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 NXnCeVRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PoT2lEPTB;MD6wNlU1PCEQvF2= MnWwV2FPT0WU
HCC2218 MoLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Hn[WlEPTB;MD6wOVMzPiEQvF2= M2WzWXNCVkeHUh?=
OCUB-M MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;nUmlEPTB;MD6wOVc1KM7:TR?= Mn3qV2FPT0WU
ECC12 MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj1TWM2OD1yLkC5NlMyKM7:TR?= MYXTRW5ITVJ?
DSH1 M2XneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Kx[mlEPTB;MD6wPVM6PiEQvF2= M4\MUXNCVkeHUh?=
BT-474 NFT1boFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHKSZBKSzVyPUCuNlE{OTVizszN NHvienNUSU6JRWK=
BB30-HNC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwMkS2OVQh|ryP MVLTRW5ITVJ?
EKVX NEnvcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwNES4O|Qh|ryP MV7TRW5ITVJ?
TE-12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fFVWlEPTB;MD60PVA2PyEQvF2= M3fnUXNCVkeHUh?=
A388 NGHjXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XNe2lEPTB;MD63NlI2QCEQvF2= MmnWV2FPT0WU
TE-9 M2LzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwN{S0OVMh|ryP M1jJZ3NCVkeHUh?=
LB2241-RCC Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwMUW0NFMh|ryP MV7TRW5ITVJ?
LB996-RCC NXn4[Il2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrYfVZKSzVyPUGuN|YzOjhizszN MmnNV2FPT0WU
LC-1F M4rOfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHadnNsUUN3ME2xMlM5OjR2IN88US=> M1fnSXNCVkeHUh?=
TE-6 NFy0dHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX0TWM2OD1zLkW1NlAyKM7:TR?= NWTnUGR6W0GQR1XS
A253 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTtTWM2OD1zLkm3N|M2KM7:TR?= NFT3[2ZUSU6JRWK=
OS-RC-2 NY\BTGRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwOUmxPVkh|ryP MXHTRW5ITVJ?
TE-1 NFTxS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13ifGlEPTB;Mj6wOFg{KM7:TR?= NX;H[4RjW0GQR1XS
RL95-2 NIHKXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNwMUW2O{DPxE1? MnPoV2FPT0WU
LS-513 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HsW2lEPTB;Mz60NFA1OSEQvF2= NFj5OJlUSU6JRWK=
DJM-1 MoTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTNwNE[5O|Uh|ryP MnjKV2FPT0WU
NMC-G1 NEfy[3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fhPWlEPTB;Mz61OFUxOSEQvF2= MluwV2FPT0WU
TE-10 MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrFTWM2OD1|LkW1N|U3KM7:TR?= NGHLSYhUSU6JRWK=
TE-5 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fURmlEPTB;ND6wN|c{KM7:TR?= NXrPXY5WW0GQR1XS
TK10 NFXJbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHK4b5hKSzVyPUSuNVY2OjJizszN NVHHc3lGW0GQR1XS
UACC-812 NYrGPG54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfmTWM2OD12LkW2NVU{KM7:TR?= M2La[nNCVkeHUh?=
SW962 MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnSeVNFUUN3ME21MlAzOTV7IN88US=> MlOwV2FPT0WU
SW954 M3L1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvqTWM2OD13LkO5NlQ2KM7:TR?= M3;TUnNCVkeHUh?=
COLO-668 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnhTWM2OD13LkeyOlY4KM7:TR?= NFn5bJlUSU6JRWK=
LB1047-RCC M4HjN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[0ZWlEPTB;NT64NFA1PiEQvF2= NIjlfFRUSU6JRWK=
NB5 NGP1OZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1y2ZWlEPTB;Nj6yNVAxOSEQvF2= NHXpNYVUSU6JRWK=
NTERA-S-cl-D1 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jx[mlEPTB;Nj6yOlU3OSEQvF2= NETON21USU6JRWK=
IST-MEL1 M{\GN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULhd|lGUUN3ME22MlQ{Pjl2IN88US=> NVm4OWJVW0GQR1XS
GI-1 NYns[mN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLMc5ZoUUN3ME22MlUyPjh{IN88US=> NInMNIdUSU6JRWK=
TGBC1TKB NXL6O2wzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v0OmlEPTB;Nz6wO|E5OyEQvF2= Mmj3V2FPT0WU
GT3TKB NU\QZVlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjsTWM2OD15LkKyO|Q1KM7:TR?= Ml7uV2FPT0WU
EVSA-T Mn\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jsfmlEPTB;Nz60NlgyOSEQvF2= M4njenNCVkeHUh?=
D-502MG NHm3OVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7zXmpKSzVyPUeuOFg5QTRizszN M4DROnNCVkeHUh?=
TE-8 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXoPIhmUUN3ME23Mlc3OTV7IN88US=> NEDiWVhUSU6JRWK=
OVCAR-4 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j0bWlEPTB;OT6xNVY4PSEQvF2= M{\tdnNCVkeHUh?=
D-336MG NHTXPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\qTWM2OD17LkS3N|k2KM7:TR?= Ml3wV2FPT0WU
GCIY MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXnSFhKSzVyPUmuOVc1OiEQvF2= M1vjUHNCVkeHUh?=
KS-1 NHHuT4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLSc3lNUUN3ME25MlY3Ojh5IN88US=> NXfTfllIW0GQR1XS
HCC2998 NUTtTmJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjmV21KSzVyPUmuPVY{ODdizszN M3yyWXNCVkeHUh?=
D-247MG MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLNTWM2OD17Lkm4NlkyKM7:TR?= MULTRW5ITVJ?
TE-15 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnlTWM2OD1zMD6yOFUh|ryP NGLENWZUSU6JRWK=
IST-MES1 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFyLkK1OlUh|ryP NVXGO4RtW0GQR1XS
ETK-1 NITCeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLxTWM2OD1zMD62NlMh|ryP MlP4V2FPT0WU
RCC10RGB M{fjUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm2XnZ4UUN3ME2xNE46PjFizszN MUTTRW5ITVJ?
KNS-42 MknmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vscmlEPTB;MUGuO|I2PSEQvF2= MnTlV2FPT0WU
LB771-HNC NEC5eGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPLUHpmUUN3ME2xNk4yPzF{IN88US=> NEfhZ4RUSU6JRWK=
SR NUS2d29mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nycWlEPTB;MUKuNlA3PCEQvF2= MoTIV2FPT0WU
NCI-H1355 M3r4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTa[41KSzVyPUGyMlg6QDVizszN MVLTRW5ITVJ?
ES6 NFXZPGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rpTWlEPTB;MUOuNFc5KM7:TR?= Mn;qV2FPT0WU
SK-NEP-1 NY\I[4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO4THNKSzVyPUGzMlI2PzdizszN NIfoWXhUSU6JRWK=
D-392MG NIPEN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPkdY1NUUN3ME2xN{43PDJ6IN88US=> M37pc3NCVkeHUh?=
NB7 NF7YPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnviTWM2OD1zND6yN|c1KM7:TR?= NWrXVZRuW0GQR1XS
SK-LMS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D3XmlEPTB;MUSuOVE1PSEQvF2= MXjTRW5ITVJ?
SK-UT-1 MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF2Lke4PFkh|ryP MmHBV2FPT0WU
CA46 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHycpY3UUN3ME2xOU4xPTh4IN88US=> MojNV2FPT0WU
IST-SL2 NEnXcVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3SxXmlEPTB;MUWuNVkxOSEQvF2= NIXLS5dUSU6JRWK=
BC-1 M4C0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECyTpVKSzVyPUG1MlM{OTRizszN MkPmV2FPT0WU
LS-123 Mlz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF3LkixO|Mh|ryP M160[3NCVkeHUh?=
Ramos-2G6-4C10 MnfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF4LkC5NlQh|ryP NIfvUVlUSU6JRWK=
MZ1-PC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPkTWM2OD1zNj63N|E{KM7:TR?= M1K0fnNCVkeHUh?=
LB647-SCLC NEnCcm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF4LkmzO|Ih|ryP M3rPU3NCVkeHUh?=
NCI-H1694 M33kZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF5LkG1Nlkh|ryP MkOxV2FPT0WU
NCI-H322M M2THN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HHbGlEPTB;MUeuOFM3PiEQvF2= M3jJ[XNCVkeHUh?=
ES7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;xcGxKSzVyPUG4MlM6OTRizszN NGjROYdUSU6JRWK=
LC-2-ad NHXGeZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HoNGlEPTB;MUiuOFM5PiEQvF2= MYHTRW5ITVJ?
SF268 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz5TWM2OD1zOD63OFA6KM7:TR?= NVXZfWp7W0GQR1XS
RPMI-8402 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTF7LkC3OFIh|ryP M3XDUnNCVkeHUh?=
HCE-T MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJyLkKzOFQh|ryP NHvVZlFUSU6JRWK=
A101D MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXXOng5UUN3ME2yNE45PTh5IN88US=> MmjUV2FPT0WU
MRK-nu-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3ld4FKSzVyPUKwMlkyOyEQvF2= MYjTRW5ITVJ?
LXF-289 M{PWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJzLkCzPEDPxE1? NUfENodIW0GQR1XS
NALM-6 NVnYboJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonsTWM2OD1{MT6xPVY4KM7:TR?= NV\Bd5ozW0GQR1XS
DOHH-2 NWPlbI9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X5PGlEPTB;MkGuOFgyOyEQvF2= MVrTRW5ITVJ?
EW-16 NX\vW2M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rKcWlEPTB;MkKuNVQxOiEQvF2= M3K1c3NCVkeHUh?=
A4-Fuk MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTJ{LkKxOFkh|ryP M4jI[nNCVkeHUh?=
HD-MY-Z MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXrTJNKSzVyPUKyMlM6PjVizszN MUDTRW5ITVJ?
SKM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ{LkezOVEh|ryP NXjNR3BrW0GQR1XS
DMS-153 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ|LkSyNFQh|ryP MkTiV2FPT0WU
LB373-MEL-D NXj5bGZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XvR2lEPTB;MkOuOVQ2OiEQvF2= M1S4SnNCVkeHUh?=
LP-1 M2rZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ|LkiwPVch|ryP MkL0V2FPT0WU
GI-ME-N MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH1SHBtUUN3ME2yOE4zQTJizszN M2LNc3NCVkeHUh?=
MPP-89 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUW1SlRkUUN3ME2yOU4zODN4IN88US=> NHzYcnZUSU6JRWK=
U-698-M NEPzOY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLaTWM2OD1{NT6yOVA{KM7:TR?= M1vDUnNCVkeHUh?=
HC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e4VmlEPTB;MkWuOlQyQCEQvF2= MWnTRW5ITVJ?
HCC2157 M4nQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KxWGlEPTB;MkWuOlc{KM7:TR?= MWXTRW5ITVJ?
MOLT-4 Mn6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPvOnc{UUN3ME2yOk4zPzNizszN MUfTRW5ITVJ?
LS-411N MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnZXm5IUUN3ME2yOk4{OzZ7IN88US=> M2TPXXNCVkeHUh?=
Becker NGPrXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K4[GlEPTB;Mk[uOVE5OSEQvF2= NGGwV|lUSU6JRWK=
NCI-H23 NGn2UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\pNZlKSzVyPUK2Mlc2PzVizszN MYHTRW5ITVJ?
IST-SL1 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXXZWJ5UUN3ME2yO{4{QDZ5IN88US=> MkHSV2FPT0WU
MZ2-MEL NE\kOoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnRTWM2OD1{Nz60OVY3KM7:TR?= NF3XWoFUSU6JRWK=
RKO MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjRTWRZUUN3ME2yPE4yPDR4IN88US=> NHvodYNUSU6JRWK=
TE-441-T M4iwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG3[Jd[UUN3ME2yPE44QDlizszN NEHQUmFUSU6JRWK=
EW-24 M{LNTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJ7LkGyOVkh|ryP NX7NVoFbW0GQR1XS
no-10 M4HwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTFTWM2OD1{OT6xOlMyKM7:TR?= NXLMNIxHW0GQR1XS
D-542MG NFe3e5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJ7LkmyNlEh|ryP MYnTRW5ITVJ?
ST486 NE\JOoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rmTGlEPTB;M{CuOlQ2OSEQvF2= NUnnZYN6W0GQR1XS
KURAMOCHI NHXqbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;oVIlpUUN3ME2zNE45ODV5IN88US=> MlTTV2FPT0WU
ES8 MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHETWM2OD1|MT61PVczKM7:TR?= NHjhfpBUSU6JRWK=
BL-41 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrXfmUyUUN3ME2zNk4yODV2IN88US=> NI\RcJFUSU6JRWK=
NB6 M1O4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLvSXo2UUN3ME2zNk4{QDV3IN88US=> MXvTRW5ITVJ?
NCI-H1304 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\mTWM2OD1|Mj60PVY4KM7:TR?= MoKwV2FPT0WU
MS-1 M{LQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTN{Lke3OVEh|ryP NXjBfHNRW0GQR1XS
MFH-ino NEGxdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTN2LkOyNlQh|ryP MVnTRW5ITVJ?
NOS-1 M3uzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTJTWM2OD1|ND62O|Q5KM7:TR?= MnfuV2FPT0WU
HUTU-80 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjwWYV2UUN3ME2zOU4{PjZ5IN88US=> MWnTRW5ITVJ?
EB2 NXrsSmZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fG[2lEPTB;M{[uOlE5QSEQvF2= M4HH[HNCVkeHUh?=
L-540 NH3vXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrZU5BnUUN3ME2zO{4zOzB6IN88US=> MlPCV2FPT0WU
NCI-H747 NGPsOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LvUmlEPTB;M{iuPFg1PiEQvF2= NFixfpFUSU6JRWK=
NCI-H446 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID3cGpKSzVyPUO5Mlk3PTFizszN MmD6V2FPT0WU
MOLT-16 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXVOmNuUUN3ME20Nk41OTVizszN MlvYV2FPT0WU
BC-3 NYnIc5I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nhZWlEPTB;NEWuOFg6PiEQvF2= NGXqdHZUSU6JRWK=
SJSA-1 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfXcVhKSzVyPUS1MlU1PzRizszN Mk\1V2FPT0WU
BB65-RCC MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrTWYZKSzVyPUS1MlY3PiEQvF2= M1:yOnNCVkeHUh?=
SNB75 NHHZOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES3e4RKSzVyPUS2MlAyQCEQvF2= NV\x[mE3W0GQR1XS

... 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 <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)

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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
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* 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID