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)
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 M{T0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O0UWlEPTB;MD6wNlU1PCEQvF2= MWnTRW5ITVJ?
HCC2218 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj2TWM2OD1yLkC1N|I3KM7:TR?= NIPBTJFUSU6JRWK=
OCUB-M MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHuNFZKSzVyPUCuNFU4PCEQvF2= MmLvV2FPT0WU
ECC12 M3nOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\ZSW9IUUN3ME2wMlA6OjNzIN88US=> Mn3MV2FPT0WU
DSH1 NFi3eYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7RVnNKSzVyPUCuNFk{QTZizszN NYW4fY06W0GQR1XS
BT-474 NHf4[lVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXXcW1KSzVyPUCuNlE{OTVizszN MXHTRW5ITVJ?
BB30-HNC NFvJOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TpW2lEPTB;MD6yOFY2PCEQvF2= MVnTRW5ITVJ?
EKVX MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmroTWM2OD1yLkS0PFc1KM7:TR?= M1fSS3NCVkeHUh?=
TE-12 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[wTWM2OD1yLkS5NFU4KM7:TR?= M{WwfnNCVkeHUh?=
A388 NITWfW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXNTWM2OD1yLkeyNlU5KM7:TR?= MX7TRW5ITVJ?
TE-9 M33CVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2mzfWlEPTB;MD63OFQ2OyEQvF2= NGeyd2dUSU6JRWK=
LB2241-RCC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFwMUW0NFMh|ryP NHfR[3lUSU6JRWK=
LB996-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjkWVRKSzVyPUGuN|YzOjhizszN M33UWXNCVkeHUh?=
LC-1F Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m4NWlEPTB;MT6zPFI1PCEQvF2= NUXmPYYzW0GQR1XS
TE-6 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnheGNKSzVyPUGuOVUzODFizszN M3vYPXNCVkeHUh?=
A253 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL1XWhDUUN3ME2xMlk4OzN3IN88US=> MWfTRW5ITVJ?
OS-RC-2 NUHSWlZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHHcIlQUUN3ME2xMlk6OTl7IN88US=> NFjhcWhUSU6JRWK=
TE-1 NFfLWWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLpTXFKSzVyPUKuNFQ5OyEQvF2= NHjrTHRUSU6JRWK=
RL95-2 NHj0[HhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHZZnlYUUN3ME2zMlE2PjdizszN NEHBO3JUSU6JRWK=
LS-513 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fNcmlEPTB;Mz60NFA1OSEQvF2= M1q0OnNCVkeHUh?=
DJM-1 MnXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTNwNE[5O|Uh|ryP MUnTRW5ITVJ?
NMC-G1 NWr4d3NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTNwNUS1NFEh|ryP NWm3O4dxW0GQR1XS
TE-10 NEXF[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfRbYVNUUN3ME2zMlU2OzV4IN88US=> NXrQcI4xW0GQR1XS
TE-5 MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTpco5KSzVyPUSuNFM4OyEQvF2= NF3VSIdUSU6JRWK=
TK10 NIDUfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTRwMU[1NlIh|ryP M{K1NXNCVkeHUh?=
UACC-812 NVn2ZYFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTRwNU[xOVMh|ryP M2qyV3NCVkeHUh?=
SW962 NXzNT4xKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmewTWM2OD13LkCyNVU6KM7:TR?= M{TWVnNCVkeHUh?=
SW954 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrBe4xKSzVyPUWuN|kzPDVizszN NX72ZmFtW0GQR1XS
COLO-668 NVuyb5JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTVwN{K2Olch|ryP NULSW|JqW0GQR1XS
LB1047-RCC NXXFUVFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Dx[WlEPTB;NT64NFA1PiEQvF2= NXPTTJR7W0GQR1XS
NB5 M3;0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTyRXE5UUN3ME22MlIyODBzIN88US=> MUjTRW5ITVJ?
NTERA-S-cl-D1 M3:0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTZwMk[1OlEh|ryP NY\KTlVyW0GQR1XS
IST-MEL1 Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTQTJJKSzVyPU[uOFM3QTRizszN MXrTRW5ITVJ?
GI-1 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;2UGlEPTB;Nj61NVY5OiEQvF2= M{HXO3NCVkeHUh?=
TGBC1TKB M3;6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTdwMEexPFMh|ryP NFy3e5ZUSU6JRWK=
GT3TKB Ml\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTdwMkK3OFQh|ryP MYDTRW5ITVJ?
EVSA-T M3LqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFSx[nNKSzVyPUeuOFI5OTFizszN MX;TRW5ITVJ?
D-502MG NF\uPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDiRVNKSzVyPUeuOFg5QTRizszN MX;TRW5ITVJ?
TE-8 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljVTWM2OD15Lke2NVU6KM7:TR?= M3KycHNCVkeHUh?=
OVCAR-4 NYDpZ5RNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPtTWM2OD17LkGxOlc2KM7:TR?= NY\2NY4{W0GQR1XS
D-336MG MljXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTlwNEezPVUh|ryP NVXYPWhSW0GQR1XS
GCIY NXfy[FlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD3TWM2OD17LkW3OFIh|ryP MV;TRW5ITVJ?
KS-1 NYrDVmJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4i5[WlEPTB;OT62OlI5PyEQvF2= M1\jTnNCVkeHUh?=
HCC2998 M4L2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\tTWM2OD17Lkm2N|A4KM7:TR?= NVnUWo9YW0GQR1XS
D-247MG M{PQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\rTWM2OD17Lkm4NlkyKM7:TR?= NGTCR3dUSU6JRWK=
TE-15 NX7rdoJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTFTWM2OD1zMD6yOFUh|ryP NYjLZm1CW0GQR1XS
IST-MES1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr2e3VKSzVyPUGwMlI2PjVizszN MmHFV2FPT0WU
ETK-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVuwfW1lUUN3ME2xNE43OjNizszN NUHvN|ZoW0GQR1XS
RCC10RGB MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFyLkm2NUDPxE1? NFLCWJlUSU6JRWK=
KNS-42 NVnWb3d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv5WJlKSzVyPUGxMlczPTVizszN NYnESW1rW0GQR1XS
LB771-HNC Mk\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33PT2lEPTB;MUKuNVcyOiEQvF2= MnXBV2FPT0WU
SR NYm3ZpNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfBUWtLUUN3ME2xNk4zODZ2IN88US=> MmPVV2FPT0WU
NCI-H1355 MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37tVWlEPTB;MUKuPFk5PSEQvF2= NVPNO2k4W0GQR1XS
ES6 M17YNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHPUmlqUUN3ME2xN{4xPzhizszN Mm\aV2FPT0WU
SK-NEP-1 MofuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj6T25EUUN3ME2xN{4zPTd5IN88US=> MXrTRW5ITVJ?
D-392MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4i5SGlEPTB;MUOuOlQzQCEQvF2= NIWwZWRUSU6JRWK=
NB7 NIOzPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTF2LkKzO|Qh|ryP MX7TRW5ITVJ?
SK-LMS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\rW5RTUUN3ME2xOE42OTR3IN88US=> NWn0O|NMW0GQR1XS
SK-UT-1 MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoToTWM2OD1zND63PFg6KM7:TR?= NXmwOIRnW0GQR1XS
CA46 NU\J[JdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jYVWlEPTB;MUWuNFU5PiEQvF2= MX3TRW5ITVJ?
IST-SL2 NIjkSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HZOGlEPTB;MUWuNVkxOSEQvF2= NEmzc5pUSU6JRWK=
BC-1 NGf5WGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\iTWM2OD1zNT6zN|E1KM7:TR?= Mom1V2FPT0WU
LS-123 MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTF3LkixO|Mh|ryP MmqzV2FPT0WU
Ramos-2G6-4C10 NYTpcWhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfIVo5KSzVyPUG2MlA6OjRizszN Mkn5V2FPT0WU
MZ1-PC NXXNdoQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr5[3hKSzVyPUG2Mlc{OTNizszN NFfoUYVUSU6JRWK=
LB647-SCLC NUflOoZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rhfmlEPTB;MU[uPVM4OiEQvF2= NYD3Z|FQW0GQR1XS
NCI-H1694 NXfDTGhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTF5LkG1Nlkh|ryP NVPaR2ltW0GQR1XS
NCI-H322M MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TlR2lEPTB;MUeuOFM3PiEQvF2= MX3TRW5ITVJ?
ES7 NGH0clZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHpN|UzUUN3ME2xPE4{QTF2IN88US=> MVzTRW5ITVJ?
LC-2-ad MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXO[ZJKSzVyPUG4MlQ{QDZizszN NXn6eYk3W0GQR1XS
SF268 MmHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjJVZVKSzVyPUG4Mlc1ODlizszN MmHvV2FPT0WU
RPMI-8402 NI\4RppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTF7LkC3OFIh|ryP NV\UfVlsW0GQR1XS
HCE-T NHzNdlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH4eoRWUUN3ME2yNE4zOzR2IN88US=> NGnRfWVUSU6JRWK=
A101D MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C3SWlEPTB;MkCuPFU5PyEQvF2= MonkV2FPT0WU
MRK-nu-1 NVO0SlVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTJyLkmxN{DPxE1? MVXTRW5ITVJ?
LXF-289 NIXEUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX34[JlJUUN3ME2yNU4xOzhizszN MV3TRW5ITVJ?
NALM-6 NXvteXJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX3TYJKSzVyPUKxMlE6PjdizszN M2rpdnNCVkeHUh?=
DOHH-2 NYfFNIc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJzLkS4NVMh|ryP MkDFV2FPT0WU
EW-16 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3sUXRFUUN3ME2yNk4yPDB{IN88US=> M{[zTnNCVkeHUh?=
A4-Fuk M1H4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ{LkKxOFkh|ryP NHvwdWpUSU6JRWK=
HD-MY-Z NXP4e2ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[0R3lKSzVyPUKyMlM6PjVizszN NHHzbpdUSU6JRWK=
SKM-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELOTohKSzVyPUKyMlc{PTFizszN M1\SdXNCVkeHUh?=
DMS-153 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\tXmlEPTB;MkOuOFIxPCEQvF2= MWTTRW5ITVJ?
LB373-MEL-D MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHrbW9vUUN3ME2yN{42PDV{IN88US=> NVXISHdQW0GQR1XS
LP-1 NYfsbotbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrSVldVUUN3ME2yN{45ODl5IN88US=> NGLOWmNUSU6JRWK=
GI-ME-N NYSyZm1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJ2LkK5NkDPxE1? NHuxeFdUSU6JRWK=
MPP-89 NFvR[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEf0SGVKSzVyPUK1MlIxOzZizszN MVLTRW5ITVJ?
U-698-M Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJ3LkK1NFMh|ryP NU[wZmJiW0GQR1XS
HC-1 NIrnTGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfBVYg5UUN3ME2yOU43PDF6IN88US=> NYfvU2JOW0GQR1XS
HCC2157 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlftTWM2OD1{NT62O|Mh|ryP Mom0V2FPT0WU
MOLT-4 NIHFOWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXyVFZKSzVyPUK2MlI4OyEQvF2= NIL1WZpUSU6JRWK=
LS-411N M{LWZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTjN29KSzVyPUK2MlM{PjlizszN MlHQV2FPT0WU
Becker MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJ4LkWxPFEh|ryP M4nNeXNCVkeHUh?=
NCI-H23 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\nWWlEPTB;Mk[uO|U4PSEQvF2= M4Pu[nNCVkeHUh?=
IST-SL1 NWPEd5RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\u[WFDUUN3ME2yO{4{QDZ5IN88US=> MX7TRW5ITVJ?
MZ2-MEL MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTJ5LkS1OlYh|ryP MUnTRW5ITVJ?
RKO NVXQZnlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn4TWM2OD1{OD6xOFQ3KM7:TR?= MWfTRW5ITVJ?
TE-441-T M4fJcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ6Lke4PUDPxE1? NYLHdpJ5W0GQR1XS
EW-24 NWWycZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjvW5FsUUN3ME2yPU4yOjV7IN88US=> NHvZOHJUSU6JRWK=
no-10 MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ7LkG2N|Eh|ryP MVHTRW5ITVJ?
D-542MG NUf5PZNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ7LkmyNlEh|ryP MWnTRW5ITVJ?
ST486 M4nY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNyLk[0OVEh|ryP M3\qNnNCVkeHUh?=
KURAMOCHI NGjlWWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLWPHlKSzVyPUOwMlgxPTdizszN NFntbnRUSU6JRWK=
ES8 NHHneHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;yfGlEPTB;M{GuOVk4OiEQvF2= MmjuV2FPT0WU
BL-41 NU[zXJhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknITWM2OD1|Mj6xNFU1KM7:TR?= NWC1PWlUW0GQR1XS
NB6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvpUlRKSzVyPUOyMlM5PTVizszN MV7TRW5ITVJ?
NCI-H1304 MmrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTN{LkS5Olch|ryP MVjTRW5ITVJ?
MS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXwdnZKSzVyPUOyMlc4PTFizszN MVPTRW5ITVJ?
MFH-ino M2fBNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P2eWlEPTB;M{SuN|IzPCEQvF2= M2D6ZnNCVkeHUh?=
NOS-1 M3LXWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH0PYZLUUN3ME2zOE43PzR6IN88US=> NUPoRlJkW0GQR1XS
HUTU-80 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXlTWM2OD1|NT6zOlY4KM7:TR?= NWO5VYU1W0GQR1XS
EB2 NV7LNmlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTN4Lk[xPFkh|ryP M2\OUnNCVkeHUh?=
L-540 M4q3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPaTWM2OD1|Nz6yN|A5KM7:TR?= MlnlV2FPT0WU
NCI-H747 NVOzbXF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTN6Lki4OFYh|ryP M3nrVXNCVkeHUh?=
NCI-H446 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fvUWlEPTB;M{muPVY2OSEQvF2= M1f4SHNCVkeHUh?=
MOLT-16 NEXtUWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr3bWZKSzVyPUSyMlQyPSEQvF2= NUL1V3ZMW0GQR1XS
BC-3 MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWwdZlOUUN3ME20OU41QDl4IN88US=> M4PINXNCVkeHUh?=
SJSA-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;HTWM2OD12NT61OFc1KM7:TR?= MkTtV2FPT0WU
BB65-RCC NGPKXoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR3Lk[2OkDPxE1? MlXHV2FPT0WU
SNB75 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTUTXZpUUN3ME20Ok4xOThizszN MlTrV2FPT0WU

... 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 to the product 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
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
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