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 NW\VXodLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwMEK1OFQh|ryP NHjpOZBUSU6JRWK=
HCC2218 Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVznfWNJUUN3ME2wMlA2OzJ4IN88US=> MY\TRW5ITVJ?
OCUB-M MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m0UGlEPTB;MD6wOVc1KM7:TR?= NVmydIhTW0GQR1XS
ECC12 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwMEmyN|Eh|ryP MXfTRW5ITVJ?
DSH1 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwMEmzPVYh|ryP NGfOfYZUSU6JRWK=
BT-474 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXyTWM2OD1yLkKxN|E2KM7:TR?= NXLEbZpwW0GQR1XS
BB30-HNC NFPDSWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPVTWM2OD1yLkK0OlU1KM7:TR?= NUfvbG92W0GQR1XS
EKVX MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrwb3BKSzVyPUCuOFQ5PzRizszN MYPTRW5ITVJ?
TE-12 MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DEcWlEPTB;MD60PVA2PyEQvF2= MYjTRW5ITVJ?
A388 MmC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHpb2xKSzVyPUCuO|IzPThizszN M1\UNHNCVkeHUh?=
TE-9 NHv6eIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLmTWM2OD1yLke0OFU{KM7:TR?= NWHTWVNKW0GQR1XS
LB2241-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLhNmRQUUN3ME2xMlE2PDB|IN88US=> M2LZSXNCVkeHUh?=
LB996-RCC NGqzO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXO2PXhqUUN3ME2xMlM3OjJ6IN88US=> MUjTRW5ITVJ?
LC-1F MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3aTWM2OD1zLkO4NlQ1KM7:TR?= MXLTRW5ITVJ?
TE-6 M1PxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnETWM2OD1zLkW1NlAyKM7:TR?= M{\GUHNCVkeHUh?=
A253 M2XaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjxdWVKSzVyPUGuPVc{OzVizszN MYHTRW5ITVJ?
OS-RC-2 NIH5cGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFwOUmxPVkh|ryP MVzTRW5ITVJ?
TE-1 M1PtPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml21TWM2OD1{LkC0PFMh|ryP MUnTRW5ITVJ?
RL95-2 MmX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTNwMUW2O{DPxE1? M3jpWHNCVkeHUh?=
LS-513 M1iwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[5XXJKSzVyPUOuOFAxPDFizszN M3H0bnNCVkeHUh?=
DJM-1 M3zle2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfDRYVxUUN3ME2zMlQ3QTd3IN88US=> NIT6V|RUSU6JRWK=
NMC-G1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNwNUS1NFEh|ryP NHHwdINUSU6JRWK=
TE-10 NXLNdW1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jGcGlEPTB;Mz61OVM2PiEQvF2= NXXpWpNSW0GQR1XS
TE-5 NVy3[XZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TXTWlEPTB;ND6wN|c{KM7:TR?= NF3PTppUSU6JRWK=
TK10 NFz3NnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTRwMU[1NlIh|ryP NVXG[nl7W0GQR1XS
UACC-812 NXSwR2ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[0TWM2OD12LkW2NVU{KM7:TR?= NWT3bIJiW0GQR1XS
SW962 MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLxTWM2OD13LkCyNVU6KM7:TR?= MUfTRW5ITVJ?
SW954 NEPCeYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTVwM{myOFUh|ryP MW\TRW5ITVJ?
COLO-668 NWOxNoltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXGcJRKSzVyPUWuO|I3PjdizszN MXHTRW5ITVJ?
LB1047-RCC MmryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfnbWNsUUN3ME21MlgxODR4IN88US=> MnjQV2FPT0WU
NB5 M3\Ne2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LNXGlEPTB;Nj6yNVAxOSEQvF2= NUDrbmpDW0GQR1XS
NTERA-S-cl-D1 NX\LelJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvtTWM2OD14LkK2OVYyKM7:TR?= M2T5cHNCVkeHUh?=
IST-MEL1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnwV21OUUN3ME22MlQ{Pjl2IN88US=> MV\TRW5ITVJ?
GI-1 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTGZWRKSzVyPU[uOVE3QDJizszN MkHjV2FPT0WU
TGBC1TKB NFfhe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33hVmlEPTB;Nz6wO|E5OyEQvF2= MXLTRW5ITVJ?
GT3TKB NInFeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzsTWM2OD15LkKyO|Q1KM7:TR?= NXfQTpRsW0GQR1XS
EVSA-T NXjXdGNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\yTWM2OD15LkSyPFEyKM7:TR?= MnzkV2FPT0WU
D-502MG MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrrNo9LUUN3ME23MlQ5QDl2IN88US=> MVHTRW5ITVJ?
TE-8 M4fKb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zaNGlEPTB;Nz63OlE2QSEQvF2= M{DD[3NCVkeHUh?=
OVCAR-4 NV;Lb24xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[2T2lEPTB;OT6xNVY4PSEQvF2= MV;TRW5ITVJ?
D-336MG M13xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\FTWM2OD17LkS3N|k2KM7:TR?= Mm\PV2FPT0WU
GCIY NXzGd4RGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK1TWM2OD17LkW3OFIh|ryP M4TYRXNCVkeHUh?=
KS-1 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M133OGlEPTB;OT62OlI5PyEQvF2= NYexZVlVW0GQR1XS
HCC2998 NX3zO5lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTlwOU[zNFch|ryP NFjBfVBUSU6JRWK=
D-247MG Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP3TWM2OD17Lkm4NlkyKM7:TR?= MWLTRW5ITVJ?
TE-15 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17zfWlEPTB;MUCuNlQ2KM7:TR?= M4HLSnNCVkeHUh?=
IST-MES1 NYm4XYE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzje2FKSzVyPUGwMlI2PjVizszN MoHQV2FPT0WU
ETK-1 NGLzbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTj[W5KSzVyPUGwMlYzOyEQvF2= NXvhelZOW0GQR1XS
RCC10RGB NHXFbWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvjbIxKSzVyPUGwMlk3OSEQvF2= MWXTRW5ITVJ?
KNS-42 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[1TWM2OD1zMT63NlU2KM7:TR?= M1LKUHNCVkeHUh?=
LB771-HNC MnTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF{LkG3NVIh|ryP MkPpV2FPT0WU
SR MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvRS2dKSzVyPUGyMlIxPjRizszN MnrrV2FPT0WU
NCI-H1355 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD5WpNPUUN3ME2xNk45QTh3IN88US=> MmG5V2FPT0WU
ES6 NXn6T49mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT3TWM2OD1zMz6wO|gh|ryP NWnpeJVUW0GQR1XS
SK-NEP-1 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTF|LkK1O|ch|ryP MUTTRW5ITVJ?
D-392MG Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF|Lk[0Nlgh|ryP MnTGV2FPT0WU
NB7 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1KwdGlEPTB;MUSuNlM4PCEQvF2= Ml\SV2FPT0WU
SK-LMS-1 NXf6do1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PlNmlEPTB;MUSuOVE1PSEQvF2= NIjvW2lUSU6JRWK=
SK-UT-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\XcVY6UUN3ME2xOE44QDh7IN88US=> Mn73V2FPT0WU
CA46 NUH3VHQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHzTWM2OD1zNT6wOVg3KM7:TR?= NFjlWGtUSU6JRWK=
IST-SL2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofGTWM2OD1zNT6xPVAyKM7:TR?= MWHTRW5ITVJ?
BC-1 NX3o[oN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF3LkOzNVQh|ryP NEPSWZpUSU6JRWK=
LS-123 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPzTWM2OD1zNT64NVc{KM7:TR?= MkHSV2FPT0WU
Ramos-2G6-4C10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TjTGlEPTB;MU[uNFkzPCEQvF2= M3T3VnNCVkeHUh?=
MZ1-PC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHzTWM2OD1zNj63N|E{KM7:TR?= NXrwSINOW0GQR1XS
LB647-SCLC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nXO2lEPTB;MU[uPVM4OiEQvF2= M{j0[nNCVkeHUh?=
NCI-H1694 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF5LkG1Nlkh|ryP Mlr0V2FPT0WU
NCI-H322M NWflUWNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfFTWM2OD1zNz60N|Y3KM7:TR?= NFnWNWNUSU6JRWK=
ES7 MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTF6LkO5NVQh|ryP NVX4OJZRW0GQR1XS
LC-2-ad NVy5UFBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGH2RnZKSzVyPUG4MlQ{QDZizszN NHnCTXFUSU6JRWK=
SF268 M4jQRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXub4s{UUN3ME2xPE44PDB7IN88US=> NXXofmN{W0GQR1XS
RPMI-8402 NYXsfXNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLGXmdKSzVyPUG5MlA4PDJizszN NGnaSHFUSU6JRWK=
HCE-T NYD1XmJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrQ[2tSUUN3ME2yNE4zOzR2IN88US=> NH60blhUSU6JRWK=
A101D NUO2O3U2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLITWM2OD1{MD64OVg4KM7:TR?= MYPTRW5ITVJ?
MRK-nu-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nyW2lEPTB;MkCuPVE{KM7:TR?= MVjTRW5ITVJ?
LXF-289 NF;zdGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrsR|lKSzVyPUKxMlA{QCEQvF2= NHGxUoRUSU6JRWK=
NALM-6 MmDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfIblA6UUN3ME2yNU4yQTZ5IN88US=> NVPzVmF[W0GQR1XS
DOHH-2 M3jtS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE[2N2tKSzVyPUKxMlQ5OTNizszN MofJV2FPT0WU
EW-16 NF\kW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTpXpYyUUN3ME2yNk4yPDB{IN88US=> NIH3Oo5USU6JRWK=
A4-Fuk MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjQS5AyUUN3ME2yNk4zOTR7IN88US=> M{DYdXNCVkeHUh?=
HD-MY-Z MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrYXHBKSzVyPUKyMlM6PjVizszN MUPTRW5ITVJ?
SKM-1 NGHPUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJ{LkezOVEh|ryP NYXEfo1PW0GQR1XS
DMS-153 NUHld|lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\GdndKSzVyPUKzMlQzODRizszN MXLTRW5ITVJ?
LB373-MEL-D NWXsdGhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJ|LkW0OVIh|ryP NFzrNWhUSU6JRWK=
LP-1 NWK3UXNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJ|LkiwPVch|ryP MYrTRW5ITVJ?
GI-ME-N M3vUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor2TWM2OD1{ND6yPVIh|ryP M{XjPXNCVkeHUh?=
MPP-89 NF3wbWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3iTWM2OD1{NT6yNFM3KM7:TR?= NIX5bHpUSU6JRWK=
U-698-M M{TUXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJ3LkK1NFMh|ryP NULBN2g5W0GQR1XS
HC-1 NIP5[45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJ3Lk[0NVgh|ryP NYHqeXlWW0GQR1XS
HCC2157 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTCTWM2OD1{NT62O|Mh|ryP MXHTRW5ITVJ?
MOLT-4 Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ4LkK3N{DPxE1? MnSzV2FPT0WU
LS-411N MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ4LkOzOlkh|ryP M3vyc3NCVkeHUh?=
Becker MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTJ4LkWxPFEh|ryP NVPWU3hOW0GQR1XS
NCI-H23 MkHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPGdItKSzVyPUK2Mlc2PzVizszN NUPNfGlJW0GQR1XS
IST-SL1 MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT0cGlKSzVyPUK3MlM5PjdizszN NULEdYozW0GQR1XS
MZ2-MEL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG3b41vUUN3ME2yO{41PTZ4IN88US=> M3mxbnNCVkeHUh?=
RKO NWG1R4hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;VPGlEPTB;MkiuNVQ1PiEQvF2= NHT0TWhUSU6JRWK=
TE-441-T MofXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJ6Lke4PUDPxE1? NHHnVFFUSU6JRWK=
EW-24 NEXmRmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7oWo1KSzVyPUK5MlEzPTlizszN MV7TRW5ITVJ?
no-10 Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn2fI9KSzVyPUK5MlE3OzFizszN M33M[3NCVkeHUh?=
D-542MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJ7LkmyNlEh|ryP M4LGcnNCVkeHUh?=
ST486 NYXYeGhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTBVIVDUUN3ME2zNE43PDVzIN88US=> MXfTRW5ITVJ?
KURAMOCHI NX7qUJQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm4TWM2OD1|MD64NFU4KM7:TR?= MVjTRW5ITVJ?
ES8 MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorXTWM2OD1|MT61PVczKM7:TR?= NHTy[FNUSU6JRWK=
BL-41 M3fve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvVVWVKSzVyPUOyMlExPTRizszN NFPSOJZUSU6JRWK=
NB6 NELtVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rVSGlEPTB;M{KuN|g2PSEQvF2= M2HUNXNCVkeHUh?=
NCI-H1304 M37PUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTN{LkS5Olch|ryP MXnTRW5ITVJ?
MS-1 M{P5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7pUpJTUUN3ME2zNk44PzVzIN88US=> NEPydWpUSU6JRWK=
MFH-ino MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjwW3lKSzVyPUO0MlMzOjRizszN M1yze3NCVkeHUh?=
NOS-1 M1ywOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjpTWM2OD1|ND62O|Q5KM7:TR?= M{HjPXNCVkeHUh?=
HUTU-80 MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULFSHNoUUN3ME2zOU4{PjZ5IN88US=> M2rQXnNCVkeHUh?=
EB2 MoH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\qTWM2OD1|Nj62NVg6KM7:TR?= MkGyV2FPT0WU
L-540 M1:wV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXET4kyUUN3ME2zO{4zOzB6IN88US=> NHewbGhUSU6JRWK=
NCI-H747 NHTLVVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN6Lki4OFYh|ryP M3TpfnNCVkeHUh?=
NCI-H446 MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrVfIxKSzVyPUO5Mlk3PTFizszN MnrpV2FPT0WU
MOLT-16 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KwT2lEPTB;NEKuOFE2KM7:TR?= NWP6[W9EW0GQR1XS
BC-3 M3m2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInifnJKSzVyPUS1MlQ5QTZizszN MnrGV2FPT0WU
SJSA-1 NIrUZ3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnEeoZ7UUN3ME20OU42PDd2IN88US=> MWTTRW5ITVJ?
BB65-RCC NXHqPXA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[4SZRKSzVyPUS1MlY3PiEQvF2= NFj1fI1USU6JRWK=
SNB75 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonpTWM2OD12Nj6wNVgh|ryP NHnrRmdUSU6JRWK=

... 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(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
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
    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
NCT02015169 Completed HER2-positive Gastric Cancer Patients With Liver Metastasis Samsung Medical Center July 9 2012 Phase 2
NCT00073528 Completed Neoplasms Breast Novartis Pharmaceuticals|Novartis December 9 2003 Phase 3
NCT03418558 Recruiting Metastatic Colorectal Cancer Fondazione del Piemonte per l''Oncologia July 8 2015 Phase 2
NCT01591577 Recruiting Newly Diagnosed Glioblastoma Multiforme Jonsson Comprehensive Cancer Center|GlaxoSmithKline December 7 2012 Phase 2
NCT00667251 Active not recruiting Breast Cancer Novartis Pharmaceuticals|NCIC Clinical Trials Group|Novartis October 7 2008 Phase 3
NCT00367471 Active not recruiting Neoplasms Breast Novartis Pharmaceuticals|Novartis December 7 2006 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