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 38 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

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 M2fMRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe4c4FjUUN3ME2wMlAzPTR2IN88US=> MYDTRW5ITVJ?
HCC2218 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fYfGlEPTB;MD6wOVMzPiEQvF2= NHW4Om1USU6JRWK=
OCUB-M MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\rWmlEPTB;MD6wOVc1KM7:TR?= NU\sXZhTW0GQR1XS
ECC12 M2\RRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHWy[pBKSzVyPUCuNFkzOzFizszN M2\4OHNCVkeHUh?=
DSH1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3KepFrUUN3ME2wMlA6Ozl4IN88US=> M33QOnNCVkeHUh?=
BT-474 M2G0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnywTWM2OD1yLkKxN|E2KM7:TR?= NUW4dXlkW0GQR1XS
BB30-HNC NHzlSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vIOmlEPTB;MD6yOFY2PCEQvF2= NXX5b3ZJW0GQR1XS
EKVX MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DXPGlEPTB;MD60OFg4PCEQvF2= MkfEV2FPT0WU
TE-12 NV;rdo97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL3T2JKSzVyPUCuOFkxPTdizszN NVHEOZRKW0GQR1XS
A388 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS4S2FKSzVyPUCuO|IzPThizszN NWrO[GIyW0GQR1XS
TE-9 NVTCbWtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jKXGlEPTB;MD63OFQ2OyEQvF2= MmC4V2FPT0WU
LB2241-RCC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTKdYxWUUN3ME2xMlE2PDB|IN88US=> NYHjS|NwW0GQR1XS
LB996-RCC NInuUVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjXbZUzUUN3ME2xMlM3OjJ6IN88US=> NH;TTG9USU6JRWK=
LC-1F MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;pTWM2OD1zLkO4NlQ1KM7:TR?= NUW1RZlTW0GQR1XS
TE-6 NGLMOlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Pud2lEPTB;MT61OVIxOSEQvF2= MXHTRW5ITVJ?
A253 NWDVbos6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFwOUezN|Uh|ryP MUjTRW5ITVJ?
OS-RC-2 M1X4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LjSmlEPTB;MT65PVE6QSEQvF2= MVnTRW5ITVJ?
TE-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJwMES4N{DPxE1? M2fwOnNCVkeHUh?=
RL95-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PjUmlEPTB;Mz6xOVY4KM7:TR?= MXTTRW5ITVJ?
LS-513 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNwNECwOFEh|ryP M{XVT3NCVkeHUh?=
DJM-1 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXZ[llLUUN3ME2zMlQ3QTd3IN88US=> MlX3V2FPT0WU
NMC-G1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DibmlEPTB;Mz61OFUxOSEQvF2= NXTrW2d{W0GQR1XS
TE-10 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\STWM2OD1|LkW1N|U3KM7:TR?= NFTVPVFUSU6JRWK=
TE-5 NUK3RYFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojuTWM2OD12LkCzO|Mh|ryP Mlf2V2FPT0WU
TK10 M13wSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fnSmlEPTB;ND6xOlUzOiEQvF2= M4DZcXNCVkeHUh?=
UACC-812 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPRZWp{UUN3ME20MlU3OTV|IN88US=> NFzPVXlUSU6JRWK=
SW962 M3HFUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTVwMEKxOVkh|ryP M1[4WXNCVkeHUh?=
SW954 M{G2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTVwM{myOFUh|ryP M3fDdHNCVkeHUh?=
COLO-668 NF7VboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXiNXdKSzVyPUWuO|I3PjdizszN MU\TRW5ITVJ?
LB1047-RCC Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTVwOECwOFYh|ryP MV;TRW5ITVJ?
NB5 NIXXe21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37LXWlEPTB;Nj6yNVAxOSEQvF2= MUTTRW5ITVJ?
NTERA-S-cl-D1 NH;ON4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDadIo6UUN3ME22MlI3PTZzIN88US=> Mn3NV2FPT0WU
IST-MEL1 NFzyc2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTZwNEO2PVQh|ryP NHrGXI9USU6JRWK=
GI-1 NVn1W4U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfNTWM2OD14LkWxOlgzKM7:TR?= M2n2cHNCVkeHUh?=
TGBC1TKB NITBVVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrEe|BKSzVyPUeuNFcyQDNizszN NXTKNYN3W0GQR1XS
GT3TKB M3rRfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XMSmlEPTB;Nz6yNlc1PCEQvF2= MXvTRW5ITVJ?
EVSA-T M3LqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPQTWM2OD15LkSyPFEyKM7:TR?= Mkf4V2FPT0WU
D-502MG NUDkNGZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXDTWM2OD15LkS4PFk1KM7:TR?= M1nxdHNCVkeHUh?=
TE-8 MnLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTGTWM2OD15Lke2NVU6KM7:TR?= NVTDbXVrW0GQR1XS
OVCAR-4 MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37wXWlEPTB;OT6xNVY4PSEQvF2= MX7TRW5ITVJ?
D-336MG MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTlwNEezPVUh|ryP NGfSN3BUSU6JRWK=
GCIY MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTlwNUe0NkDPxE1? NYSw[ZZLW0GQR1XS
KS-1 M1jE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTlwNk[yPFch|ryP MWjTRW5ITVJ?
HCC2998 M1POVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjoOnFoUUN3ME25Mlk3OzB5IN88US=> NHz3OYNUSU6JRWK=
D-247MG M3PHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTlwOUiyPVEh|ryP NYnTVWE2W0GQR1XS
TE-15 NWjYdG9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfmSIV{UUN3ME2xNE4zPDVizszN NH3qNoJUSU6JRWK=
IST-MES1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvF[ZpKSzVyPUGwMlI2PjVizszN MYHTRW5ITVJ?
ETK-1 NYrme5FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M170bWlEPTB;MUCuOlI{KM7:TR?= MWjTRW5ITVJ?
RCC10RGB NXjmXY54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPBTWM2OD1zMD65OlEh|ryP MWjTRW5ITVJ?
KNS-42 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFzLkeyOVUh|ryP MXPTRW5ITVJ?
LB771-HNC NILWUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWWwUVU4UUN3ME2xNk4yPzF{IN88US=> NFzQb3lUSU6JRWK=
SR NH36UHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF{LkKwOlQh|ryP MoHPV2FPT0WU
NCI-H1355 NUK1S2kxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC1TWM2OD1zMj64PVg2KM7:TR?= NWXyVY1zW0GQR1XS
ES6 Mki2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLxRphYUUN3ME2xN{4xPzhizszN NHnpW4RUSU6JRWK=
SK-NEP-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXBU3BLUUN3ME2xN{4zPTd5IN88US=> MlG4V2FPT0WU
D-392MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG3SHpMUUN3ME2xN{43PDJ6IN88US=> MWTTRW5ITVJ?
NB7 MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLMSoM3UUN3ME2xOE4zOzd2IN88US=> NFHrfohUSU6JRWK=
SK-LMS-1 NHfafXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvVcVdsUUN3ME2xOE42OTR3IN88US=> MX3TRW5ITVJ?
SK-UT-1 NV;5cZVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nwTmlEPTB;MUSuO|g5QSEQvF2= M1W4ZXNCVkeHUh?=
CA46 NUPIV4Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF3LkC1PFYh|ryP MYLTRW5ITVJ?
IST-SL2 MlfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHifmdKSzVyPUG1MlE6ODFizszN NFLtSYRUSU6JRWK=
BC-1 NXPuRXhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1myfGlEPTB;MUWuN|MyPCEQvF2= MmXtV2FPT0WU
LS-123 MkG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF3LkixO|Mh|ryP NXHt[I13W0GQR1XS
Ramos-2G6-4C10 NUXL[WJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojMTWM2OD1zNj6wPVI1KM7:TR?= M1;hPXNCVkeHUh?=
MZ1-PC NGiwOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXSNXhXUUN3ME2xOk44OzF|IN88US=> MYfTRW5ITVJ?
LB647-SCLC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTF4LkmzO|Ih|ryP M{jabXNCVkeHUh?=
NCI-H1694 NX;VR5lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF5LkG1Nlkh|ryP NIf1ZnFUSU6JRWK=
NCI-H322M NFfadYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\MfHJbUUN3ME2xO{41OzZ4IN88US=> NY\EO5ZqW0GQR1XS
ES7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF6LkO5NVQh|ryP MV3TRW5ITVJ?
LC-2-ad Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq0XIhKSzVyPUG4MlQ{QDZizszN NE\SeWZUSU6JRWK=
SF268 NIPVNZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF6Lke0NFkh|ryP Mk\MV2FPT0WU
RPMI-8402 MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr4TJVzUUN3ME2xPU4xPzR{IN88US=> MVfTRW5ITVJ?
HCE-T Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnCUIQxUUN3ME2yNE4zOzR2IN88US=> M1H4T3NCVkeHUh?=
A101D NFvLSnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXCfI5DUUN3ME2yNE45PTh5IN88US=> M{XKZXNCVkeHUh?=
MRK-nu-1 NFPvPHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLjTWM2OD1{MD65NVMh|ryP NU\rbpJ2W0GQR1XS
LXF-289 MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TKPWlEPTB;MkGuNFM5KM7:TR?= NXnrXGtvW0GQR1XS
NALM-6 NYS1eYJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnsTWM2OD1{MT6xPVY4KM7:TR?= M1K1e3NCVkeHUh?=
DOHH-2 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJzLkS4NVMh|ryP NXK3RoN3W0GQR1XS
EW-16 NGLvTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnFc2s3UUN3ME2yNk4yPDB{IN88US=> NH:5cVBUSU6JRWK=
A4-Fuk NVrrcHhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELPOYNKSzVyPUKyMlIyPDlizszN NHjJNoFUSU6JRWK=
HD-MY-Z MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\jWG1KSzVyPUKyMlM6PjVizszN NXjSdFg3W0GQR1XS
SKM-1 MmLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT4fnlKSzVyPUKyMlc{PTFizszN MX3TRW5ITVJ?
DMS-153 M1uw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf5OZFKSzVyPUKzMlQzODRizszN M3XoUnNCVkeHUh?=
LB373-MEL-D NIPuOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPWTWM2OD1{Mz61OFUzKM7:TR?= NXzEbYU{W0GQR1XS
LP-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLYT|BpUUN3ME2yN{45ODl5IN88US=> NVv3VpU2W0GQR1XS
GI-ME-N NHXk[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVja[FdMUUN3ME2yOE4zQTJizszN NEH6eHZUSU6JRWK=
MPP-89 MkjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHPTWM2OD1{NT6yNFM3KM7:TR?= MoHRV2FPT0WU
U-698-M Ml\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[0PWlEPTB;MkWuNlUxOyEQvF2= NVXOSmhkW0GQR1XS
HC-1 NHLvboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ3Lk[0NVgh|ryP NFPDUIVUSU6JRWK=
HCC2157 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\RbmlKSzVyPUK1MlY4OyEQvF2= M2PI[HNCVkeHUh?=
MOLT-4 M2G5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ4LkK3N{DPxE1? M1TDTHNCVkeHUh?=
LS-411N MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq3TWM2OD1{Nj6zN|Y6KM7:TR?= MkPRV2FPT0WU
Becker Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDrOWtNUUN3ME2yOk42OThzIN88US=> NVT2[lVTW0GQR1XS
NCI-H23 NF3IV25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ4Lke1O|Uh|ryP M1vWNXNCVkeHUh?=
IST-SL1 NGDndmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\DTWM2OD1{Nz6zPFY4KM7:TR?= NHj6RpdUSU6JRWK=
MZ2-MEL Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTTSpNKSzVyPUK3MlQ2PjZizszN M4TjfHNCVkeHUh?=
RKO NWDOdnNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH0RXhKSzVyPUK4MlE1PDZizszN NFrwXYZUSU6JRWK=
TE-441-T MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[5cmlEPTB;MkiuO|g6KM7:TR?= M1;HTnNCVkeHUh?=
EW-24 M4nBNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjrUGJKSzVyPUK5MlEzPTlizszN NWjveFBJW0GQR1XS
no-10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrETWM2OD1{OT6xOlMyKM7:TR?= M3HyfnNCVkeHUh?=
D-542MG MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTETWM2OD1{OT65NlIyKM7:TR?= NIHQZ2NUSU6JRWK=
ST486 M{fp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGKzfo1KSzVyPUOwMlY1PTFizszN NWrRSY1uW0GQR1XS
KURAMOCHI M3TKUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K3XGlEPTB;M{CuPFA2PyEQvF2= NFH0TnlUSU6JRWK=
ES8 M3fBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3QUWZKSzVyPUOxMlU6PzJizszN NH:2ZWtUSU6JRWK=
BL-41 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC4TWM2OD1|Mj6xNFU1KM7:TR?= NHj0SmdUSU6JRWK=
NB6 M1j5Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3qzUmlEPTB;M{KuN|g2PSEQvF2= Mke5V2FPT0WU
NCI-H1304 MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPBbGlYUUN3ME2zNk41QTZ5IN88US=> NVHkeIpbW0GQR1XS
MS-1 NYXOVopGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTN{Lke3OVEh|ryP MmLoV2FPT0WU
MFH-ino MkLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[zOIZRUUN3ME2zOE4{OjJ2IN88US=> M4n4SHNCVkeHUh?=
NOS-1 NG[zVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTN2Lk[3OFgh|ryP M13FV3NCVkeHUh?=
HUTU-80 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonUTWM2OD1|NT6zOlY4KM7:TR?= MWDTRW5ITVJ?
EB2 NWXyW|d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHCdVJKSzVyPUO2MlYyQDlizszN NHLXN5NUSU6JRWK=
L-540 NI\UfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSwUFQzUUN3ME2zO{4zOzB6IN88US=> MY\TRW5ITVJ?
NCI-H747 NI[4[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFywPW1KSzVyPUO4Mlg5PDZizszN NVHNTIhoW0GQR1XS
NCI-H446 NXSwUY1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\aWGlEPTB;M{muPVY2OSEQvF2= NIf6U4NUSU6JRWK=
MOLT-16 NYfK[2hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR{LkSxOUDPxE1? MkfxV2FPT0WU
BC-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PBcGlEPTB;NEWuOFg6PiEQvF2= NFnOTHFUSU6JRWK=
SJSA-1 M4npeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T1O2lEPTB;NEWuOVQ4PCEQvF2= NWXqe3Y1W0GQR1XS
BB65-RCC MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnqNnNoUUN3ME20OU43PjZizszN M1z5NXNCVkeHUh?=
SNB75 MkH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTR4LkCxPEDPxE1? MWTTRW5ITVJ?

... 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:[1]
+ Expand

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]
+ Expand
  • 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]
+ 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 Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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 (g) = Concentration (mol/L) × Volume (L) × 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
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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):
    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
NCT00107003 Completed Glioma|Brain Tumor|Glioblastoma Multiforme|GBM|Gliosarcoma|GS National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 30, 2005 Phase 2
NCT00251433 Active, not recruiting Neoplasms, Breast Novartis Pharmaceuticals|Novartis September 26, 2005 Phase 1
NCT01306045 Recruiting Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 21, 2011 Phase 2
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|Phase 2
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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID