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 NYXmUIVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwMEK1OFQh|ryP M3vSUnNCVkeHUh?=
HCC2218 NWjObHoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DLVWlEPTB;MD6wOVMzPiEQvF2= MoLKV2FPT0WU
OCUB-M MkLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnoTWM2OD1yLkC1O|Qh|ryP M1[2eXNCVkeHUh?=
ECC12 M3jYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL1XJhKSzVyPUCuNFkzOzFizszN M3LIXHNCVkeHUh?=
DSH1 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;5TWM2OD1yLkC5N|k3KM7:TR?= MnPzV2FPT0WU
BT-474 MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMkGzNVUh|ryP NYTxV29uW0GQR1XS
BB30-HNC M2PGOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnPTWM2OD1yLkK0OlU1KM7:TR?= M3TsUXNCVkeHUh?=
EKVX NEC1bnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zCfWlEPTB;MD60OFg4PCEQvF2= MoC3V2FPT0WU
TE-12 NF:wOXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITiWJRKSzVyPUCuOFkxPTdizszN M4fybnNCVkeHUh?=
A388 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfyTWM2OD1yLkeyNlU5KM7:TR?= NGTiRXNUSU6JRWK=
TE-9 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fYW2lEPTB;MD63OFQ2OyEQvF2= MlviV2FPT0WU
LB2241-RCC NHjFXZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLpVGdYUUN3ME2xMlE2PDB|IN88US=> NXThfIlIW0GQR1XS
LB996-RCC MnP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknUTWM2OD1zLkO2NlI5KM7:TR?= MoXnV2FPT0WU
LC-1F MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFwM{iyOFQh|ryP M3LhTnNCVkeHUh?=
TE-6 NE[2e2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInmT2tKSzVyPUGuOVUzODFizszN NGjsfFJUSU6JRWK=
A253 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XlbmlEPTB;MT65O|M{PSEQvF2= NFXzN|hUSU6JRWK=
OS-RC-2 NF7Ge|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG3fItKSzVyPUGuPVkyQTlizszN NEH6d|JUSU6JRWK=
TE-1 NGXGOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\RZ2lEPTB;Mj6wOFg{KM7:TR?= MnzsV2FPT0WU
RL95-2 Mk\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2n4[WlEPTB;Mz6xOVY4KM7:TR?= MorJV2FPT0WU
LS-513 NIS4e4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTNwNECwOFEh|ryP NWS2U|RPW0GQR1XS
DJM-1 M{nYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXqTJJKSzVyPUOuOFY6PzVizszN MojUV2FPT0WU
NMC-G1 MmPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTNwNUS1NFEh|ryP MlLwV2FPT0WU
TE-10 MnjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNwNUWzOVYh|ryP M1HsOXNCVkeHUh?=
TE-5 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILIfJFKSzVyPUSuNFM4OyEQvF2= M1voSnNCVkeHUh?=
TK10 M2LuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnSTWM2OD12LkG2OVIzKM7:TR?= NF;6XJpUSU6JRWK=
UACC-812 NV\3WopTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\LTWM2OD12LkW2NVU{KM7:TR?= M4jveXNCVkeHUh?=
SW962 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DJfWlEPTB;NT6wNlE2QSEQvF2= NVO0dJdyW0GQR1XS
SW954 NHL2OnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljITWM2OD13LkO5NlQ2KM7:TR?= M1LQRnNCVkeHUh?=
COLO-668 NV;DNWxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17pTGlEPTB;NT63NlY3PyEQvF2= NYXxeZdsW0GQR1XS
LB1047-RCC MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LvbmlEPTB;NT64NFA1PiEQvF2= NYnmZohlW0GQR1XS
NB5 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnpWoRKSzVyPU[uNlExODFizszN NF;GU|BUSU6JRWK=
NTERA-S-cl-D1 MlrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\y[WlEPTB;Nj6yOlU3OSEQvF2= MXjTRW5ITVJ?
IST-MEL1 M1TqUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnMe|hKSzVyPU[uOFM3QTRizszN NFTjPYJUSU6JRWK=
GI-1 MkiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXS2XHVxUUN3ME22MlUyPjh{IN88US=> NVrDdHF7W0GQR1XS
TGBC1TKB M1X5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;wR5RKSzVyPUeuNFcyQDNizszN NVfndI53W0GQR1XS
GT3TKB MkP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vS[2lEPTB;Nz6yNlc1PCEQvF2= NHPqWFZUSU6JRWK=
EVSA-T NH3HfGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSzZ3FJUUN3ME23MlQzQDFzIN88US=> MlX0V2FPT0WU
D-502MG M2rWOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q1cWlEPTB;Nz60PFg6PCEQvF2= MoHRV2FPT0WU
TE-8 NWTJXIZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH3THgyUUN3ME23Mlc3OTV7IN88US=> NVjDPFZmW0GQR1XS
OVCAR-4 M{nvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\3cYhoUUN3ME25MlEyPjd3IN88US=> MlnFV2FPT0WU
D-336MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSxXHBKSzVyPUmuOFc{QTVizszN NWjKSlhMW0GQR1XS
GCIY M3\Vdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjlcVRKSzVyPUmuOVc1OiEQvF2= MlyyV2FPT0WU
KS-1 NXLncGEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDmTWM2OD17Lk[2Nlg4KM7:TR?= M1nF[HNCVkeHUh?=
HCC2998 MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnnUXliUUN3ME25Mlk3OzB5IN88US=> NXrHO4ROW0GQR1XS
D-247MG NUnLWWpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLwPJNKSzVyPUmuPVgzQTFizszN MnfhV2FPT0WU
TE-15 MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[0W2lEPTB;MUCuNlQ2KM7:TR?= NI\ifWFUSU6JRWK=
IST-MES1 NUXEOpFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHYdXFKSzVyPUGwMlI2PjVizszN NIfiXnBUSU6JRWK=
ETK-1 M{TifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHZcpVKSzVyPUGwMlYzOyEQvF2= NVTqZ3l4W0GQR1XS
RCC10RGB NXG1OFhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITjc5hKSzVyPUGwMlk3OSEQvF2= MXXTRW5ITVJ?
KNS-42 NInNe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;FOWlEPTB;MUGuO|I2PSEQvF2= MWjTRW5ITVJ?
LB771-HNC MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfVOY5KSzVyPUGyMlE4OTJizszN NGDmV2RUSU6JRWK=
SR NUPjRWV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zvSWlEPTB;MUKuNlA3PCEQvF2= NHPKXHlUSU6JRWK=
NCI-H1355 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF{Lki5PFUh|ryP M3zRZXNCVkeHUh?=
ES6 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;oN|lKSzVyPUGzMlA4QCEQvF2= M3u4fHNCVkeHUh?=
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDMTJJ2UUN3ME2xN{4zPTd5IN88US=> NFzp[|VUSU6JRWK=
D-392MG M1;qUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF|Lk[0Nlgh|ryP NEXtVnFUSU6JRWK=
NB7 NXvOT5N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LObmlEPTB;MUSuNlM4PCEQvF2= NXzTOYJDW0GQR1XS
SK-LMS-1 NXviTVhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTF2LkWxOFUh|ryP MoCwV2FPT0WU
SK-UT-1 M3Pyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXW4NYMyUUN3ME2xOE44QDh7IN88US=> MYjTRW5ITVJ?
CA46 M{L5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTF3LkC1PFYh|ryP NH3GVJZUSU6JRWK=
IST-SL2 NITveIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLDPVlMUUN3ME2xOU4yQTBzIN88US=> MXLTRW5ITVJ?
BC-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfJNJpKSzVyPUG1MlM{OTRizszN NGjLZlhUSU6JRWK=
LS-123 NFn2UWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnThTWM2OD1zNT64NVc{KM7:TR?= MXPTRW5ITVJ?
Ramos-2G6-4C10 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvMRVJGUUN3ME2xOk4xQTJ2IN88US=> MXPTRW5ITVJ?
MZ1-PC M4TsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLCZYhxUUN3ME2xOk44OzF|IN88US=> Mnv3V2FPT0WU
LB647-SCLC NUfRbIxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF4LkmzO|Ih|ryP Ml7DV2FPT0WU
NCI-H1694 NVvBW2NET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfNVGtjUUN3ME2xO{4yPTJ7IN88US=> MWDTRW5ITVJ?
NCI-H322M M4nleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\IWnpjUUN3ME2xO{41OzZ4IN88US=> M4DKOnNCVkeHUh?=
ES7 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF6LkO5NVQh|ryP NEfxTJZUSU6JRWK=
LC-2-ad M1PaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF6LkSzPFYh|ryP MonrV2FPT0WU
SF268 NITmVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLEOFVKSzVyPUG4Mlc1ODlizszN NXX5U2RJW0GQR1XS
RPMI-8402 NWrYRVQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXu4foMxUUN3ME2xPU4xPzR{IN88US=> MVzTRW5ITVJ?
HCE-T NWrmdVI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXOSGhrUUN3ME2yNE4zOzR2IN88US=> MVnTRW5ITVJ?
A101D MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHuTWM2OD1{MD64OVg4KM7:TR?= MmTaV2FPT0WU
MRK-nu-1 MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLBZ|UxUUN3ME2yNE46OTNizszN Ml[yV2FPT0WU
LXF-289 NFrJb5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJzLkCzPEDPxE1? MXjTRW5ITVJ?
NALM-6 NYrIZ4pHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDHTWM2OD1{MT6xPVY4KM7:TR?= NIC3OGNUSU6JRWK=
DOHH-2 NYmyNVRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJzLkS4NVMh|ryP MYPTRW5ITVJ?
EW-16 M{OybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTJ{LkG0NFIh|ryP NXjSOlZmW0GQR1XS
A4-Fuk NFjzXpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJ{LkKxOFkh|ryP MV;TRW5ITVJ?
HD-MY-Z M3TPTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjKcpZuUUN3ME2yNk4{QTZ3IN88US=> NIrneG1USU6JRWK=
SKM-1 NE\OU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HneWlEPTB;MkKuO|M2OSEQvF2= NH\lVG1USU6JRWK=
DMS-153 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z3d2lEPTB;MkOuOFIxPCEQvF2= NFnYR25USU6JRWK=
LB373-MEL-D M2nyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjifVhKSzVyPUKzMlU1PTJizszN M2\wNnNCVkeHUh?=
LP-1 MkXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTwXHE2UUN3ME2yN{45ODl5IN88US=> NVq3eoxOW0GQR1XS
GI-ME-N M3XOXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzUTWM2OD1{ND6yPVIh|ryP MWrTRW5ITVJ?
MPP-89 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r4VWlEPTB;MkWuNlA{PiEQvF2= MnHOV2FPT0WU
U-698-M M4PLXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXRTWM2OD1{NT6yOVA{KM7:TR?= NGW3e|lUSU6JRWK=
HC-1 NH\wWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETBb3dKSzVyPUK1MlY1OThizszN M4jjZXNCVkeHUh?=
HCC2157 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HlVmlEPTB;MkWuOlc{KM7:TR?= MX3TRW5ITVJ?
MOLT-4 NEW5XnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ4LkK3N{DPxE1? MnK5V2FPT0WU
LS-411N NXX0eGhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrYTWM2OD1{Nj6zN|Y6KM7:TR?= MkHNV2FPT0WU
Becker NWPlV5BMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPrVJhKSzVyPUK2MlUyQDFizszN MYjTRW5ITVJ?
NCI-H23 NYL5NmZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJ4Lke1O|Uh|ryP NHjzeXBUSU6JRWK=
IST-SL1 NHTkfohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vJUWlEPTB;MkeuN|g3PyEQvF2= NWG1c45uW0GQR1XS
MZ2-MEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3tTWM2OD1{Nz60OVY3KM7:TR?= NWXUWIUxW0GQR1XS
RKO M{XKW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLtW4VKSzVyPUK4MlE1PDZizszN NIfuTZVUSU6JRWK=
TE-441-T NXS2V5hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GwNGlEPTB;MkiuO|g6KM7:TR?= M2fGVXNCVkeHUh?=
EW-24 NH;yRYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrkRpZ7UUN3ME2yPU4yOjV7IN88US=> MUDTRW5ITVJ?
no-10 MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJ7LkG2N|Eh|ryP MWnTRW5ITVJ?
D-542MG NWn1blVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfCW4xKSzVyPUK5MlkzOjFizszN MmPEV2FPT0WU
ST486 NF:2SHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP3N4pKSzVyPUOwMlY1PTFizszN MUDTRW5ITVJ?
KURAMOCHI M4Hr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX5SVRpUUN3ME2zNE45ODV5IN88US=> MUTTRW5ITVJ?
ES8 NV;4VpBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof5TWM2OD1|MT61PVczKM7:TR?= MVrTRW5ITVJ?
BL-41 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\lUGlEPTB;M{KuNVA2PCEQvF2= MlS2V2FPT0WU
NB6 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDxTWM2OD1|Mj6zPFU2KM7:TR?= MnTlV2FPT0WU
NCI-H1304 NVryXWVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\UfmlEPTB;M{KuOFk3PyEQvF2= M4nyeHNCVkeHUh?=
MS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTN{Lke3OVEh|ryP NIXIT|lUSU6JRWK=
MFH-ino M3XJUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvLWmxJUUN3ME2zOE4{OjJ2IN88US=> NXPYNZZMW0GQR1XS
NOS-1 M1Xwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfxfVN1UUN3ME2zOE43PzR6IN88US=> M3T6dnNCVkeHUh?=
HUTU-80 NEe1e3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PyZWlEPTB;M{WuN|Y3PyEQvF2= NV30W|JUW0GQR1XS
EB2 MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;K[YVKSzVyPUO2MlYyQDlizszN NYT2Z5lCW0GQR1XS
L-540 M{XOV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTN5LkKzNFgh|ryP M{LGfXNCVkeHUh?=
NCI-H747 NIrZ[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTN6Lki4OFYh|ryP MUXTRW5ITVJ?
NCI-H446 Mlu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjhVm5KSzVyPUO5Mlk3PTFizszN M{PwfXNCVkeHUh?=
MOLT-16 NFPwfYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTR{LkSxOUDPxE1? MYDTRW5ITVJ?
BC-3 M{nLeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzWTWM2OD12NT60PFk3KM7:TR?= NXPm[5E5W0GQR1XS
SJSA-1 NWOyWZdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTR3LkW0O|Qh|ryP MUnTRW5ITVJ?
BB65-RCC NUT6bnlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O3SmlEPTB;NEWuOlY3KM7:TR?= NGLQ[|VUSU6JRWK=
SNB75 NXLVUGNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXaVlFKSzVyPUS2MlAyQCEQvF2= NUntfJR3W0GQR1XS

... 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
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
NCT02650752 Active not recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 6 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