOyNlQh|ryP MWXTRW5ITVJ?
NOS-1 NVTURohjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLWTWM2OD1|ND62O|Q5KM7:TR?= MUfTRW5ITVJ?
HUTU-80 M3yyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTN3LkO2Olch|ryP MnPrV2FPT0WU
EB2 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X3OGlEPTB;M{[uOlE5QSEQvF2= Mn;XV2FPT0WU
L-540 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DqVWlEPTB;M{euNlMxQCEQvF2= Ml;XV2FPT0WU
NCI-H747 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTN6Lki4OFYh|ryP M4fB[XNCVkeHUh?=
NCI-H446 NW[xbZV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f0OmlEPTB;M{muPVY2OSEQvF2= NY\6VmluW0GQR1XS
MOLT-16 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG1TWM2OD12Mj60NVUh|ryP MlK2V2FPT0WU
BC-3 NWG0[Fc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\GellTUUN3ME20OU41QDl4IN88US=> MV;TRW5ITVJ?
SJSA-1 NV7vNXNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR3LkW0O|Qh|ryP NYfwSJh2W0GQR1XS
BB65-RCC MlXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XzPWlEPTB;NEWuOlY3KM7:TR?= NVHWbFQ4W0GQR1XS
SNB75 NGT5SlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR4LkCxPEDPxE1? MUfTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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
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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
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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
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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)

  • 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02836847 Recruiting Cholangiocarcinoma of the Extrahepatic Bile Duct|Gallbladder Cancer Shanghai Jiao Tong University School of Medicine|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Ruijin Hospital|RenJi Hospital|Eastern Hepatobiliary Surgery Hospital|Huashan Hospital July 2016 Phase 2
NCT02650752 Recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 2016 Phase 1
NCT02581124 Completed Anemia of Chronic Kidney Disease Akros Pharma Inc. October 2015 Phase 1
NCT02559778 Recruiting Neuroblastoma Giselle Sholler|Dell, Inc.|Beat NB Cancer Foundation|Because of Ezra|Spectrum Health Hospitals September 2015 Phase 1
NCT02422199 Active, not recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co., Ltd. May 2015 Phase 1|Phase 2
NCT02362958 Recruiting HER2 Positive Breast Cancer Sun Yat-sen University February 2015 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