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.
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 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMEK1OFQh|ryP M4DU[XNCVkeHUh?=
HCC2218 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMEWzNlYh|ryP NGrWNndUSU6JRWK=
OCUB-M MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLyTVc2UUN3ME2wMlA2PzRizszN MmrVV2FPT0WU
ECC12 MlXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPh[3Q5UUN3ME2wMlA6OjNzIN88US=> M4jNcXNCVkeHUh?=
DSH1 M1izW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvId49KSzVyPUCuNFk{QTZizszN M1zQU3NCVkeHUh?=
BT-474 MmD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVza[4JLUUN3ME2wMlIyOzF3IN88US=> NWnaW2RTW0GQR1XS
EKVX NFPD[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\CUpdrUUN3ME2wMlQ1QDd2IN88US=> M3vrNnNCVkeHUh?=
TE-12 Ml25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy3d|BKSzVyPUCuOFkxPTdizszN NVzYXI8yW0GQR1XS
A388 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvsXYdKSzVyPUCuO|IzPThizszN NEL5[JBUSU6JRWK=
TE-9 M2jzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL1TWM2OD1yLke0OFU{KM7:TR?= M{K1VnNCVkeHUh?=
LB996-RCC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3noWmlEPTB;MT6zOlIzQCEQvF2= M3m5N3NCVkeHUh?=
LC-1F NVP1NYpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;wNXpsUUN3ME2xMlM5OjR2IN88US=> M2nBOXNCVkeHUh?=
A253 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwOUezN|Uh|ryP MmD2V2FPT0WU
OS-RC-2 NH62fodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nMR2lEPTB;MT65PVE6QSEQvF2= NXzIcFBuW0GQR1XS
TE-1 M2WzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DLR2lEPTB;Mj6wOFg{KM7:TR?= MnHhV2FPT0WU
RL95-2 M3nQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HHNWlEPTB;Mz6xOVY4KM7:TR?= MkjiV2FPT0WU
LS-513 M2LsNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq2T|d3UUN3ME2zMlQxODRzIN88US=> NWraTJU{W0GQR1XS
DJM-1 M4ntPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPPdVlKSzVyPUOuOFY6PzVizszN Mny0V2FPT0WU
NMC-G1 NHfWdmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUP4S|F[UUN3ME2zMlU1PTBzIN88US=> NHHhcmRUSU6JRWK=
TE-5 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTYdphKSzVyPUSuNFM4OyEQvF2= M1fDbHNCVkeHUh?=
SW962 M{fvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDSTWM2OD13LkCyNVU6KM7:TR?= NVq5NIpkW0GQR1XS
SW954 MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfX[mpIUUN3ME21MlM6OjR3IN88US=> NFGxbndUSU6JRWK=
COLO-668 Ml;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX36VJF1UUN3ME21MlczPjZ5IN88US=> NIH6UGRUSU6JRWK=
NB5 M3f3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTZwMkGwNFEh|ryP M1\SWHNCVkeHUh?=
NTERA-S-cl-D1 M1u1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFf5RZhKSzVyPU[uNlY2PjFizszN MoqyV2FPT0WU
IST-MEL1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnoSo5KSzVyPU[uOFM3QTRizszN NWDYXol1W0GQR1XS
GI-1 NGnE[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTZwNUG2PFIh|ryP M2nCZXNCVkeHUh?=
TGBC1TKB NEfUO4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTdwMEexPFMh|ryP MnnrV2FPT0WU
D-502MG M2XTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jDSmlEPTB;Nz60PFg6PCEQvF2= NISzdpdUSU6JRWK=
TE-8 NFzPW5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTCd5B6UUN3ME23Mlc3OTV7IN88US=> MnjRV2FPT0WU
D-336MG MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Oz[2lEPTB;OT60O|M6PSEQvF2= MnLHV2FPT0WU
GCIY NEDNcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\yfGFWUUN3ME25MlU4PDJizszN M{n0NXNCVkeHUh?=
KS-1 NXO1Sng2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTlwNk[yPFch|ryP NX\iSZFnW0GQR1XS
HCC2998 MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTlwOU[zNFch|ryP NFL3UJFUSU6JRWK=
D-247MG M{OzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTlwOUiyPVEh|ryP NG\GUGVUSU6JRWK=
TE-15 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n6UWlEPTB;MUCuNlQ2KM7:TR?= NFzqTFVUSU6JRWK=
ETK-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LHWmlEPTB;MUCuOlI{KM7:TR?= MkLpV2FPT0WU
RCC10RGB M3vpbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnnTWM2OD1zMD65OlEh|ryP NEjuNYtUSU6JRWK=
KNS-42 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFzLkeyOVUh|ryP Ml;yV2FPT0WU
LB771-HNC NF3CWFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDvTWM2OD1zMj6xO|EzKM7:TR?= MnTKV2FPT0WU
SR NYnzOWJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLNOlBKSzVyPUGyMlIxPjRizszN M1\rfnNCVkeHUh?=
NCI-H1355 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfkUnprUUN3ME2xNk45QTh3IN88US=> MlvxV2FPT0WU
ES6 M2H6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PpW2lEPTB;MUOuNFc5KM7:TR?= NWXEeGZ2W0GQR1XS
SK-NEP-1 NFrNdVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTF|LkK1O|ch|ryP MkT1V2FPT0WU
D-392MG NFu0TVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z4RWlEPTB;MUOuOlQzQCEQvF2= NIX0N5lUSU6JRWK=
NB7 MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHBTWM2OD1zND6yN|c1KM7:TR?= MnfzV2FPT0WU
SK-LMS-1 M1j2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmeyTWM2OD1zND61NVQ2KM7:TR?= M2jmcHNCVkeHUh?=
SK-UT-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zsSWlEPTB;MUSuO|g5QSEQvF2= Ml3TV2FPT0WU
CA46 NWLmc3d3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPVTWM2OD1zNT6wOVg3KM7:TR?= NFq3dVFUSU6JRWK=
BC-1 NHjnem1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jLUmlEPTB;MUWuN|MyPCEQvF2= MVLTRW5ITVJ?
LS-123 M1fKUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjiN5hKSzVyPUG1MlgyPzNizszN MoTJV2FPT0WU
Ramos-2G6-4C10 MoWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYC2W3E2UUN3ME2xOk4xQTJ2IN88US=> NUSyVmJjW0GQR1XS
MZ1-PC NW\RdohET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37a[WlEPTB;MU[uO|MyOyEQvF2= M3y0VXNCVkeHUh?=
NCI-H1694 NH3yfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnYPWprUUN3ME2xO{4yPTJ7IN88US=> M4fBZnNCVkeHUh?=
NCI-H322M M1T5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3CdYpKSzVyPUG3MlQ{PjZizszN MkDTV2FPT0WU
ES7 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC2TWM2OD1zOD6zPVE1KM7:TR?= NX\xXno6W0GQR1XS
LC-2-ad NGXv[oRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF6LkSzPFYh|ryP M2m4ZnNCVkeHUh?=
SF268 M2[yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnsd5BmUUN3ME2xPE44PDB7IN88US=> NY\0OYU4W0GQR1XS
RPMI-8402 NUnYVpNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTF7LkC3OFIh|ryP MlrYV2FPT0WU
HCE-T M{\RPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LWW2lEPTB;MkCuNlM1PCEQvF2= M4nPTHNCVkeHUh?=
A101D M2LBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTJyLki1PFch|ryP M2TUTHNCVkeHUh?=
MRK-nu-1 M1SwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LVTWlEPTB;MkCuPVE{KM7:TR?= NFS0bpNUSU6JRWK=
DOHH-2 M2HE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULabotJUUN3ME2yNU41QDF|IN88US=> M2LaZ3NCVkeHUh?=
EW-16 NH3uO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJ{LkG0NFIh|ryP NWP6ZW1CW0GQR1XS
A4-Fuk NGXj[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJ{LkKxOFkh|ryP M2PkfXNCVkeHUh?=
SKM-1 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Xmb2lEPTB;MkKuO|M2OSEQvF2= MXTTRW5ITVJ?
LP-1 NGj0RVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDDc5dQUUN3ME2yN{45ODl5IN88US=> NVfNTph7W0GQR1XS
GI-ME-N NIfzOGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPjTWM2OD1{ND6yPVIh|ryP MW\TRW5ITVJ?
MPP-89 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n5fWlEPTB;MkWuNlA{PiEQvF2= M4XrfXNCVkeHUh?=
U-698-M MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfYPVRKSzVyPUK1MlI2ODNizszN NYnObmNXW0GQR1XS
HC-1 NEDQRphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rPdmlEPTB;MkWuOlQyQCEQvF2= NITzTpZUSU6JRWK=
HCC2157 MnXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG2TWM2OD1{NT62O|Mh|ryP MVnTRW5ITVJ?
MOLT-4 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH6UpVTUUN3ME2yOk4zPzNizszN MnnCV2FPT0WU
LS-411N MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVv2Sm5kUUN3ME2yOk4{OzZ7IN88US=> MVnTRW5ITVJ?
Becker NHL4SZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXkTWM2OD1{Nj61NVgyKM7:TR?= NUHLSoRNW0GQR1XS
NCI-H23 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDGTWM2OD1{Nj63OVc2KM7:TR?= MVfTRW5ITVJ?
IST-SL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TOO2lEPTB;MkeuN|g3PyEQvF2= NXXYeI5IW0GQR1XS
MZ2-MEL M4XHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnW4TWM2OD1{Nz60OVY3KM7:TR?= MlnJV2FPT0WU
RKO M2\Td2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\wXmQ2UUN3ME2yPE4yPDR4IN88US=> MUjTRW5ITVJ?
TE-441-T NYPHZ3RqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlThTWM2OD1{OD63PFkh|ryP NF;aZ|VUSU6JRWK=
EW-24 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG3e4xIUUN3ME2yPU4yOjV7IN88US=> M3r1OXNCVkeHUh?=
no-10 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXFTWM2OD1{OT6xOlMyKM7:TR?= MoPjV2FPT0WU
D-542MG NHfEc|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfqOWxKSzVyPUK5MlkzOjFizszN MUPTRW5ITVJ?
ST486 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXKTWM2OD1|MD62OFUyKM7:TR?= NEKyVolUSU6JRWK=
ES8 M2XNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTNzLkW5O|Ih|ryP NWC3XGRQW0GQR1XS
BL-41 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHjVYVrUUN3ME2zNk4yODV2IN88US=> M2\0d3NCVkeHUh?=
NCI-H1304 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TCPWlEPTB;M{KuOFk3PyEQvF2= Ml\JV2FPT0WU
MS-1 M{nEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7WTWM2OD1|Mj63O|UyKM7:TR?= NWXtSYc4W0GQR1XS
MFH-ino NGfKV2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT6TWM2OD1|ND6zNlI1KM7:TR?= NEj2WGdUSU6JRWK=
NOS-1 NF[xem9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXKwfVNZUUN3ME2zOE43PzR6IN88US=> M3KwUnNCVkeHUh?=
HUTU-80 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnOVW1KSzVyPUO1MlM3PjdizszN MUfTRW5ITVJ?
EB2 M2DGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWSxOY5QUUN3ME2zOk43OTh7IN88US=> NYTwV2FDW0GQR1XS
L-540 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKzTWM2OD1|Nz6yN|A5KM7:TR?= M{TrO3NCVkeHUh?=
NCI-H446 NHjKW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i1RWlEPTB;M{muPVY2OSEQvF2= MlO2V2FPT0WU
MOLT-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLrTWM2OD12Mj60NVUh|ryP M4XMenNCVkeHUh?=
SJSA-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrnT5lKSzVyPUS1MlU1PzRizszN MYfTRW5ITVJ?
SNB75 NHWxcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH6TWM2OD12Nj6wNVgh|ryP MnjqV2FPT0WU

... 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]


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:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 231277-92-2
Storage powder
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
    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

* 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.

  • * 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