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 NY\WeHN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfYd45KSzVyPUCuNFI2PDRizszN MVrTRW5ITVJ?
HCC2218 NXHKeVloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXWNXlKSzVyPUCuNFU{OjZizszN NHjrXoRUSU6JRWK=
OCUB-M MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjNbY9XUUN3ME2wMlA2PzRizszN NVvXboxTW0GQR1XS
ECC12 NFjNXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEf1N3VKSzVyPUCuNFkzOzFizszN MXfTRW5ITVJ?
DSH1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTYVoFWUUN3ME2wMlA6Ozl4IN88US=> M1TJbXNCVkeHUh?=
BT-474 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnEVmVGUUN3ME2wMlIyOzF3IN88US=> NXXiSphHW0GQR1XS
BB30-HNC MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jHVWlEPTB;MD6yOFY2PCEQvF2= NFTPd2FUSU6JRWK=
EKVX NVj3d3d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX2R|ZKSzVyPUCuOFQ5PzRizszN MWLTRW5ITVJ?
TE-12 NUixS|IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\GbYpmUUN3ME2wMlQ6ODV5IN88US=> M3HleXNCVkeHUh?=
A388 NInXcYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHmTWM2OD1yLkeyNlU5KM7:TR?= NVTxO5FJW0GQR1XS
TE-9 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7YTWM2OD1yLke0OFU{KM7:TR?= MoLrV2FPT0WU
LB2241-RCC NXi5bJJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLZTWM2OD1zLkG1OFA{KM7:TR?= NIXi[HBUSU6JRWK=
LB996-RCC M4HqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwM{[yNlgh|ryP MXjTRW5ITVJ?
LC-1F Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFm3OlZKSzVyPUGuN|gzPDRizszN MWrTRW5ITVJ?
TE-6 NWfUcZlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTRTWM2OD1zLkW1NlAyKM7:TR?= MVfTRW5ITVJ?
A253 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\HTFFkUUN3ME2xMlk4OzN3IN88US=> M2DaOHNCVkeHUh?=
OS-RC-2 NX;6[3NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e2OWlEPTB;MT65PVE6QSEQvF2= NEfCTXJUSU6JRWK=
TE-1 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHZb4VEUUN3ME2yMlA1QDNizszN M3nTbXNCVkeHUh?=
RL95-2 NVzKOW1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;hOmlEPTB;Mz6xOVY4KM7:TR?= MWfTRW5ITVJ?
LS-513 NIXhNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTNwNECwOFEh|ryP MoDMV2FPT0WU
DJM-1 NIO4OZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4WwPWlEPTB;Mz60Olk4PSEQvF2= M2SyVXNCVkeHUh?=
NMC-G1 NF3ufGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrVTWM2OD1|LkW0OVAyKM7:TR?= NXzYcpRNW0GQR1XS
TE-10 NEDTNlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT6TWM2OD1|LkW1N|U3KM7:TR?= Ml7sV2FPT0WU
TE-5 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnybHZKSzVyPUSuNFM4OyEQvF2= NF3BOndUSU6JRWK=
TK10 MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTRwMU[1NlIh|ryP NXPqfIVmW0GQR1XS
UACC-812 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTRwNU[xOVMh|ryP NGD6V2dUSU6JRWK=
SW962 NUD1Z4RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HWfmlEPTB;NT6wNlE2QSEQvF2= MYHTRW5ITVJ?
SW954 NIfrbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkK1TWM2OD13LkO5NlQ2KM7:TR?= MXvTRW5ITVJ?
COLO-668 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELFN|hKSzVyPUWuO|I3PjdizszN NIjVcmJUSU6JRWK=
LB1047-RCC NHLPd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPkTWM2OD13LkiwNFQ3KM7:TR?= NHSxWXFUSU6JRWK=
NB5 NFO2UIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTZwMkGwNFEh|ryP MlLUV2FPT0WU
NTERA-S-cl-D1 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\YWGlEPTB;Nj6yOlU3OSEQvF2= NF;P[VJUSU6JRWK=
IST-MEL1 M2PSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\ETWM2OD14LkSzOlk1KM7:TR?= MVfTRW5ITVJ?
GI-1 NHXrOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTZwNUG2PFIh|ryP NYHUUXRPW0GQR1XS
TGBC1TKB NX[1[5E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLzTWM2OD15LkC3NVg{KM7:TR?= M3TwOHNCVkeHUh?=
GT3TKB MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vaR2lEPTB;Nz6yNlc1PCEQvF2= MljyV2FPT0WU
EVSA-T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uy[2lEPTB;Nz60NlgyOSEQvF2= NYTKWHhuW0GQR1XS
D-502MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTdwNEi4PVQh|ryP NVnhVoVtW0GQR1XS
TE-8 NIn5ZmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[0c2lEPTB;Nz63OlE2QSEQvF2= MnjWV2FPT0WU
OVCAR-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrPWmY2UUN3ME25MlEyPjd3IN88US=> NV;0S21sW0GQR1XS
D-336MG NEnQcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n3OGlEPTB;OT60O|M6PSEQvF2= NUnCdWExW0GQR1XS
GCIY M1nlTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TDSmlEPTB;OT61O|QzKM7:TR?= M1ThZ3NCVkeHUh?=
KS-1 M{nJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3HTWM2OD17Lk[2Nlg4KM7:TR?= NEjlWm9USU6JRWK=
HCC2998 MkjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL6TWM2OD17Lkm2N|A4KM7:TR?= NXTIPIJ3W0GQR1XS
D-247MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEX4XGRKSzVyPUmuPVgzQTFizszN M4DBZXNCVkeHUh?=
TE-15 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zOfmlEPTB;MUCuNlQ2KM7:TR?= MX;TRW5ITVJ?
IST-MES1 M{jtO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnlTWM2OD1zMD6yOVY2KM7:TR?= MV3TRW5ITVJ?
ETK-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfoO4xKSzVyPUGwMlYzOyEQvF2= NVu5SFQ3W0GQR1XS
RCC10RGB NXLlSFh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPKd3FKSzVyPUGwMlk3OSEQvF2= MoTMV2FPT0WU
KNS-42 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzRPWFuUUN3ME2xNU44OjV3IN88US=> M{LKd3NCVkeHUh?=
LB771-HNC MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3lZW9nUUN3ME2xNk4yPzF{IN88US=> MVXTRW5ITVJ?
SR NIi4PWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\rTWM2OD1zMj6yNFY1KM7:TR?= NH;RcIxUSU6JRWK=
NCI-H1355 M4HKOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXRWpd5UUN3ME2xNk45QTh3IN88US=> NFLqeY1USU6JRWK=
ES6 M1ro[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jtWmlEPTB;MUOuNFc5KM7:TR?= MXnTRW5ITVJ?
SK-NEP-1 M1e2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zFUWlEPTB;MUOuNlU4PyEQvF2= NH[1d|JUSU6JRWK=
D-392MG NH;NW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\VeVBsUUN3ME2xN{43PDJ6IN88US=> NWHLU5lFW0GQR1XS
NB7 NX3XZ5FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHe1VlJKSzVyPUG0MlI{PzRizszN NF21T4JUSU6JRWK=
SK-LMS-1 NFHFSGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqwTWM2OD1zND61NVQ2KM7:TR?= NXu2U|M2W0GQR1XS
SK-UT-1 Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF2Lke4PFkh|ryP Mm\hV2FPT0WU
CA46 NVvhdGU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW3TWM2OD1zNT6wOVg3KM7:TR?= MVzTRW5ITVJ?
IST-SL2 NV\YbVNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnRfWhKSzVyPUG1MlE6ODFizszN M3r1WHNCVkeHUh?=
BC-1 NFmzeZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrNOVJKSzVyPUG1MlM{OTRizszN NHHk[m9USU6JRWK=
LS-123 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTkTWM2OD1zNT64NVc{KM7:TR?= M4nTN3NCVkeHUh?=
Ramos-2G6-4C10 NXvWS2tYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF4LkC5NlQh|ryP NVH3V|ZjW0GQR1XS
MZ1-PC NUHESpJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPUTWM2OD1zNj63N|E{KM7:TR?= NYLqfWF2W0GQR1XS
LB647-SCLC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF4LkmzO|Ih|ryP M1:wdnNCVkeHUh?=
NCI-H1694 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7RTWM2OD1zNz6xOVI6KM7:TR?= MUjTRW5ITVJ?
NCI-H322M MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HNOWlEPTB;MUeuOFM3PiEQvF2= MmfUV2FPT0WU
ES7 NUT1cGVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITOSGhKSzVyPUG4MlM6OTRizszN M{PiWnNCVkeHUh?=
LC-2-ad NYjFRm5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;EXWhKSzVyPUG4MlQ{QDZizszN NULTe|g5W0GQR1XS
SF268 MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nEOGlEPTB;MUiuO|QxQSEQvF2= MkGzV2FPT0WU
RPMI-8402 NYLObHJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPJOoVKSzVyPUG5MlA4PDJizszN NUD2W2xIW0GQR1XS
HCE-T M1L0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[zWmlEPTB;MkCuNlM1PCEQvF2= M{f2cnNCVkeHUh?=
A101D M33UTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;xZVJoUUN3ME2yNE45PTh5IN88US=> NVHVU2tIW0GQR1XS
MRK-nu-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TTPWlEPTB;MkCuPVE{KM7:TR?= M37JdHNCVkeHUh?=
LXF-289 NUPpWo9PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJzLkCzPEDPxE1? NFzB[FNUSU6JRWK=
NALM-6 M{XlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW4d5c3UUN3ME2yNU4yQTZ5IN88US=> NHXSe2ZUSU6JRWK=
DOHH-2 NGrVc|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfDTWM2OD1{MT60PFE{KM7:TR?= MkiyV2FPT0WU
EW-16 NXvCXJBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT3TWM2OD1{Mj6xOFAzKM7:TR?= NFW5dJJUSU6JRWK=
A4-Fuk MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jDcWlEPTB;MkKuNlE1QSEQvF2= MkXtV2FPT0WU
HD-MY-Z MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJ{LkO5OlUh|ryP NH3wc41USU6JRWK=
SKM-1 NFvrfIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJ{LkezOVEh|ryP MYTTRW5ITVJ?
DMS-153 MnrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHxS|dKSzVyPUKzMlQzODRizszN NEP4[IhUSU6JRWK=
LB373-MEL-D MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLCOGh{UUN3ME2yN{42PDV{IN88US=> NVjMXW9iW0GQR1XS
LP-1 NH;qRmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPrcoNyUUN3ME2yN{45ODl5IN88US=> M13KUXNCVkeHUh?=
GI-ME-N MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLlV5lKSzVyPUK0MlI6OiEQvF2= M3L2[HNCVkeHUh?=
MPP-89 MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C2WmlEPTB;MkWuNlA{PiEQvF2= NWCxfGNxW0GQR1XS
U-698-M NGnnRYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDjNWhKSzVyPUK1MlI2ODNizszN NY\jRoFHW0GQR1XS
HC-1 MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJ3Lk[0NVgh|ryP NF;oTXhUSU6JRWK=
HCC2157 NF3J[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\FbpRTUUN3ME2yOU43PzNizszN NXzx[mVSW0GQR1XS
MOLT-4 NV3EWlk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJ4LkK3N{DPxE1? NGLhc4pUSU6JRWK=
LS-411N NFXZbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJ4LkOzOlkh|ryP M1LRXnNCVkeHUh?=
Becker NYizcmFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP5TWM2OD1{Nj61NVgyKM7:TR?= Mn7HV2FPT0WU
NCI-H23 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ4Lke1O|Uh|ryP NVzOeXJ[W0GQR1XS
IST-SL1 NF6yUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL2XlVKSzVyPUK3MlM5PjdizszN NXTMTndmW0GQR1XS
MZ2-MEL MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojTTWM2OD1{Nz60OVY3KM7:TR?= MYHTRW5ITVJ?
RKO NY[2XXEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPZSZdKSzVyPUK4MlE1PDZizszN M2\hPHNCVkeHUh?=
TE-441-T NF7hOY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G3VGlEPTB;MkiuO|g6KM7:TR?= NI\QVJRUSU6JRWK=
EW-24 M3HhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPIRZBxUUN3ME2yPU4yOjV7IN88US=> MV;TRW5ITVJ?
no-10 NYSxVINwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\X[oVKSzVyPUK5MlE3OzFizszN MlPGV2FPT0WU
D-542MG MmCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;UbmMxUUN3ME2yPU46OjJzIN88US=> MlvEV2FPT0WU
ST486 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDkSHRPUUN3ME2zNE43PDVzIN88US=> NVmyRmFMW0GQR1XS
KURAMOCHI MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG2TWM2OD1|MD64NFU4KM7:TR?= NXPmR3V3W0GQR1XS
ES8 NIHRbGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3GTWM2OD1|MT61PVczKM7:TR?= NY\qW3lsW0GQR1XS
BL-41 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTuPZZZUUN3ME2zNk4yODV2IN88US=> NXy1e4xyW0GQR1XS
NB6 NVjnb2lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrlc3BYUUN3ME2zNk4{QDV3IN88US=> NFrBWVBUSU6JRWK=
NCI-H1304 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTN{LkS5Olch|ryP MULTRW5ITVJ?
MS-1 M{DmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfiS2VKSzVyPUOyMlc4PTFizszN Ml3CV2FPT0WU
MFH-ino M4rmUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OwPWlEPTB;M{SuN|IzPCEQvF2= M2PXcnNCVkeHUh?=
NOS-1 NVrhfo5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3V[ldKSzVyPUO0MlY4PDhizszN NIfyT4lUSU6JRWK=
HUTU-80 NX\FRo1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfBcGtpUUN3ME2zOU4{PjZ5IN88US=> MmP5V2FPT0WU
EB2 NVPwUY1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKwfolRUUN3ME2zOk43OTh7IN88US=> MX7TRW5ITVJ?
L-540 NFTa[FNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[1TWM2OD1|Nz6yN|A5KM7:TR?= MUXTRW5ITVJ?
NCI-H747 NWrmWWl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzVU|JKSzVyPUO4Mlg5PDZizszN NFKzOXdUSU6JRWK=
NCI-H446 MkKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHRe5BKSzVyPUO5Mlk3PTFizszN M{fVWnNCVkeHUh?=
MOLT-16 NFPDflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm5blM2UUN3ME20Nk41OTVizszN NWjQfGQ3W0GQR1XS
BC-3 NFrqR5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnkcpdKUUN3ME20OU41QDl4IN88US=> MVjTRW5ITVJ?
SJSA-1 M4jafWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzGTWM2OD12NT61OFc1KM7:TR?= Mo\MV2FPT0WU
BB65-RCC MmnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELtb2tKSzVyPUS1MlY3PiEQvF2= MUTTRW5ITVJ?
SNB75 NH:1OGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nlVGlEPTB;NE[uNFE5KM7:TR?= NFjSUIlUSU6JRWK=

... 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
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
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