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 87 Publications

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 NX;GVGkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fzbmlEPTB;MD6wNlU1PCEQvF2= MoHYV2FPT0WU
HCC2218 NIf0WVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpTWM2OD1yLkC1N|I3KM7:TR?= NIe0PZlUSU6JRWK=
OCUB-M M13ISmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFewVoNKSzVyPUCuNFU4PCEQvF2= MlXlV2FPT0WU
ECC12 M2PmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXQd2Z3UUN3ME2wMlA6OjNzIN88US=> M3KzUnNCVkeHUh?=
DSH1 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMEmzPVYh|ryP NWTqOlhyW0GQR1XS
BT-474 MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL6dVdXUUN3ME2wMlIyOzF3IN88US=> NX3HS4VNW0GQR1XS
BB30-HNC MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMkS2OVQh|ryP MlmzV2FPT0WU
EKVX NIP3[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL4WIFJUUN3ME2wMlQ1QDd2IN88US=> Ml[4V2FPT0WU
TE-12 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z0dmlEPTB;MD60PVA2PyEQvF2= NIDTfY9USU6JRWK=
A388 NITQbGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYm1SJlSUUN3ME2wMlczOjV6IN88US=> NWqzN2MyW0GQR1XS
TE-9 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnVcmtuUUN3ME2wMlc1PDV|IN88US=> M2D4OHNCVkeHUh?=
LB2241-RCC MnzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXaSVhTUUN3ME2xMlE2PDB|IN88US=> MnPjV2FPT0WU
LB996-RCC NVO0SY5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwM{[yNlgh|ryP M1vrdXNCVkeHUh?=
LC-1F NYr5O3J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnOyTWM2OD1zLkO4NlQ1KM7:TR?= MXHTRW5ITVJ?
TE-6 NXnDe5JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n0e2lEPTB;MT61OVIxOSEQvF2= NFLtRmdUSU6JRWK=
A253 M4LJSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;ORWlEPTB;MT65O|M{PSEQvF2= MUPTRW5ITVJ?
OS-RC-2 NYrlWWs1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwOUmxPVkh|ryP M3[zZ3NCVkeHUh?=
TE-1 NF\Be2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTOSmxxUUN3ME2yMlA1QDNizszN MVnTRW5ITVJ?
RL95-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPrTWM2OD1|LkG1Olch|ryP NUTjZoE3W0GQR1XS
LS-513 M3jQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S4V2lEPTB;Mz60NFA1OSEQvF2= NHLMb5RUSU6JRWK=
DJM-1 NHTYNHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TtRmlEPTB;Mz60Olk4PSEQvF2= NWjnfHNrW0GQR1XS
NMC-G1 NEXKSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrWXZp1UUN3ME2zMlU1PTBzIN88US=> NInsdJBUSU6JRWK=
TE-10 MmHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG5PINbUUN3ME2zMlU2OzV4IN88US=> MlmwV2FPT0WU
TE-5 M3G4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTRwMEO3N{DPxE1? NIiyXlhUSU6JRWK=
TK10 MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfFTYpKSzVyPUSuNVY2OjJizszN MWDTRW5ITVJ?
UACC-812 NGraT2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\1do5KSzVyPUSuOVYyPTNizszN MVjTRW5ITVJ?
SW962 NWjJ[WFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;0VmlEPTB;NT6wNlE2QSEQvF2= MXzTRW5ITVJ?
SW954 NF76Oo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvKZnBKSzVyPUWuN|kzPDVizszN NY\IbVA{W0GQR1XS
COLO-668 NVHmeJJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGH2XZVKSzVyPUWuO|I3PjdizszN M{OzdXNCVkeHUh?=
LB1047-RCC M2\RTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTVwOECwOFYh|ryP NIS1cXFUSU6JRWK=
NB5 NVfob5VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fPXGlEPTB;Nj6yNVAxOSEQvF2= NYC0eJFYW0GQR1XS
NTERA-S-cl-D1 MnHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLXTWM2OD14LkK2OVYyKM7:TR?= M3ezTHNCVkeHUh?=
IST-MEL1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTlTWM2OD14LkSzOlk1KM7:TR?= NXHSZVY3W0GQR1XS
GI-1 NW\pRYVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGf4N4lKSzVyPU[uOVE3QDJizszN M13tUXNCVkeHUh?=
TGBC1TKB NGP3T2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jqO2lEPTB;Nz6wO|E5OyEQvF2= NIfDVJFUSU6JRWK=
GT3TKB MlrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofWTWM2OD15LkKyO|Q1KM7:TR?= MmHUV2FPT0WU
EVSA-T MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK4TVd{UUN3ME23MlQzQDFzIN88US=> MUHTRW5ITVJ?
D-502MG Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXoXG9DUUN3ME23MlQ5QDl2IN88US=> NX\6dWpHW0GQR1XS
TE-8 M4rHPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfmTWM2OD15Lke2NVU6KM7:TR?= NVflTmVHW0GQR1XS
OVCAR-4 NVXkbWRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLmdZBNUUN3ME25MlEyPjd3IN88US=> M{PkOXNCVkeHUh?=
D-336MG MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVSzZZdVUUN3ME25MlQ4Ozl3IN88US=> MoHaV2FPT0WU
GCIY NUj0TpZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrL[GtKSzVyPUmuOVc1OiEQvF2= NYPmXIQ6W0GQR1XS
KS-1 NYjHXno6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LDfmlEPTB;OT62OlI5PyEQvF2= M3v2OXNCVkeHUh?=
HCC2998 NWfPeHJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG0TWM2OD17Lkm2N|A4KM7:TR?= MkHzV2FPT0WU
D-247MG MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFeyS3hKSzVyPUmuPVgzQTFizszN NX[0[mNpW0GQR1XS
TE-15 M{PqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjDdWF7UUN3ME2xNE4zPDVizszN NGPpS3FUSU6JRWK=
IST-MES1 NHHwdpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW2TWM2OD1zMD6yOVY2KM7:TR?= MXnTRW5ITVJ?
ETK-1 M2fROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v0ZWlEPTB;MUCuOlI{KM7:TR?= MnTmV2FPT0WU
RCC10RGB MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTsRmxKSzVyPUGwMlk3OSEQvF2= MkXoV2FPT0WU
KNS-42 M{XTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXaTWM2OD1zMT63NlU2KM7:TR?= NF[2eWxUSU6JRWK=
LB771-HNC MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHtTWM2OD1zMj6xO|EzKM7:TR?= MnvwV2FPT0WU
SR NWjiZWE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF{LkKwOlQh|ryP MkDHV2FPT0WU
NCI-H1355 NXzUSWNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfr[GZEUUN3ME2xNk45QTh3IN88US=> MmCzV2FPT0WU
ES6 NUDw[5hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHMVIV[UUN3ME2xN{4xPzhizszN Mn;sV2FPT0WU
SK-NEP-1 NYLGOmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jMT2lEPTB;MUOuNlU4PyEQvF2= NULs[2tjW0GQR1XS
D-392MG M4[1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfWRZl3UUN3ME2xN{43PDJ6IN88US=> MX3TRW5ITVJ?
NB7 NVHvU5kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPrTWM2OD1zND6yN|c1KM7:TR?= M37Vc3NCVkeHUh?=
SK-LMS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPiTWM2OD1zND61NVQ2KM7:TR?= MVnTRW5ITVJ?
SK-UT-1 MkTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPmOHFKSzVyPUG0Mlc5QDlizszN M1HiNHNCVkeHUh?=
CA46 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX71WVdJUUN3ME2xOU4xPTh4IN88US=> NGS2d5pUSU6JRWK=
IST-SL2 NGPrS5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTF3LkG5NFEh|ryP MVzTRW5ITVJ?
BC-1 M3HafWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmraTWM2OD1zNT6zN|E1KM7:TR?= MnPRV2FPT0WU
LS-123 NHXo[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm2TWM2OD1zNT64NVc{KM7:TR?= MUHTRW5ITVJ?
Ramos-2G6-4C10 MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C5ZmlEPTB;MU[uNFkzPCEQvF2= M3;WfHNCVkeHUh?=
MZ1-PC NVjmW4dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nu[2lEPTB;MU[uO|MyOyEQvF2= MUjTRW5ITVJ?
LB647-SCLC M4D2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLhTWM2OD1zNj65N|czKM7:TR?= MoLPV2FPT0WU
NCI-H1694 NFPobG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\0OWlEPTB;MUeuNVUzQSEQvF2= NGr3R4ZUSU6JRWK=
NCI-H322M NXGyPZVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mor0TWM2OD1zNz60N|Y3KM7:TR?= M2HtV3NCVkeHUh?=
ES7 MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vKcWlEPTB;MUiuN|kyPCEQvF2= NIHr[JhUSU6JRWK=
LC-2-ad Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnOTWM2OD1zOD60N|g3KM7:TR?= NX;HTXc2W0GQR1XS
SF268 MknDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED6N|NKSzVyPUG4Mlc1ODlizszN MorKV2FPT0WU
RPMI-8402 NG\IRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHIeYxwUUN3ME2xPU4xPzR{IN88US=> MXHTRW5ITVJ?
HCE-T NW\tOGplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq0UnBlUUN3ME2yNE4zOzR2IN88US=> NXjhV|ExW0GQR1XS
A101D NHq1N4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfnbYdKSzVyPUKwMlg2QDdizszN NHPmb5VUSU6JRWK=
MRK-nu-1 NYT4TIc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zCT2lEPTB;MkCuPVE{KM7:TR?= M{W3[3NCVkeHUh?=
LXF-289 Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXuyRmtjUUN3ME2yNU4xOzhizszN NV65fHMzW0GQR1XS
NALM-6 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm4TWM2OD1{MT6xPVY4KM7:TR?= NVnmfmM3W0GQR1XS
DOHH-2 M4Tsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHRVGViUUN3ME2yNU41QDF|IN88US=> M{LPcHNCVkeHUh?=
EW-16 NFLxR2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJ{LkG0NFIh|ryP MlTuV2FPT0WU
A4-Fuk M3vXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHqTWM2OD1{Mj6yNVQ6KM7:TR?= MWPTRW5ITVJ?
HD-MY-Z NFzzWopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\mc2lEPTB;MkKuN|k3PSEQvF2= M{fzOHNCVkeHUh?=
SKM-1 NWXPR21xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrZXJRWUUN3ME2yNk44OzVzIN88US=> MUnTRW5ITVJ?
DMS-153 NWTod2JFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX24U5ZZUUN3ME2yN{41OjB2IN88US=> NX3adm1QW0GQR1XS
LB373-MEL-D NEfCW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvsU2hZUUN3ME2yN{42PDV{IN88US=> M{C4XHNCVkeHUh?=
LP-1 NIG5cWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPTTWM2OD1{Mz64NFk4KM7:TR?= NIjZb3ZUSU6JRWK=
GI-ME-N MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7PdGJFUUN3ME2yOE4zQTJizszN NXGzUJlPW0GQR1XS
MPP-89 NIriNZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DXOGlEPTB;MkWuNlA{PiEQvF2= NHfqZXRUSU6JRWK=
U-698-M NF;TUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz2bYVoUUN3ME2yOU4zPTB|IN88US=> NWXVVmVvW0GQR1XS
HC-1 Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTnTWM2OD1{NT62OFE5KM7:TR?= M3vKOHNCVkeHUh?=
HCC2157 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXKZmcyUUN3ME2yOU43PzNizszN NUHI[pBtW0GQR1XS
MOLT-4 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ4LkK3N{DPxE1? M{fDbnNCVkeHUh?=
LS-411N Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUK1TG9zUUN3ME2yOk4{OzZ7IN88US=> MXfTRW5ITVJ?
Becker MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITaWpNKSzVyPUK2MlUyQDFizszN NVjUSGs3W0GQR1XS
NCI-H23 M4HNWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3iw[2lEPTB;Mk[uO|U4PSEQvF2= MnTwV2FPT0WU
IST-SL1 NXPX[GdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULB[WdGUUN3ME2yO{4{QDZ5IN88US=> MlfiV2FPT0WU
MZ2-MEL NG[wZ2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJ5LkS1OlYh|ryP NEnGN|VUSU6JRWK=
RKO MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HsTWlEPTB;MkiuNVQ1PiEQvF2= MlHxV2FPT0WU
TE-441-T MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fDTmlEPTB;MkiuO|g6KM7:TR?= M4K0eHNCVkeHUh?=
EW-24 MnzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDYVYpiUUN3ME2yPU4yOjV7IN88US=> M3O2fXNCVkeHUh?=
no-10 MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u2SmlEPTB;MkmuNVY{OSEQvF2= MXfTRW5ITVJ?
D-542MG M1zPU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ7LkmyNlEh|ryP MUPTRW5ITVJ?
ST486 MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrvPIdKSzVyPUOwMlY1PTFizszN MUPTRW5ITVJ?
KURAMOCHI NX3Lc5Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\2[GRKSzVyPUOwMlgxPTdizszN NE\ReolUSU6JRWK=
ES8 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4WzUGlEPTB;M{GuOVk4OiEQvF2= M2jRU3NCVkeHUh?=
BL-41 NXvCOldUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rhd2lEPTB;M{KuNVA2PCEQvF2= MY\TRW5ITVJ?
NB6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\FZ41TUUN3ME2zNk4{QDV3IN88US=> NYHH[ZlKW0GQR1XS
NCI-H1304 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDXTHBKSzVyPUOyMlQ6PjdizszN M{\kXXNCVkeHUh?=
MS-1 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTN{Lke3OVEh|ryP Mn;uV2FPT0WU
MFH-ino MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofHTWM2OD1|ND6zNlI1KM7:TR?= MUjTRW5ITVJ?
NOS-1 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN2Lk[3OFgh|ryP NXPKOXNYW0GQR1XS
HUTU-80 MnXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXyc29KSzVyPUO1MlM3PjdizszN NIHBd|FUSU6JRWK=
EB2 M363fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTN4Lk[xPFkh|ryP MlTyV2FPT0WU
L-540 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTN5LkKzNFgh|ryP NWP4cXcyW0GQR1XS
NCI-H747 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[zS2lEPTB;M{iuPFg1PiEQvF2= MYjTRW5ITVJ?
NCI-H446 NUnYPIpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jaPWlEPTB;M{muPVY2OSEQvF2= M{\1THNCVkeHUh?=
MOLT-16 NHW5SGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr2TYFKSzVyPUSyMlQyPSEQvF2= M{PLbXNCVkeHUh?=
BC-3 NGqwbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;ETopYUUN3ME20OU41QDl4IN88US=> NInjOVhUSU6JRWK=
SJSA-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XJUGlEPTB;NEWuOVQ4PCEQvF2= M{HoSXNCVkeHUh?=
BB65-RCC NYnhc|Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf0TWM2OD12NT62OlYh|ryP NIW2TXFUSU6JRWK=
SNB75 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTR4LkCxPEDPxE1? NEDMdINUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; 

PubMed: 29799521     


Downregulation of HSF1, mutp53, and Mdm2 in lapatinib-sensitive parental BT474, but not in lapatinib-resistant BT474R cells, treated with indicated lapatinib concentrations for 24 h.

pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP ; 

PubMed: 28938602     


SKBR3 and 78617 cells were treated with lapatinib as in panel A, then the expression of phospho-ErbB2 (Tyr1221/1222), ErbB2, phospho-EGFR (Tyr1068), EGFR, phospho-Akt (Ser473), Akt, phospho-Erk1/2 (Thr202/Tyr204), Erk2, phospho-mTOR (Ser2448), and mTOR were analyzed using Western blotting. 

p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1; 

PubMed: 22853430     


A panel of HER2-amplified breast cancer cells were treated with 200nM lapatinib for up to 72 hours to detect the initial downregulation and subsequent upregulation of HER2-HER3 and downstream signaling. Immunoblots were performed using the indicated antibodies.

29799521 28938602 22853430
Immunofluorescence
LC3 ; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 6 days and UACC893 GFP-LC3 cells were cultured for 7 days with 5 μM EZN3046 or EZN4150 .

Vimentin / E-cadherin; 

PubMed: 28243326     


Cells treated with lapatinib (5µM) increased the expression of E-cadherin and inhibited the expression of Vimentin by immunofluorescence. (Magnification: 1000×).

26637440 28243326
Growth inhibition assay
Cell viability (OE19); 

PubMed: 25350844     


Dose-response curves from escalated dose of lapatinib in the presence of 1 µM concentration of saracatinib. The calculated values of IC50 for lapatinib were following; 207.3 nM and 145 nM, respectively, after lapatinib alone and in the presence of saracatinib for parental OE19; >1,000 nM after lapatinib alone for LR2A and LR2B; 91.66 nM and 224.0 nM in the presence of saracatinib in LR2A and LR2B, respectively. Values were presented as relative cellular viability relative to vehicle-treated controls with the mean ± S.E. of quadruplicate from a representative experiment. The p values calculated by two-way ANOVA were <0.0001 comparing lapatinib alone with lapatinib plus saracatinib both in the LR2A and LR2B.

Cell viability (A431 cells); 

PubMed: 28243326     


The MTT assay was performed on the viability of A431 cells by lapatinib at different concentrations (0.1-50μM) and IC50 value was analyzed as indicated on the plot (t-test).

25350844 28243326
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)

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*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 )

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* 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

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  • Computed Result

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    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03075995 Unknown status Other: hight-fat breakfast Breast Cancer Sun Yat-sen University April 12 2017 Not Applicable
NCT02338245 Completed Drug: ASLAN001|Drug: Lapatinib|Drug: Capecitabine Metastatic Breast Cancer Aslan Pharmaceuticals December 29 2014 Phase 2
NCT02294786 Terminated Drug: Lapatinib|Drug: Capecitabine|Drug: Octreotide Cancer Novartis Pharmaceuticals|Novartis December 17 2014 Phase 2
NCT02213042 Active not recruiting Drug: Lapatinib|Biological: Trastuzumab Neoplasms Breast Novartis Pharmaceuticals|Novartis October 24 2014 Phase 2
NCT01782651 Completed Drug: Lapatinib plus capecitabine Neoplasms Breast GlaxoSmithKline August 2014 --
NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie July 2014 Not Applicable

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

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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