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 NX7FSnBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzoeYRWUUN3ME2wMlAzPTR2IN88US=> NInsT|ZUSU6JRWK=
HCC2218 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHRS4tKSzVyPUCuNFU{OjZizszN MXnTRW5ITVJ?
OCUB-M MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7uO4hKSzVyPUCuNFU4PCEQvF2= NUHNU3FIW0GQR1XS
ECC12 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwMEmyN|Eh|ryP M4qxTnNCVkeHUh?=
DSH1 NHrnfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1myO2lEPTB;MD6wPVM6PiEQvF2= MVTTRW5ITVJ?
BT-474 M{e4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELWbGhKSzVyPUCuNlE{OTVizszN NYi2fVJuW0GQR1XS
BB30-HNC M{PKdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfaT3ZCUUN3ME2wMlI1PjV2IN88US=> NYSxdpdMW0GQR1XS
EKVX NVTJboVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqyW4RKSzVyPUCuOFQ5PzRizszN NGjJ[ZBUSU6JRWK=
TE-12 NYPPNYx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC0TXhPUUN3ME2wMlQ6ODV5IN88US=> NVLPTVJVW0GQR1XS
A388 NWD5d3dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHaTWM2OD1yLkeyNlU5KM7:TR?= M{Ozb3NCVkeHUh?=
TE-9 M1PIc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TaXWlEPTB;MD63OFQ2OyEQvF2= NHHlbnJUSU6JRWK=
LB2241-RCC M4ezNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknQTWM2OD1zLkG1OFA{KM7:TR?= NWfQeplNW0GQR1XS
LB996-RCC NIjOe|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF34N|VKSzVyPUGuN|YzOjhizszN MlPIV2FPT0WU
LC-1F NE\SXXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17FUWlEPTB;MT6zPFI1PCEQvF2= MkH0V2FPT0WU
TE-6 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrTW5ZSUUN3ME2xMlU2OjBzIN88US=> M{\XPHNCVkeHUh?=
A253 M3nOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvtXI5KSzVyPUGuPVc{OzVizszN NXvwelZIW0GQR1XS
OS-RC-2 MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXWXZhrUUN3ME2xMlk6OTl7IN88US=> NH;6bFFUSU6JRWK=
TE-1 NVruPGxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfkWlBKSzVyPUKuNFQ5OyEQvF2= MUjTRW5ITVJ?
RL95-2 M1TiS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ZTWM2OD1|LkG1Olch|ryP MnLBV2FPT0WU
LS-513 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXXZ3N5UUN3ME2zMlQxODRzIN88US=> MXLTRW5ITVJ?
DJM-1 NH;MN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPZTWM2OD1|LkS2PVc2KM7:TR?= M{HHb3NCVkeHUh?=
NMC-G1 MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULnOoUyUUN3ME2zMlU1PTBzIN88US=> NF\1OIdUSU6JRWK=
TE-10 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uzOmlEPTB;Mz61OVM2PiEQvF2= NUDnWpRwW0GQR1XS
TE-5 MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIO1TlVKSzVyPUSuNFM4OyEQvF2= MXHTRW5ITVJ?
TK10 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf1XHl{UUN3ME20MlE3PTJ{IN88US=> NFK0d2VUSU6JRWK=
UACC-812 MmnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXJTWM2OD12LkW2NVU{KM7:TR?= MknaV2FPT0WU
SW962 M{SyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:1SWlEPTB;NT6wNlE2QSEQvF2= NWjIdng2W0GQR1XS
SW954 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXn[mJxUUN3ME21MlM6OjR3IN88US=> MlK0V2FPT0WU
COLO-668 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLN[mZJUUN3ME21MlczPjZ5IN88US=> NF;XWZVUSU6JRWK=
LB1047-RCC NILle5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDLephKSzVyPUWuPFAxPDZizszN Ml7xV2FPT0WU
NB5 NEfH[YdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTZwMkGwNFEh|ryP NFTNT2hUSU6JRWK=
NTERA-S-cl-D1 MnyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moq3TWM2OD14LkK2OVYyKM7:TR?= M4LwTXNCVkeHUh?=
IST-MEL1 M2fuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\1TWM2OD14LkSzOlk1KM7:TR?= MljxV2FPT0WU
GI-1 MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTZwNUG2PFIh|ryP NYrrOGJNW0GQR1XS
TGBC1TKB M3HBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrXTWM2OD15LkC3NVg{KM7:TR?= NWnLXXlXW0GQR1XS
GT3TKB MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHaTWM2OD15LkKyO|Q1KM7:TR?= NEXyXlVUSU6JRWK=
EVSA-T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX4TWM2OD15LkSyPFEyKM7:TR?= NHLkfGVUSU6JRWK=
D-502MG Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTdwNEi4PVQh|ryP MUjTRW5ITVJ?
TE-8 M1\BUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\3WXRKSzVyPUeuO|YyPTlizszN Ml\DV2FPT0WU
OVCAR-4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTlwMUG2O|Uh|ryP NVrnfVFYW0GQR1XS
D-336MG NX76bGRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW3TWM2OD17LkS3N|k2KM7:TR?= MnHtV2FPT0WU
GCIY NVvCZo1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nFVGlEPTB;OT61O|QzKM7:TR?= MXXTRW5ITVJ?
KS-1 NXXPTFVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\0PWlEPTB;OT62OlI5PyEQvF2= M3;wVnNCVkeHUh?=
HCC2998 NFi4T|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjtOoxKSzVyPUmuPVY{ODdizszN NHPpW2RUSU6JRWK=
D-247MG MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnGb2szUUN3ME25Mlk5OjlzIN88US=> NEf5Zo5USU6JRWK=
TE-15 NXPKR5NST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jCd2lEPTB;MUCuNlQ2KM7:TR?= MUXTRW5ITVJ?
IST-MES1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLkK1OlUh|ryP M1fQNXNCVkeHUh?=
ETK-1 M1LwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfLfJdKSzVyPUGwMlYzOyEQvF2= NYD1PXczW0GQR1XS
RCC10RGB M1vtbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFyLkm2NUDPxE1? M{[5OXNCVkeHUh?=
KNS-42 NGPSNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fteGlEPTB;MUGuO|I2PSEQvF2= Mo\WV2FPT0WU
LB771-HNC NXfSbmtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PJdmlEPTB;MUKuNVcyOiEQvF2= MlftV2FPT0WU
SR NES1T5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DKXGlEPTB;MUKuNlA3PCEQvF2= M3rUTXNCVkeHUh?=
NCI-H1355 Mln0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF{Lki5PFUh|ryP NXTxTY1bW0GQR1XS
ES6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS2VoNWUUN3ME2xN{4xPzhizszN NGqwemRUSU6JRWK=
SK-NEP-1 M37mcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPES5B4UUN3ME2xN{4zPTd5IN88US=> M4fRfnNCVkeHUh?=
D-392MG NYHKbZJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTF|Lk[0Nlgh|ryP NHTpPHVUSU6JRWK=
NB7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TRVmlEPTB;MUSuNlM4PCEQvF2= MUjTRW5ITVJ?
SK-LMS-1 NVXRZ5BQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf4TWM2OD1zND61NVQ2KM7:TR?= M2fRS3NCVkeHUh?=
SK-UT-1 NX;LfmRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDubmR4UUN3ME2xOE44QDh7IN88US=> NX\nWnJ3W0GQR1XS
CA46 NVXzVnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDpcY1LUUN3ME2xOU4xPTh4IN88US=> MonGV2FPT0WU
IST-SL2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL2TWM2OD1zNT6xPVAyKM7:TR?= M4T5[XNCVkeHUh?=
BC-1 NYL4NlhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP6RoJKSzVyPUG1MlM{OTRizszN NUXVbnQzW0GQR1XS
LS-123 M1nGdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWwNVJiUUN3ME2xOU45OTd|IN88US=> NH;wfoxUSU6JRWK=
Ramos-2G6-4C10 M2HYOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLQbmQ3UUN3ME2xOk4xQTJ2IN88US=> M2\WXXNCVkeHUh?=
MZ1-PC NH3BNnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPRTWM2OD1zNj63N|E{KM7:TR?= MVHTRW5ITVJ?
LB647-SCLC NIDGXJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIL5RYtKSzVyPUG2Mlk{PzJizszN NHzzeFFUSU6JRWK=
NCI-H1694 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF5LkG1Nlkh|ryP NV\QW4hHW0GQR1XS
NCI-H322M MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\mT2NOUUN3ME2xO{41OzZ4IN88US=> NGLKWIFUSU6JRWK=
ES7 NUPPe3NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HGOGlEPTB;MUiuN|kyPCEQvF2= M4ToWHNCVkeHUh?=
LC-2-ad NF[wZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;iTWM2OD1zOD60N|g3KM7:TR?= MWXTRW5ITVJ?
SF268 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofTTWM2OD1zOD63OFA6KM7:TR?= MU\TRW5ITVJ?
RPMI-8402 NXvscJVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO0TWM2OD1zOT6wO|QzKM7:TR?= MWfTRW5ITVJ?
HCE-T NFTXOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T2[mlEPTB;MkCuNlM1PCEQvF2= MX\TRW5ITVJ?
A101D MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXrO2ZKSzVyPUKwMlg2QDdizszN NHzCPZVUSU6JRWK=
MRK-nu-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETKTXdKSzVyPUKwMlkyOyEQvF2= NVrFUZZJW0GQR1XS
LXF-289 M1vteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfPO2RKSzVyPUKxMlA{QCEQvF2= MVfTRW5ITVJ?
NALM-6 NUTqeYRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPlTWM2OD1{MT6xPVY4KM7:TR?= MnnBV2FPT0WU
DOHH-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e3NWlEPTB;MkGuOFgyOyEQvF2= MkDPV2FPT0WU
EW-16 NVzNbXZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDZ[JhKSzVyPUKyMlE1ODJizszN NIXhSWNUSU6JRWK=
A4-Fuk M13JeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mne2TWM2OD1{Mj6yNVQ6KM7:TR?= Ml3pV2FPT0WU
HD-MY-Z MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvwTWM2OD1{Mj6zPVY2KM7:TR?= NXXwelh3W0GQR1XS
SKM-1 MoS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXPRnZKSzVyPUKyMlc{PTFizszN NV[wcoE3W0GQR1XS
DMS-153 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDXNY5KSzVyPUKzMlQzODRizszN NXrHNpVVW0GQR1XS
LB373-MEL-D M2TCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjMOVNKSzVyPUKzMlU1PTJizszN NGfsNnNUSU6JRWK=
LP-1 M4\YNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ|LkiwPVch|ryP M33Nb3NCVkeHUh?=
GI-ME-N M3fBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TsRmlEPTB;MkSuNlkzKM7:TR?= MY\TRW5ITVJ?
MPP-89 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnQOm5QUUN3ME2yOU4zODN4IN88US=> NGL5TFJUSU6JRWK=
U-698-M MkLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW4TWM2OD1{NT6yOVA{KM7:TR?= NWLFZVVwW0GQR1XS
HC-1 NYDnc4w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXNTWM2OD1{NT62OFE5KM7:TR?= MWDTRW5ITVJ?
HCC2157 NVjFNI9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OwbWlEPTB;MkWuOlc{KM7:TR?= NILtXpRUSU6JRWK=
MOLT-4 M3jTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD2TWM2OD1{Nj6yO|Mh|ryP Mn;KV2FPT0WU
LS-411N MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XUc2lEPTB;Mk[uN|M3QSEQvF2= MXfTRW5ITVJ?
Becker MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ4LkWxPFEh|ryP NU\W[IpbW0GQR1XS
NCI-H23 NHPpTnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ4Lke1O|Uh|ryP NEDx[2JUSU6JRWK=
IST-SL1 NHrNfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uzRWlEPTB;MkeuN|g3PyEQvF2= NV;4dlY1W0GQR1XS
MZ2-MEL NGqzfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJ5LkS1OlYh|ryP NXzKeXpFW0GQR1XS
RKO MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHW3cHlKSzVyPUK4MlE1PDZizszN MX3TRW5ITVJ?
TE-441-T MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJ6Lke4PUDPxE1? NU\zbHBIW0GQR1XS
EW-24 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17SfGlEPTB;MkmuNVI2QSEQvF2= MnXjV2FPT0WU
no-10 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\M[WlxUUN3ME2yPU4yPjNzIN88US=> MYHTRW5ITVJ?
D-542MG NEHyfnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDxUGxKSzVyPUK5MlkzOjFizszN M1jrWHNCVkeHUh?=
ST486 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vlVmlEPTB;M{CuOlQ2OSEQvF2= M2LjbHNCVkeHUh?=
KURAMOCHI M4f0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNyLkiwOVch|ryP NWXBdYwxW0GQR1XS
ES8 NFrjVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDzdXBKSzVyPUOxMlU6PzJizszN M{\CTHNCVkeHUh?=
BL-41 NHHIbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq3XGMzUUN3ME2zNk4yODV2IN88US=> MV;TRW5ITVJ?
NB6 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDaTXBKSzVyPUOyMlM5PTVizszN MlL4V2FPT0WU
NCI-H1304 M2XlfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDUTWM2OD1|Mj60PVY4KM7:TR?= MmXKV2FPT0WU
MS-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LmWGlEPTB;M{KuO|c2OSEQvF2= NVzDZoZVW0GQR1XS
MFH-ino MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7ZW3hKSzVyPUO0MlMzOjRizszN MoLYV2FPT0WU
NOS-1 M4HydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTN2Lk[3OFgh|ryP MmjzV2FPT0WU
HUTU-80 NX7lb41uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHpUIFKSzVyPUO1MlM3PjdizszN MmLpV2FPT0WU
EB2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTN4Lk[xPFkh|ryP M{DBeHNCVkeHUh?=
L-540 NW\xVm9PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTN5LkKzNFgh|ryP NVvqRWtTW0GQR1XS
NCI-H747 NEnJN3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnSS2lKSzVyPUO4Mlg5PDZizszN NF;LV3ZUSU6JRWK=
NCI-H446 NGXzbpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NICwNWFKSzVyPUO5Mlk3PTFizszN M3XNb3NCVkeHUh?=
MOLT-16 M{D5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR{LkSxOUDPxE1? NUnJdGF6W0GQR1XS
BC-3 MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR3LkS4PVYh|ryP MXnTRW5ITVJ?
SJSA-1 MkHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDEenV1UUN3ME20OU42PDd2IN88US=> NHzXfFVUSU6JRWK=
BB65-RCC NF:0RllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\GcpdNUUN3ME20OU43PjZizszN NIHQ[XpUSU6JRWK=
SNB75 M1rCU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR4LkCxPEDPxE1? NYHBWFlsW0GQR1XS

... 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 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