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 54 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 NEO1NJRRem:uaX\ldoF1cW:wIHHzd4F6 M{\NNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= NWT3U4JbOTZ2OEO3O|I>
BT474 cell line MmK5VJJwdGmoZYLheIlwdiCjc4PhfS=> MnPoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN M{\leVE3PDh|N{ey
HN5 cell NF31WZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2nNWWlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? NHjPeIEyPjd5N{SxNC=>
BT474 cell NHPxXXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1uyR2lvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP NFLqPHIyPjd5N{SxNC=>
N87 cell NWrZb4NiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGPsWHRKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? MX2xOlc4PzRzMB?=
HFF cell NGWx[IxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;wcWlvcGmkaYTpc44hd2ZiSF\GJINmdGxiZ4Lve5RpNCCLQ{WwQVkvQSEQvF2= NVXsNW5wOTZ5N{e0NVA>
SKBR3 cells MUDDfZRwfG:6aXPpeJkh[XO|YYm= MkD6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAyPyEQvF2= NH;IUJIyQTB{OESyOS=>
A431 cells M3\oW2N6fG:2b4jpZ4l1gSCjc4PhfS=> MlHrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVA1KM7:TR?= MnLRNVk5QDh5NkG=
SKBR3 cells NX7TTlhDS3m2b4TvfIlkcXS7IHHzd4F6 NWW4ToRqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB{OTFOwG0> NHLaemkyQTh6OEe2NS=>
HepG2 cells M4rWNHBzd2yrZnXyZZRqd25iYYPzZZk> NFu4dWlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjJ5IN88US=> NFjh[FUzODF2M{e3PC=>
Hep3B2 cells MnLJVJJwdGmoZYLheIlwdiCjc4PhfS=> NWLH[WVESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SjJiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNEmg{txO MV6yNFE1Ozd5OB?=
SKHEP1 cells MmfmVJJwdGmoZYLheIlwdiCjc4PhfS=> MkHCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVUvOyEQvF2= NWHQeWtiOjBzNEO3O|g>
MCF7 cells NYnYR3B7WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVjleHZrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjZizszN NFWw[oczODF2M{e3PC=>
MDA-MB-231 cells Mn7PVJJwdGmoZYLheIlwdiCjc4PhfS=> M3O2TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkBpenNiYomgRXRRKGOxboTlcpQh[XO|YYmsJGlEPTB;NT60JO69VQ>? NEn1cWwzODF2M{e3PC=>
SK-BR-3 cells M1PYXnBzd2yrZnXyZZRqd25iYYPzZZk> MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvODRizszN MnmxNlAyPDN5N{i=
A431 cells MXHGeY5kfGmxbjDhd5NigQ>? NX\YdYxiUW6qaXLpeIlwdiCxZjDFS2ZTKGmwdILhZ4VtdHWuYYKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFG0N|Eh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wOVIh|ryP MX[yNFM1PjZ3NR?=
N87 cells NEXxU3pHfW6ldHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKEW{YlKyJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE56NzDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjFizszN MXuyNFM1PjZ3NR?=
MIAPaCa cells M2LETmZ2dmO2aX;uJIF{e2G7 M1TtXmlvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjR|MzFOwG0> Mn\UNlA5OTd3MkO=
MIAPaCa cells MlLUSpVv[3Srb36gZZN{[Xl? M2T4S2lvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zNDFOwG0> M4P6SlIxQDF5NUKz
CAL27 cells Moi0R5l1d3SxeHnjbZR6KGG|c3H5 NFL6ZlhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB5IN88UU4> NWXzXINbOjFyOEC2Nlk>
SKOV3 cells NILpPFVEgXSxdH;4bYNqfHliYYPzZZk> NVnURpJHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNib4\ldoV5eHKnc4PpcochUEWUMjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByMzFOwG0v NID0d3YzOTB6ME[yPS=>
CAL27 cells MlrrSpVv[3Srb36gZZN{[Xl? MVixOkBp MUnJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? MljqNlExQDB4Mkm=
SK-BR-3 cells MoXBVJJwdGmoZYLheIlwdiCjc4PhfS=> NVu3UWpGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGemKEMjDveoVz\XiycnXzd4lv\yCqdX3hckBUUy2EUj2zJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA{OiEQvF2= M4nFNFIyPTdyOESz
BXF T24 cells NIfXPFVEgXSxdH;4bYNqfHliYYPzZZk> NIrsWlc1KGSjeYO= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCXGYhXDJ2IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME25MlY2KM7:TR?= MY[yNlE3QTZyMR?=
CXF 269L cells NYfzOlBUS3m2b4TvfIlkcXS7IHHzd4F6 Ml;EOEBl[Xm| MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDXGYhOjZ7TDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4{PiEQvF2= NFi3VWszOjF4OU[wNS=>
DIFI cells NIrnSWpEgXSxdH;4bYNqfHliYYPzZZk> Moi1OEBl[Xm| MojBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSGlHUSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MD6yN|Uh|ryP NWXsZ5B4OjJzNkm2NFE>
HT-29 cells NICwVo1EgXSxdH;4bYNqfHliYYPzZZk> M3nLW|Qh\GG7cx?= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND62NkDPxE1? NYDQ[JB6OjJzNkm2NFE>
RKO cells M4G4eGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGrN[VI1KGSjeYO= MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDST28h[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwM{Wg{txO MojSNlIyPjl4MEG=
GXF251L cells NY\sTlJbS3m2b4TvfIlkcXS7IHHzd4F6 NWfuRpJiPCCmYYnz M4SyU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN MYCyNlE3QTZyMR?=
LIXF 575L cells NEjxdFFEgXSxdH;4bYNqfHliYYPzZZk> MnzPOEBl[Xm| MmrQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUGlZTiB3N{XMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF04NjF6IN88US=> NWTtVHFxOjJzNkm2NFE>
LXFA 289L cells MlLaR5l1d3SxeHnjbZR6KGG|c3H5 NFq4fpM1KGSjeYO= NHW0SZJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEK4PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwN{mg{txO NYTleYhkOjJzNkm2NFE>
LXFA 526L MknZR5l1d3SxeHnjbZR6KGG|c3H5 MV:0JIRigXN? MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZCKDV{NlygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVQvOjFizszN NFnOd2szOjF4OU[wNS=>
LXFA 629L cells MkXBR5l1d3SxeHnjbZR6KGG|c3H5 MlfqOEBl[Xm| NUPwRpVMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC2NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1{Lki3JO69VQ>? NU\FcpY2OjJzNkm2NFE>
LXFL 1121L cells M1zxTWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXnwcHlGPCCmYYnz M4XJZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkxiMUGyNWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwN{Og{txO MkL4NlIyPjl4MEG=
LXFL 529L cells MXfDfZRwfG:6aXPpeJkh[XO|YYm= M4n0UFQh\GG7cx?= NXzvNHNGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDC1NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkWxJO69VQ>? MVyyNlE3QTZyMR?=
MCF7 cells M4DrbWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWnPO|V1PCCmYYnz NFv5O2ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20Mlg{KM7:TR?= MXyyNlE3QTZyMR?=
MDA231 cells MlrIR5l1d3SxeHnjbZR6KGG|c3H5 M3LVNFQh\GG7cx?= M1;tNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTJ|MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9O{44KM7:TR?= NUDYSZdwOjJzNkm2NFE>
OVXF 899L NGLyN3dEgXSxdH;4bYNqfHliYYPzZZk> MlqyOEBl[Xm| NEX4VmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXliIIEi5PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTNwM{Wg{txO Mlm3NlIyPjl4MEG=
PAXF 546L cells M3jjOmN6fG:2b4jpZ4l1gSCjc4PhfS=> NI\BXXk1KGSjeYO= MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQRXhHKDV2NlygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVYvOTJizszN M3nXbFIzOTZ7NkCx
PANC1 cells NXGzTYtvS3m2b4TvfIlkcXS7IHHzd4F6 NVXZV5VwPCCmYYnz NX6wc3U2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEGQQ{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVgvOTJizszN Mmj3NlIyPjl4MEG=
22Rv1 cell M{fXPWN6fG:2b4jpZ4l1gSCjc4PhfS=> NYP6WI97PCCmYYnz NX\Xb2dXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOjKUdkGgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVYvODZizszN MYOyNlE3QTZyMR?=
DU145 cells MV3DfZRwfG:6aXPpeJkh[XO|YYm= NGHmcGg1KGSjeYO= MoX2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUKuPVkh|ryP NU\FcnBKOjJzNkm2NFE>
LNCAP cells MXrDfZRwfG:6aXPpeJkh[XO|YYm= MoTIOEBl[Xm| NXS2N2NES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN NEXme5QzOjF4OU[wNS=>
PC3M cells NHrXOINEgXSxdH;4bYNqfHliYYPzZZk> M2fZRVQh\GG7cx?= NWjOeJVpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|TTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE42PSEQvF2= M3jFclIzOTZ7NkCx
NIH/3T3 cells NUGzT3NvWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1zt[|czKGh? MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12LkOg{txO M2KyeFIzPTl3MUe3
NCI-H1648 cell M4L3Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\1T|d1UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCyOVQ1KM7:TR?= M4rmOHNCVkeHUh?=
NMC-G1 cell NH2yXYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX3nXJhiUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV2NUCxJO69VQ>? MV3TRW5ITVJ?
NTERA-S-cl-D1 cell M1;tNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofRTY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6yOlU3OSEQvF2= MoTCV2FPT0WU
OCUB-M cell MmmzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\GTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA2PzRizszN MX;TRW5ITVJ?
OS-RC-2 cell NWD2Z2hWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnO1TY5pcWKrdHnvckBw\iCqdX3hckBQWy2UQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46QTF7OTFOwG0> NVLVXWtXW0GQR1XS
OVCAR-4 cell NVHwZ5V5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TFZWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO MWTTRW5ITVJ?
RL95-2 cell M4LT[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\hTY5pcWKrdHnvckBw\iCqdX3hckBTVDl3LUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2PjdizszN MX;TRW5ITVJ?
SW954 cell M37QNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= MVfTRW5ITVJ?
SW962 cell NIXURnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIOwcXZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> M4XCcnNCVkeHUh?=
TE-1 cell NYnnVWdJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{L4eWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNFIyPTlizszN NXH2[W9IW0GQR1XS
A253 cell NX3ZOGt3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnGbXZKdmirYnn0bY9vKG:oIHj1cYFvKEF{NUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA1QDNizszN NFzzO5lUSU6JRWK=
A388 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP NVK3NlNbW0GQR1XS
BB30-HNC cell M2fyemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXnLfVNCUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP M2mzbXNCVkeHUh?=
TE-12 cell M2jPN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63NlI2QCEQvF2= M2PaUnNCVkeHUh?=
TE-5 cell NFj0PXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVrBSJlEUW6qaXLpeIlwdiCxZjDoeY1idiCWRT21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDZ3NDFOwG0> MVPTRW5ITVJ?
TE-6 cell M1XEWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHyUnBPUW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QTB3NzFOwG0> M3H0eHNCVkeHUh?=
TE-8 cell NWLHdVFWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3W0fWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNFM4OyEQvF2= NIfSZpNUSU6JRWK=
TE-9 cell M1TpbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H0b2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVUzODFizszN NUfTSXgyW0GQR1XS
TK10 cell NHzEZY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;qUWlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN NHvweWlUSU6JRWK=
DSH1 cell Mn;VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2LwZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN NUjDSI1GW0GQR1XS
ECC12 cell NY[weHJZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGVESzF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVI{OSEQvF2= MlH4V2FPT0WU
EKVX cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= NF;mWHhUSU6JRWK=
HCC2218 cell MlHYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\RU2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkKxPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV|Mk[g{txO NWrKbnpNW0GQR1XS
LB2241-RCC cell NUD4c2JsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HudWlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMUW0NFMh|ryP NIjvd5NUSU6JRWK=
LB996-RCC cell NWL2W4NTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYmwOlE5UW6qaXLpeIlwdiCxZjDoeY1idiCOQkm5Ok1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkO2NlI5KM7:TR?= M1jUeHNCVkeHUh?=
LC-1F cell M{LRb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnUb|JUUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO MmT3V2FPT0WU
LS-513 cell MkfYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnnTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQxODRzIN88US=> NIrjOnFUSU6JRWK=

... Click to View More Cell Line Experimental Data

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]
+ 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
  • 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 (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

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

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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).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
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
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 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 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