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 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

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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 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMEK1OFQh|ryP MXjTRW5ITVJ?
HCC2218 MmmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCzNXlJUUN3ME2wMlA2OzJ4IN88US=> NX;YXo14W0GQR1XS
OCUB-M NVnWdFdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL6b5RKSzVyPUCuNFU4PCEQvF2= M1:2SnNCVkeHUh?=
ECC12 M4PI[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjTTWpFUUN3ME2wMlA6OjNzIN88US=> NFS3V3hUSU6JRWK=
DSH1 M2ixTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDMTWM2OD1yLkC5N|k3KM7:TR?= MmXXV2FPT0WU
BT-474 NG\DdXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwMkGzNVUh|ryP M3K1VnNCVkeHUh?=
BB30-HNC M4CwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwMkS2OVQh|ryP NVe2T21RW0GQR1XS
EKVX NWnaTlBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwNES4O|Qh|ryP MYDTRW5ITVJ?
TE-12 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwNEmwOVch|ryP NHvHfHFUSU6JRWK=
A388 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwN{KyOVgh|ryP M1SwcnNCVkeHUh?=
TE-9 MnHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwN{S0OVMh|ryP NWrlZ4Y1W0GQR1XS
LB2241-RCC M2LhUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr5TWM2OD1zLkG1OFA{KM7:TR?= NXvIUlU5W0GQR1XS
LB996-RCC MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLCTWM2OD1zLkO2NlI5KM7:TR?= NFftOWVUSU6JRWK=
LC-1F NV\QXWdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwM{iyOFQh|ryP Ml70V2FPT0WU
TE-6 NXPidHhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwNUWyNFEh|ryP NU\6Nm0yW0GQR1XS
A253 MoXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L3[WlEPTB;MT65O|M{PSEQvF2= NV:2ToZrW0GQR1XS
OS-RC-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwOUmxPVkh|ryP NGjzPXJUSU6JRWK=
TE-1 NInPT5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJwMES4N{DPxE1? MX\TRW5ITVJ?
RL95-2 NHLjZ5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vuPGlEPTB;Mz6xOVY4KM7:TR?= Mlu1V2FPT0WU
LS-513 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrNTWM2OD1|LkSwNFQyKM7:TR?= MVfTRW5ITVJ?
DJM-1 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XtUmlEPTB;Mz60Olk4PSEQvF2= MX7TRW5ITVJ?
NMC-G1 NV3yWm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rtRWlEPTB;Mz61OFUxOSEQvF2= M3nMfHNCVkeHUh?=
TE-10 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzZTWM2OD1|LkW1N|U3KM7:TR?= MnLHV2FPT0WU
TE-5 MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu5b5JKSzVyPUSuNFM4OyEQvF2= M3rpdHNCVkeHUh?=
TK10 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvNUXdUUUN3ME20MlE3PTJ{IN88US=> MoDMV2FPT0WU
UACC-812 NFi1NGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7Q[mJKSzVyPUSuOVYyPTNizszN MonvV2FPT0WU
SW962 NVPwZot2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPhS2V2UUN3ME21MlAzOTV7IN88US=> MV3TRW5ITVJ?
SW954 NVPnfIVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvn[5dKSzVyPUWuN|kzPDVizszN MkTPV2FPT0WU
COLO-668 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnuZ2VQUUN3ME21MlczPjZ5IN88US=> NIrlb4xUSU6JRWK=
LB1047-RCC MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXKb3FKSzVyPUWuPFAxPDZizszN MlvGV2FPT0WU
NB5 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHjTWM2OD14LkKxNFAyKM7:TR?= MkPrV2FPT0WU
NTERA-S-cl-D1 M4W4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XHSmlEPTB;Nj6yOlU3OSEQvF2= NEHJUpVUSU6JRWK=
IST-MEL1 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[wSWlEPTB;Nj60N|Y6PCEQvF2= NHLrZ2pUSU6JRWK=
GI-1 NILmO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\LbYZKSzVyPU[uOVE3QDJizszN NWj0NWZJW0GQR1XS
TGBC1TKB NYnVU3lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzUUWNKSzVyPUeuNFcyQDNizszN M4DFfXNCVkeHUh?=
GT3TKB M{jTbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTdwMkK3OFQh|ryP NUm5blVjW0GQR1XS
EVSA-T NXv3U4wzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HWfmlEPTB;Nz60NlgyOSEQvF2= NY\wWGdkW0GQR1XS
D-502MG MnHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z4eGlEPTB;Nz60PFg6PCEQvF2= NF\kSW9USU6JRWK=
TE-8 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTdwN{[xOVkh|ryP MYjTRW5ITVJ?
OVCAR-4 NUjnVlA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;STWM2OD17LkGxOlc2KM7:TR?= NWTUU|VKW0GQR1XS
D-336MG NHfPUndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEj6cZRKSzVyPUmuOFc{QTVizszN MX7TRW5ITVJ?
GCIY NVO2cY9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7GU4pKSzVyPUmuOVc1OiEQvF2= Mkn5V2FPT0WU
KS-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjZeFhZUUN3ME25MlY3Ojh5IN88US=> MXTTRW5ITVJ?
HCC2998 NHPBW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLtTWM2OD17Lkm2N|A4KM7:TR?= NYrNSmV{W0GQR1XS
D-247MG NFnn[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSzRmUzUUN3ME25Mlk5OjlzIN88US=> NWrGfoNuW0GQR1XS
TE-15 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL4dJhKSzVyPUGwMlI1PSEQvF2= MorwV2FPT0WU
IST-MES1 M1W4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\J[2lEPTB;MUCuNlU3PSEQvF2= NYfYUVVOW0GQR1XS
ETK-1 MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvlU2JKSzVyPUGwMlYzOyEQvF2= MmTiV2FPT0WU
RCC10RGB NVeyclEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfPTWM2OD1zMD65OlEh|ryP NYj4cJlyW0GQR1XS
KNS-42 M2TyTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnufnJKSzVyPUGxMlczPTVizszN NEWwfnJUSU6JRWK=
LB771-HNC NHW4O|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnwVVdKSzVyPUGyMlE4OTJizszN NIPZNmFUSU6JRWK=
SR MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDW[2lyUUN3ME2xNk4zODZ2IN88US=> MULTRW5ITVJ?
NCI-H1355 NFnCR3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXvTWM2OD1zMj64PVg2KM7:TR?= MWjTRW5ITVJ?
ES6 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvDWppYUUN3ME2xN{4xPzhizszN MW\TRW5ITVJ?
SK-NEP-1 NHP2eHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXa[lYxUUN3ME2xN{4zPTd5IN88US=> M2X6c3NCVkeHUh?=
D-392MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv5d|VKSzVyPUGzMlY1OjhizszN NHvlUnhUSU6JRWK=
NB7 M{Gw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILseopKSzVyPUG0MlI{PzRizszN MXrTRW5ITVJ?
SK-LMS-1 NX;2dId[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXyelY4UUN3ME2xOE42OTR3IN88US=> Ml;WV2FPT0WU
SK-UT-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXGTWM2OD1zND63PFg6KM7:TR?= NIP4O4xUSU6JRWK=
CA46 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInSXYpKSzVyPUG1MlA2QDZizszN MX7TRW5ITVJ?
IST-SL2 NXHNO|FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrHTWM2OD1zNT6xPVAyKM7:TR?= NEXXeGZUSU6JRWK=
BC-1 NYn6WGdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\TUmtIUUN3ME2xOU4{OzF2IN88US=> MXTTRW5ITVJ?
LS-123 Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvYNINOUUN3ME2xOU45OTd|IN88US=> M2TicXNCVkeHUh?=
Ramos-2G6-4C10 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF4LkC5NlQh|ryP NUTzbIJ1W0GQR1XS
MZ1-PC NELnXHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF4LkezNVMh|ryP MVfTRW5ITVJ?
LB647-SCLC MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[3PJJKSzVyPUG2Mlk{PzJizszN M4HhZXNCVkeHUh?=
NCI-H1694 NYK5TY45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\wTWM2OD1zNz6xOVI6KM7:TR?= M2T1UnNCVkeHUh?=
NCI-H322M NEDWUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqxWGhKSzVyPUG3MlQ{PjZizszN NIHhcG5USU6JRWK=
ES7 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33zcmlEPTB;MUiuN|kyPCEQvF2= NXfCTplbW0GQR1XS
LC-2-ad MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj5TWM2OD1zOD60N|g3KM7:TR?= MX;TRW5ITVJ?
SF268 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G4[WlEPTB;MUiuO|QxQSEQvF2= NUnQdm1NW0GQR1XS
RPMI-8402 M2frT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF7LkC3OFIh|ryP NEH0flJUSU6JRWK=
HCE-T NHzPWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX36VpdMUUN3ME2yNE4zOzR2IN88US=> MVHTRW5ITVJ?
A101D NHHZeYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTqT4FZUUN3ME2yNE45PTh5IN88US=> M4jmTnNCVkeHUh?=
MRK-nu-1 NG\PN3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XwUWlEPTB;MkCuPVE{KM7:TR?= MmroV2FPT0WU
LXF-289 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTzSpgzUUN3ME2yNU4xOzhizszN NGfubo9USU6JRWK=
NALM-6 NHXJOoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[5Z2lEPTB;MkGuNVk3PyEQvF2= NELab3JUSU6JRWK=
DOHH-2 NGjkZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnRZmh5UUN3ME2yNU41QDF|IN88US=> NY\hcJlJW0GQR1XS
EW-16 NV3sfmcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jiNGlEPTB;MkKuNVQxOiEQvF2= MlvOV2FPT0WU
A4-Fuk NXjFNGlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;Bc3BKSzVyPUKyMlIyPDlizszN MWLTRW5ITVJ?
HD-MY-Z Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTrWVZ2UUN3ME2yNk4{QTZ3IN88US=> Mk\GV2FPT0WU
SKM-1 NHT1[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3jRm9KSzVyPUKyMlc{PTFizszN Mly0V2FPT0WU
DMS-153 Mn7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPJTWM2OD1{Mz60NlA1KM7:TR?= NXzSeYxXW0GQR1XS
LB373-MEL-D M2DoeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS2TWM2OD1{Mz61OFUzKM7:TR?= M2HSeXNCVkeHUh?=
LP-1 M4TWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVizOnBLUUN3ME2yN{45ODl5IN88US=> M{TifXNCVkeHUh?=
GI-ME-N MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzmU2lkUUN3ME2yOE4zQTJizszN MlHMV2FPT0WU
MPP-89 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPQd5VFUUN3ME2yOU4zODN4IN88US=> NILEe5JUSU6JRWK=
U-698-M MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ3LkK1NFMh|ryP MV7TRW5ITVJ?
HC-1 NWPMRnMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3ZTWM2OD1{NT62OFE5KM7:TR?= M2H4SXNCVkeHUh?=
HCC2157 MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HOeWlEPTB;MkWuOlc{KM7:TR?= MnzwV2FPT0WU
MOLT-4 NYrCUos6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3q[nVuUUN3ME2yOk4zPzNizszN MmnYV2FPT0WU
LS-411N NVXGb4VMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDqTWM2OD1{Nj6zN|Y6KM7:TR?= NFvGUIVUSU6JRWK=
Becker MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFXWprUUN3ME2yOk42OThzIN88US=> MV\TRW5ITVJ?
NCI-H23 MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfydndMUUN3ME2yOk44PTd3IN88US=> NVjOW3NJW0GQR1XS
IST-SL1 MkfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vXfmlEPTB;MkeuN|g3PyEQvF2= NHvlRnNUSU6JRWK=
MZ2-MEL NXqzeFZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3uyNWlEPTB;MkeuOFU3PiEQvF2= M3vrdHNCVkeHUh?=
RKO M2fCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrvOY9KSzVyPUK4MlE1PDZizszN NXfLU5d2W0GQR1XS
TE-441-T NYfaWY1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:wVmVKSzVyPUK4Mlc5QSEQvF2= NYPiWGo1W0GQR1XS
EW-24 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi5eZNxUUN3ME2yPU4yOjV7IN88US=> MW\TRW5ITVJ?
no-10 NFnHW3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ7LkG2N|Eh|ryP NHXWNnhUSU6JRWK=
D-542MG NHPXNGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PYc2lEPTB;MkmuPVIzOSEQvF2= MoLlV2FPT0WU
ST486 M3XWeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGq3dmRKSzVyPUOwMlY1PTFizszN M2focHNCVkeHUh?=
KURAMOCHI MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTNyLkiwOVch|ryP Mo\OV2FPT0WU
ES8 MnH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;ISHZtUUN3ME2zNU42QTd{IN88US=> NEX5N5VUSU6JRWK=
BL-41 NHvF[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPjOphZUUN3ME2zNk4yODV2IN88US=> NHXqU49USU6JRWK=
NB6 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILqUZFKSzVyPUOyMlM5PTVizszN NIXye41USU6JRWK=
NCI-H1304 M3fuOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnyTWM2OD1|Mj60PVY4KM7:TR?= MYTTRW5ITVJ?
MS-1 NX\mRXBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDaTWM2OD1|Mj63O|UyKM7:TR?= MmTHV2FPT0WU
MFH-ino MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN2LkOyNlQh|ryP MYTTRW5ITVJ?
NOS-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHxfFc{UUN3ME2zOE43PzR6IN88US=> Mli2V2FPT0WU
HUTU-80 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN3LkO2Olch|ryP NF;jeJBUSU6JRWK=
EB2 MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jrNmlEPTB;M{[uOlE5QSEQvF2= M1HLb3NCVkeHUh?=
L-540 NEHnW2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7QRmpKSzVyPUO3MlI{ODhizszN MVvTRW5ITVJ?
NCI-H747 M1HiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;LWnRUUUN3ME2zPE45QDR4IN88US=> NI\sbHZUSU6JRWK=
NCI-H446 MofOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGxTWM2OD1|OT65OlUyKM7:TR?= Ml3UV2FPT0WU
MOLT-16 NFrvZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTR{LkSxOUDPxE1? NGDBd4RUSU6JRWK=
BC-3 M4X5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjPTWM2OD12NT60PFk3KM7:TR?= NH\QcZFUSU6JRWK=
SJSA-1 NWDpd5ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvT3dKSzVyPUS1MlU1PzRizszN MkHEV2FPT0WU
BB65-RCC NFnBeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR3Lk[2OkDPxE1? M{joWHNCVkeHUh?=
SNB75 NXLQc5E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{noZWlEPTB;NE[uNFE5KM7:TR?= MkTSV2FPT0WU

... 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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* 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