Lapatinib (GW-572016) Ditosylate

Catalog No.S1028

Lapatinib (GW-572016) Ditosylate Chemical Structure

Molecular Weight(MW): 925.46

Lapatinib (GW-572016) 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 75 Publications

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Choose Selective HER2 Inhibitors

Biological Activity

Description Lapatinib (GW-572016) 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 Ditosylate 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 Ditosylate 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 Ditosylate inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib Ditosylate 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 Ditosylate 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
HN5 cell line NXrSUpdwWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4LKWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= MnLKNVY1QDN5N{K=
BT474 cell line MnezVJJwdGmoZYLheIlwdiCjc4PhfS=> MnHmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NXniUGJSOTZ2OEO3O|I>
HN5 cell NILLVlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TENWlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? NV7ocIhGOTZ5N{e0NVA>
BT474 cell M{HwZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYjzcFQ4UW6qaXLpeIlwdiCxZjDCWFQ4PCClZXzsJIdzd3e2aDDh[pRmeiB5MjDodpMtKEmFNUC9NE4xQCEQvF2= MoPONVY4Pzd2MUC=
N87 cell MkPTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLUTY5pcWKrdHnvckBw\iCQOEegZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEig{txO MVKxOlc4PzRzMB?=
HFF cell NFPYXJhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\rbod1UW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> NH\SVYgyPjd5N{SxNC=>
SKBR3 cells NWLvSldvS3m2b4TvfIlkcXS7IHHzd4F6 M2DCVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOTdizszN MkjkNVkxOjh2MkW=
A431 cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= M3\nb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlExPCEQvF2= MlS4NVk5QDh5NkG=
SKBR3 cells Mm\zR5l1d3SxeHnjbZR6KGG|c3H5 M2TpRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOjlizszN MnXnNVk5QDh5NkG=
HepG2 cells NH7pellRem:uaX\ldoF1cW:wIHHzd4F6 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME22MlI4KM7:TR?= M3nIblIxOTR|N{e4
Hep3B2 cells NFzaVHpRem:uaX\ldoF1cW:wIHHzd4F6 NX23U3dJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SjJiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNEmg{txO NX7nW4w4OjBzNEO3O|g>
SKHEP1 cells NIHpfZNRem:uaX\ldoF1cW:wIHHzd4F6 NEHYcmNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLTGVROSClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS5|IN88US=> NXrPWIxbOjBzNEO3O|g>
MCF7 cells NXW2eoZLWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVGwbY9wSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjZizszN MnLxNlAyPDN5N{i=
MDA-MB-231 cells NUC2OZFxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nZfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkBpenNiYomgRXRRKGOxboTlcpQh[XO|YYmsJGlEPTB;NT60JO69VQ>? NIPwRnQzODF2M{e3PC=>
SK-BR-3 cells M3m1RXBzd2yrZnXyZZRqd25iYYPzZZk> NYTjN5pLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJIhzeyCkeTDBWHAh[2:wdHXueEBie3OjeTygTWM2OD1yLkC0JO69VQ>? M1XPdVIxOTR|N{e4
A431 cells M4jIWmZ2dmO2aX;uJIF{e2G7 NVuwbIhoUW6qaXLpeIlwdiCxZjDFS2ZTKGmwdILhZ4VtdHWuYYKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFG0N|Eh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wOVIh|ryP M{HaNlIxOzR4NkW1
N87 cells MVnGeY5kfGmxbjDhd5NigQ>? M2HXdWlvcGmkaYTpc44hd2ZiRYLiRlIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTki3JINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMTFOwG0> MXKyNFM1PjZ3NR?=
MIAPaCa cells NIL3ZopHfW6ldHnvckBie3OjeR?= NGezSoFKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO MkDHNlA5OTd3MkO=
MIAPaCa cells M37xVGZ2dmO2aX;uJIF{e2G7 NGX1bZlKdmirYnn0bY9vKG:oIFXSRoIzKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOUUGSYVPhJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMUSg{txO MmnONlA5OTd3MkO=
CAL27 cells MlnWR5l1d3SxeHnjbZR6KGG|c3H5 NXz5RWlpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByNzFOwG0v MU[yNVA5ODZ{OR?=
SKOV3 cells NUO4XHRuS3m2b4TvfIlkcXS7IHHzd4F6 NES0cHFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJTVJ{IHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB|IN88UU4> NWTnOFJlOjFyOEC2Nlk>
CAL27 cells NXPSb5Z1TnWwY4Tpc44h[XO|YYm= MnrsNVYhcA>? NFK4SHZKdmirYnn0bY9vKG:oIFXHSk1qdmS3Y3XkJGVITlJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEODTEK3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKgZYZ1\XJiMU[gbJJ{KGK7IGfld5Rmem5iYnzveEwhUUN3ME2wMlA{OiEQvF2= M1zMZlIyODhyNkK5
SK-BR-3 cells M{XtZnBzd2yrZnXyZZRqd25iYYPzZZk> M3zIdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSZJjSjJib4\ldoV5eHKnc4PpcochcHWvYX6gV2suSlJvMzDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wN|Ih|ryP Mo\aNlE2PzB6NEO=
BXF T24 cells NHzaRohEgXSxdH;4bYNqfHliYYPzZZk> MWS0JIRigXN? M{\FT2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJZTiCWMkSgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPjVizszN NFjzN3UzOjF4OU[wNS=>
CXF 269L cells NYDYc5lbS3m2b4TvfIlkcXS7IHHzd4F6 NVq5OVVlPCCmYYnz NFzPeZREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEYEZiMk[5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:QC5|NjFOwG0> NYH1b|czOjJzNkm2NFE>
DIFI cells MlK4R5l1d3SxeHnjbZR6KGG|c3H5 NH;SVZk1KGSjeYO= NHv2OoxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFUU[LIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlI{PSEQvF2= NGmwb5QzOjF4OU[wNS=>
HT-29 cells NXzuNGQ5S3m2b4TvfIlkcXS7IHHzd4F6 MX60JIRigXN? MoHOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOlIh|ryP M1XGO|IzOTZ7NkCx
RKO cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= M4XWXFQh\GG7cx?= NHz2RXdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUWuN|Uh|ryP Mn74NlIyPjl4MEG=
GXF251L cells MW\DfZRwfG:6aXPpeJkh[XO|YYm= Mof5OEBl[Xm| M{DRbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN M2\IUlIzOTZ7NkCx
LIXF 575L cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= NHjjemI1KGSjeYO= M3y2U2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxKYEZiNUe1UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py5zODFOwG0> NUTNXHBkOjJzNkm2NFE>
LXFA 289L cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= NHHmWGk1KGSjeYO= NYPIfXlwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTCyPFlNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD13Lke5JO69VQ>? M{frelIzOTZ7NkCx
LXFA 526L MlvjR5l1d3SxeHnjbZR6KGG|c3H5 M{TCOVQh\GG7cx?= NV3XcnYxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC1NlZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkKxJO69VQ>? MnjTNlIyPjl4MEG=
LXFA 629L cells MoLWR5l1d3SxeHnjbZR6KGG|c3H5 MVm0JIRigXN? M2i0fGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiNkK5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Oi56NzFOwG0> NGXzS|gzOjF4OU[wNS=>
LXFL 1121L cells NHTabodEgXSxdH;4bYNqfHliYYPzZZk> NEKyWnU1KGSjeYO= NIr4T5REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[OIEGxNlFNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD15LkezJO69VQ>? NUDHNYZxOjJzNkm2NFE>
LXFL 529L cells MXrDfZRwfG:6aXPpeJkh[XO|YYm= NH;5bnU1KGSjeYO= MmrmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHVCB3MknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjVzIN88US=> MnjTNlIyPjl4MEG=
MCF7 cells MnPpR5l1d3SxeHnjbZR6KGG|c3H5 NEjGUlg1KGSjeYO= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkizJO69VQ>? MmDRNlIyPjl4MEG=
MDA231 cells MYHDfZRwfG:6aXPpeJkh[XO|YYm= M{PRVFQh\GG7cx?= MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEzOzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUeuO{DPxE1? MXiyNlE3QTZyMR?=
OVXF 899L MWLDfZRwfG:6aXPpeJkh[XO|YYm= NUKyXFZiPCCmYYnz MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWnhHKDh7OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvOzVizszN NGjTNmozOjF4OU[wNS=>
PAXF 546L cells MUfDfZRwfG:6aXPpeJkh[XO|YYm= NVrCNZhnPCCmYYnz NEDtSHhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSViIIEW0Omwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwMUKg{txO MVeyNlE3QTZyMR?=
PANC1 cells NFfU[4tEgXSxdH;4bYNqfHliYYPzZZk> MUO0JIRigXN? MmfXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFPSzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUiuNVIh|ryP MU[yNlE3QTZyMR?=
22Rv1 cell NH;PZlNEgXSxdH;4bYNqfHliYYPzZZk> M3nOflQh\GG7cx?= MkTsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNlJTfjFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPU[uNFYh|ryP NEPZd4MzOjF4OU[wNS=>
DU145 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= MU[0JIRigXN? NV61VllXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVIvQTlizszN MnfWNlIyPjl4MEG=
LNCAP cells MmjtR5l1d3SxeHnjbZR6KGG|c3H5 MmK0OEBl[Xm| NY[yVmsxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN M2PhXVIzOTZ7NkCx
PC3M cells Mk\ER5l1d3SxeHnjbZR6KGG|c3H5 Mkn3OEBl[Xm| NYXX[2FwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|TTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE42PSEQvF2= MUGyNlE3QTZyMR?=
NIH/3T3 cells NWHuZ|JqWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVu3NkBp MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12LkOg{txO NVvlfWd6OjJ3OUWxO|c>
NCI-H1648 cell NGrhXZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHfrXVdKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEK1OFQh|ryP M2i1eHNCVkeHUh?=
NMC-G1 cell NVTQe3J2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\VTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlU1PTBzIN88US=> M1PEenNCVkeHUh?=
NTERA-S-cl-D1 cell NXjaT5ViT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXO1TmxiUW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPjV4MTFOwG0> MWHTRW5ITVJ?
OCUB-M cell NIHL[ohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vvRWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTd2IN88US=> Mnv6V2FPT0WU
OS-RC-2 cell MmDYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;1SHJPUW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57OUG5PUDPxE1? M3ewOXNCVkeHUh?=
OVCAR-4 cell M2\VZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvSVFVKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjFzNke1JO69VQ>? Ml\yV2FPT0WU
RL95-2 cell NW\abG1qT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnvmTY5pcWKrdHnvckBw\iCqdX3hckBTVDl3LUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2PjdizszN MYPTRW5ITVJ?
SW954 cell NF3YSotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3ezZ2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6OjR3IN88US=> MUfTRW5ITVJ?
SW962 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= MV3TRW5ITVJ?
TE-1 cell NVjIOGV4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\WNGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNFIyPTlizszN MVPTRW5ITVJ?
A253 cell NH3RbppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGEzPTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP NVfseZg{W0GQR1XS
A388 cell M2jl[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP NVXxZ|VuW0GQR1XS
BB30-HNC cell M1zO[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3RTY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTd|M{Wg{txO MmDSV2FPT0WU
TE-12 cell NVvURXl7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWTVfmpNUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ{NUig{txO NEi0ZZVUSU6JRWK=
TE-5 cell M4XRZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlW1TY5pcWKrdHnvckBw\iCqdX3hckBVTS13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFY2PCEQvF2= NHi3enlUSU6JRWK=
TE-6 cell NUKwclRoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmjkTY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVA2PyEQvF2= MorQV2FPT0WU
TE-8 cell M1fBOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fjUmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNFM4OyEQvF2= M{no[HNCVkeHUh?=
TE-9 cell NEL0[GFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYG5dJBoUW6qaXLpeIlwdiCxZjDoeY1idiCWRT25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTJyMTFOwG0> NVnHNopXW0GQR1XS
TK10 cell M2rlN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV7Fb3ptUW6qaXLpeIlwdiCxZjDoeY1idiCWS{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yPjV{MjFOwG0> NGj1SIpUSU6JRWK=
DSH1 cell Mo\2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2i4e2lvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN NFXFVY5USU6JRWK=
ECC12 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4fkU2lvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6OjNzIN88US=> NG\DNm9USU6JRWK=
EKVX cell M3LZdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXLJcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= MmTPV2FPT0WU
HCC2218 cell M{XaV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnXTTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> MYPTRW5ITVJ?
LB2241-RCC cell NXrXcVFKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlTJTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zNUSwN{DPxE1? NGDmfVdUSU6JRWK=
LB996-RCC cell NHXnXJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1\WWmlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ7OU[tVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|NkKyPEDPxE1? M3jUfXNCVkeHUh?=
LC-1F cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTJOoxKUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO MmLxV2FPT0WU
LS-513 cell MlrJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{PnOWlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41ODB2MTFOwG0> NV;MO5pCW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk; 

PubMed: 25238247     


Dose response of lapatinib and PD168393 on phosphorylation of ErbB2, AKT and ERK in Calu3 and SkBr3 cells in response to EGF treatment. p-ErbB2: phosphorylated ErbB2; t-ErbB2: total-ErbB2; p-AKT: phosphorylated AKT; t-AKT: total AKT; p-ERK: phosphorylated ERK; t-ERK: total ERK.

pEGFR / EGFR / p-mTOR / 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. All values are presented as the mean ± standard error (S.E.) (**p < 0.01).

25238247 28938602
Growth inhibition assay
Cell viability ; 

PubMed: 24947784     


Huh7 (A), HepG2 (B), or HA22T (C) HCC cells were left untreated or treated with 0.1% DMSO (vehicle, D) or with DMSO containing various concentrations of lapatinib (1.25, 2.5, 5, or 10 μM) for 3 days. Relative amounts of viable cells were detected by MTS assay. O.D. values from DMSO-treated control cells were designated 100%.

24947784
In vivo Oral administration of Lapatinib Ditosylate (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. [1]

Protocol

Kinase Assay:[1]
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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]
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  • Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2
  • 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]
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  • 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 (108.05 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+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 925.46
Formula

C29H26ClFN4O4S.2C7H8O3S

CAS No. 388082-77-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × 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:

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

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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

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?

  • Answer:

    S1028 Lapatinib Ditosylate can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID