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 42 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 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTBV3JKSzVyPUCuNFI2PDRizszN MVrTRW5ITVJ?
HCC2218 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfmb3ZSUUN3ME2wMlA2OzJ4IN88US=> NWDUR2pbW0GQR1XS
OCUB-M M{P2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMEW3OEDPxE1? Mo\2V2FPT0WU
ECC12 NWe0XYpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDCWZlKSzVyPUCuNFkzOzFizszN MUTTRW5ITVJ?
DSH1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPZTWM2OD1yLkC5N|k3KM7:TR?= NIPCbWFUSU6JRWK=
BT-474 NGHRcZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTkenVKSzVyPUCuNlE{OTVizszN Mnq4V2FPT0WU
BB30-HNC Ml;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX33Vm9{UUN3ME2wMlI1PjV2IN88US=> M4fxTXNCVkeHUh?=
EKVX NHjGR3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nkcWlEPTB;MD60OFg4PCEQvF2= NX3LW2ZDW0GQR1XS
TE-12 NF3qNpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HKSGlEPTB;MD60PVA2PyEQvF2= MYHTRW5ITVJ?
A388 Mn;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LZcmlEPTB;MD63NlI2QCEQvF2= M4rFSHNCVkeHUh?=
TE-9 MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnTTWM2OD1yLke0OFU{KM7:TR?= M{H6d3NCVkeHUh?=
LB2241-RCC NHu0RYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\JbWFPUUN3ME2xMlE2PDB|IN88US=> NWX4VpZ2W0GQR1XS
LB996-RCC NHzHdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTFwM{[yNlgh|ryP M3\teXNCVkeHUh?=
LC-1F MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwM{iyOFQh|ryP M{TvcXNCVkeHUh?=
TE-6 NUC4U4I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LiPGlEPTB;MT61OVIxOSEQvF2= NXXXXop6W0GQR1XS
A253 M33Cc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGzdI1wUUN3ME2xMlk4OzN3IN88US=> NHv3dVdUSU6JRWK=
OS-RC-2 M3nWe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIn2bYhKSzVyPUGuPVkyQTlizszN NHfSVXpUSU6JRWK=
TE-1 NYjNOY9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjXWnFKSzVyPUKuNFQ5OyEQvF2= NITjdZlUSU6JRWK=
RL95-2 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDFW|BnUUN3ME2zMlE2PjdizszN MW\TRW5ITVJ?
LS-513 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDUS3NbUUN3ME2zMlQxODRzIN88US=> NVznXnp2W0GQR1XS
DJM-1 NWXEdJRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f6O2lEPTB;Mz60Olk4PSEQvF2= NXfuS3VuW0GQR1XS
NMC-G1 NETlU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\KW5NKSzVyPUOuOVQ2ODFizszN NEK3dI5USU6JRWK=
TE-10 NFnEcJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3fnFKSzVyPUOuOVU{PTZizszN MUjTRW5ITVJ?
TE-5 Mor0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTRwMEO3N{DPxE1? NUnTe|JCW0GQR1XS
TK10 NXv5e41kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlztTWM2OD12LkG2OVIzKM7:TR?= NH3HSGpUSU6JRWK=
UACC-812 NXvCdZhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[5OXFKSzVyPUSuOVYyPTNizszN MVXTRW5ITVJ?
SW962 NX30V25VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\WZZFkUUN3ME21MlAzOTV7IN88US=> MYXTRW5ITVJ?
SW954 Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\JSmlEPTB;NT6zPVI1PSEQvF2= MonjV2FPT0WU
COLO-668 NWXiVINOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L6XWlEPTB;NT63NlY3PyEQvF2= Ml3vV2FPT0WU
LB1047-RCC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITqUWhKSzVyPUWuPFAxPDZizszN M{\NW3NCVkeHUh?=
NB5 NWnENHo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnOTWM2OD14LkKxNFAyKM7:TR?= NELoOndUSU6JRWK=
NTERA-S-cl-D1 NWfQdFJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoGwTWM2OD14LkK2OVYyKM7:TR?= M372T3NCVkeHUh?=
IST-MEL1 M3LuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\CTWM2OD14LkSzOlk1KM7:TR?= MUnTRW5ITVJ?
GI-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTZwNUG2PFIh|ryP Mlq3V2FPT0WU
TGBC1TKB NVHRVYc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TQVGlEPTB;Nz6wO|E5OyEQvF2= MYTTRW5ITVJ?
GT3TKB Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq2TWM2OD15LkKyO|Q1KM7:TR?= M3n2R3NCVkeHUh?=
EVSA-T NEnL[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e4eGlEPTB;Nz60NlgyOSEQvF2= M{K4[XNCVkeHUh?=
D-502MG M2fGdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHmVIFHUUN3ME23MlQ5QDl2IN88US=> NVywT4lyW0GQR1XS
TE-8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPpTWM2OD15Lke2NVU6KM7:TR?= MWrTRW5ITVJ?
OVCAR-4 NInReYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rCPWlEPTB;OT6xNVY4PSEQvF2= M3XuTHNCVkeHUh?=
D-336MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HhNmlEPTB;OT60O|M6PSEQvF2= M2Lw[nNCVkeHUh?=
GCIY MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG5TWM2OD17LkW3OFIh|ryP NHz5[YlUSU6JRWK=
KS-1 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nt[mlEPTB;OT62OlI5PyEQvF2= NVTOcVFuW0GQR1XS
HCC2998 MmftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTCelJ3UUN3ME25Mlk3OzB5IN88US=> MnrrV2FPT0WU
D-247MG M{TCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnXTWM2OD17Lkm4NlkyKM7:TR?= M4jKSHNCVkeHUh?=
TE-15 NXiwfFJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHRXG9KSzVyPUGwMlI1PSEQvF2= Mnz4V2FPT0WU
IST-MES1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHPTWM2OD1zMD6yOVY2KM7:TR?= NHP5R4xUSU6JRWK=
ETK-1 NH[5OIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHzOoJDUUN3ME2xNE43OjNizszN MXPTRW5ITVJ?
RCC10RGB MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HZe2lEPTB;MUCuPVYyKM7:TR?= M4rpR3NCVkeHUh?=
KNS-42 NGi4WoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFzLkeyOVUh|ryP MnHxV2FPT0WU
LB771-HNC NVvIZYlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXCWIRKSzVyPUGyMlE4OTJizszN M13NTnNCVkeHUh?=
SR MoHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HueGlEPTB;MUKuNlA3PCEQvF2= MXvTRW5ITVJ?
NCI-H1355 M3PrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPuV|ZKSzVyPUGyMlg6QDVizszN MXrTRW5ITVJ?
ES6 MlHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTF|LkC3PEDPxE1? NV6wSo1PW0GQR1XS
SK-NEP-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECzPFFKSzVyPUGzMlI2PzdizszN M3\vbHNCVkeHUh?=
D-392MG NHvOT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITXUWxKSzVyPUGzMlY1OjhizszN NEHR[JhUSU6JRWK=
NB7 NFLue2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPuVJpmUUN3ME2xOE4zOzd2IN88US=> M{T3[nNCVkeHUh?=
SK-LMS-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF2LkWxOFUh|ryP MlO4V2FPT0WU
SK-UT-1 M4LZSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\UXG1MUUN3ME2xOE44QDh7IN88US=> MX3TRW5ITVJ?
CA46 NWDEeG1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPGTWM2OD1zNT6wOVg3KM7:TR?= MWDTRW5ITVJ?
IST-SL2 NXTxbZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f2N2lEPTB;MUWuNVkxOSEQvF2= NHz6XFRUSU6JRWK=
BC-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF3LkOzNVQh|ryP MUHTRW5ITVJ?
LS-123 M1eycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rLb2lEPTB;MUWuPFE4OyEQvF2= M4Dr[XNCVkeHUh?=
Ramos-2G6-4C10 NUnpPY5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2qweGlEPTB;MU[uNFkzPCEQvF2= NFPWeWZUSU6JRWK=
MZ1-PC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET0PIZKSzVyPUG2Mlc{OTNizszN M2C1TnNCVkeHUh?=
LB647-SCLC NXTHUnlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF4LkmzO|Ih|ryP M4XINXNCVkeHUh?=
NCI-H1694 NYTyRYM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzvbYJEUUN3ME2xO{4yPTJ7IN88US=> M3XOfnNCVkeHUh?=
NCI-H322M MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTF5LkSzOlYh|ryP M4n5U3NCVkeHUh?=
ES7 Ml;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX5TohKSzVyPUG4MlM6OTRizszN M1vFPXNCVkeHUh?=
LC-2-ad NEfMfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i5eGlEPTB;MUiuOFM5PiEQvF2= M3X1S3NCVkeHUh?=
SF268 M2LuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTF6Lke0NFkh|ryP M2HObXNCVkeHUh?=
RPMI-8402 NGfEbVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPlS4lFUUN3ME2xPU4xPzR{IN88US=> M1no[XNCVkeHUh?=
HCE-T M2DxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTtSYxKSzVyPUKwMlI{PDRizszN MmLpV2FPT0WU
A101D NHnZTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnlUG5KUUN3ME2yNE45PTh5IN88US=> MVnTRW5ITVJ?
MRK-nu-1 NXHROm9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHoTWM2OD1{MD65NVMh|ryP MmfRV2FPT0WU
LXF-289 M1;CbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPIS|ltUUN3ME2yNU4xOzhizszN M2i0NnNCVkeHUh?=
NALM-6 NXfJXZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLpNlVxUUN3ME2yNU4yQTZ5IN88US=> M4ew[HNCVkeHUh?=
DOHH-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnroTWM2OD1{MT60PFE{KM7:TR?= MmPiV2FPT0WU
EW-16 NX3xd|RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nxO2lEPTB;MkKuNVQxOiEQvF2= NVLlR3JtW0GQR1XS
A4-Fuk MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojoTWM2OD1{Mj6yNVQ6KM7:TR?= MXHTRW5ITVJ?
HD-MY-Z NGrORnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ{LkO5OlUh|ryP NYfFfZJSW0GQR1XS
SKM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi4boY3UUN3ME2yNk44OzVzIN88US=> NF7zUm1USU6JRWK=
DMS-153 NWLESlNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DXbWlEPTB;MkOuOFIxPCEQvF2= MXXTRW5ITVJ?
LB373-MEL-D NYTZcGp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DUTWlEPTB;MkOuOVQ2OiEQvF2= MmrRV2FPT0WU
LP-1 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\BTWM2OD1{Mz64NFk4KM7:TR?= MYPTRW5ITVJ?
GI-ME-N NXjtPW81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTPVHZIUUN3ME2yOE4zQTJizszN M3PXfXNCVkeHUh?=
MPP-89 NXHueXBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTJ3LkKwN|Yh|ryP MYnTRW5ITVJ?
U-698-M NW\5fYJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXScGlKSzVyPUK1MlI2ODNizszN MV3TRW5ITVJ?
HC-1 M4Hsdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ3Lk[0NVgh|ryP NUO0Z4JKW0GQR1XS
HCC2157 MmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ3Lk[3N{DPxE1? M3uyfnNCVkeHUh?=
MOLT-4 NVe0SIh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqxTWM2OD1{Nj6yO|Mh|ryP M4nIWXNCVkeHUh?=
LS-411N NU\u[ZdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfHO2pKSzVyPUK2MlM{PjlizszN MYDTRW5ITVJ?
Becker M2PqVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH1fIhKSzVyPUK2MlUyQDFizszN MlPSV2FPT0WU
NCI-H23 NV\XUpJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJ4Lke1O|Uh|ryP NWPMXmM4W0GQR1XS
IST-SL1 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LidGlEPTB;MkeuN|g3PyEQvF2= NIG4Wm5USU6JRWK=
MZ2-MEL MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvPTWM2OD1{Nz60OVY3KM7:TR?= M4[wfHNCVkeHUh?=
RKO NUn4R21UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XqPWlEPTB;MkiuNVQ1PiEQvF2= NWrTRY8yW0GQR1XS
TE-441-T MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn73TWM2OD1{OD63PFkh|ryP M3zSXXNCVkeHUh?=
EW-24 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPkd3ZKSzVyPUK5MlEzPTlizszN MnW3V2FPT0WU
no-10 NYi3W2RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJ7LkG2N|Eh|ryP NUjRUZFDW0GQR1XS
D-542MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJ7LkmyNlEh|ryP NECyeo1USU6JRWK=
ST486 NHHYe|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XnNWlEPTB;M{CuOlQ2OSEQvF2= NFT4UHhUSU6JRWK=
KURAMOCHI MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTNyLkiwOVch|ryP NHLLWWdUSU6JRWK=
ES8 NGLwWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrYV4VKSzVyPUOxMlU6PzJizszN M336XXNCVkeHUh?=
BL-41 M4[5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13hS2lEPTB;M{KuNVA2PCEQvF2= NGPnemJUSU6JRWK=
NB6 M4PGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPQU2tXUUN3ME2zNk4{QDV3IN88US=> NEnMbWNUSU6JRWK=
NCI-H1304 M{HZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTN{LkS5Olch|ryP NIXOOWpUSU6JRWK=
MS-1 M{PY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTGboNKSzVyPUOyMlc4PTFizszN MoezV2FPT0WU
MFH-ino MkfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzhOoxKSzVyPUO0MlMzOjRizszN NUHVNVdZW0GQR1XS
NOS-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTN2Lk[3OFgh|ryP M4j4bnNCVkeHUh?=
HUTU-80 Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorOTWM2OD1|NT6zOlY4KM7:TR?= M4\QdHNCVkeHUh?=
EB2 MmS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i1Z2lEPTB;M{[uOlE5QSEQvF2= NYH2fpE5W0GQR1XS
L-540 NUP2fmZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfHZ4FbUUN3ME2zO{4zOzB6IN88US=> MVjTRW5ITVJ?
NCI-H747 MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3jRmFKSzVyPUO4Mlg5PDZizszN MoDLV2FPT0WU
NCI-H446 NV\BU2tQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTN7Lkm2OVEh|ryP MV3TRW5ITVJ?
MOLT-16 M{Dr[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3WcXRPUUN3ME20Nk41OTVizszN NU\sV|JlW0GQR1XS
BC-3 NVfZ[XlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e5T2lEPTB;NEWuOFg6PiEQvF2= NFXUZlBUSU6JRWK=
SJSA-1 MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPoelRoUUN3ME20OU42PDd2IN88US=> MULTRW5ITVJ?
BB65-RCC M3m1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vTVGlEPTB;NEWuOlY3KM7:TR?= NI\WTnZUSU6JRWK=
SNB75 M2THZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKwVJJMUUN3ME20Ok4xOThizszN NUXlU2NYW0GQR1XS

... 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
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2
NCT03080805 Recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co. Ltd. May 3 2017 Phase 3
NCT03084939 Recruiting Breast Cancer Hoffmann-La Roche April 24 2017 Phase 3
NCT03085368 Recruiting HER2-positive Breast Cancer Peking Union Medical College Hospital|EddingPharm Oncology Co. LTD. March 1 2017 Phase 2|Phase 3
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|Phase 2

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