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 62 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 MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NHG0dIpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NYP5SoZ[OTZ2OEO3O|I>
BT474 cell line MYDQdo9tcW[ncnH0bY9vKGG|c3H5 MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= NInofpAyPjR6M{e3Ni=>
HN5 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljUTY5pcWKrdHnvckBw\iCKTkWgZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKg{txO NVvwVVBqOTZ5N{e0NVA>
BT474 cell NWe3NFlVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17DNGlvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP MXWxOlc4PzRzMB?=
N87 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIjqO3ZKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? MVKxOlc4PzRzMB?=
HFF cell Mnn6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LHOWlvcGmkaYTpc44hd2ZiSF\GJINmdGxiZ4Lve5RpNCCLQ{WwQVkvQSEQvF2= MY[xOlc4PzRzMB?=
SKBR3 cells M4\abWN6fG:2b4jpZ4l1gSCjc4PhfS=> NH3ofnlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF5IN88US=> M1nS[|E6ODJ6NEK1
A431 cells NVjKZWtMS3m2b4TvfIlkcXS7IHHzd4F6 MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6xNFQh|ryP NFnTOWkyQTh6OEe2NS=>
SKBR3 cells NH\TWoNEgXSxdH;4bYNqfHliYYPzZZk> M3HJb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOjlizszN MYOxPVg5QDd4MR?=
HepG2 cells NF2w[mdRem:uaX\ldoF1cW:wIHHzd4F6 NIDGdZRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjJ5IN88US=> NEfUZ|gzODF2M{e3PC=>
Hep3B2 cells NVXC[Id4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGX5PXRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52OTFOwG0> MXyyNFE1Ozd5OB?=
SKHEP1 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MlrjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVUvOyEQvF2= NIXQc2ozODF2M{e3PC=>
MCF7 cells Mo\jVJJwdGmoZYLheIlwdiCjc4PhfS=> NGnqcHNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvPiEQvF2= NFO3VHUzODF2M{e3PC=>
MDA-MB-231 cells NGj2b5lRem:uaX\ldoF1cW:wIHHzd4F6 NIrFXY1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPUWuOEDPxE1? NHG0S5czODF2M{e3PC=>
SK-BR-3 cells NEX3U21Rem:uaX\ldoF1cW:wIHHzd4F6 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvODRizszN MVGyNFE1Ozd5OB?=
A431 cells MV;GeY5kfGmxbjDhd5NigQ>? M4izRmlvcGmkaYTpc44hd2ZiRVfGVkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDNEOxJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMEWyJO69VQ>? MljPNlA{PDZ4NUW=
N87 cells NXe3VZZKTnWwY4Tpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKEW{YlKyJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE56NzDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjFizszN MYGyNFM1PjZ3NR?=
MIAPaCa cells MWPGeY5kfGmxbjDhd5NigQ>? NHPGS3RKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO M3HqeVIxQDF5NUKz
MIAPaCa cells Mn;tSpVv[3Srb36gZZN{[Xl? M33YVGlvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zNDFOwG0> NWL4endYOjB6MUe1NlM>
CAL27 cells M1f4PGN6fG:2b4jpZ4l1gSCjc4PhfS=> MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDRWwzPyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFS2ZTKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA4KM7:TT6= NFTwOFQzOTB6ME[yPS=>
SKOV3 cells MkfNR5l1d3SxeHnjbZR6KGG|c3H5 M{nTTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGhGWjJiYomgdoV{[Xq3cnnuJIR6\SC{ZXT1Z5Rqd25iYYPzZZktKEmFNUC9NE4xODNizszNMi=> MWeyNVA5ODZ{OR?=
CAL27 cells NU\VbGZJTnWwY4Tpc44h[XO|YYm= NVfRfZJWOTZiaB?= MVHJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? NXv3XnV2OjFyOEC2Nlk>
SK-BR-3 cells NGrNTopRem:uaX\ldoF1cW:wIHHzd4F6 NUHNN2FNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGemKEMjDveoVz\XiycnXzd4lv\yCqdX3hckBUUy2EUj2zJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA{OiEQvF2= NFX5bG0zOTV5MEi0Ny=>
BXF T24 cells MnezR5l1d3SxeHnjbZR6KGG|c3H5 M2G1SVQh\GG7cx?= M33YfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJZTiCWMkSgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPjVizszN MViyNlE3QTZyMR?=
CXF 269L cells NIn0W|JEgXSxdH;4bYNqfHliYYPzZZk> MXm0JIRigXN? M1HyVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNZTiB{NknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF05NjN4IN88US=> NGnZbY0zOjF4OU[wNS=>
DIFI cells NXjuW3JHS3m2b4TvfIlkcXS7IHHzd4F6 NXvWZXlYPCCmYYnz M1TEZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= M4LuVVIzOTZ7NkCx
HT-29 cells Mmn6R5l1d3SxeHnjbZR6KGG|c3H5 MW[0JIRigXN? MnXGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOlIh|ryP NFzWNJEzOjF4OU[wNS=>
RKO cells NWHzbYxiS3m2b4TvfIlkcXS7IHHzd4F6 M1;zbVQh\GG7cx?= NGq5[HREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUWuN|Uh|ryP M1vSfVIzOTZ7NkCx
GXF251L cells NFPvb3REgXSxdH;4bYNqfHliYYPzZZk> M3\wWFQh\GG7cx?= NWPsd2h[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT1iIMkWxUEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OS52ODFOwG0> MmjuNlIyPjl4MEG=
LIXF 575L cells NILWVYtEgXSxdH;4bYNqfHliYYPzZZk> NUHwRllCPCCmYYnz M3fjRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxKYEZiNUe1UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py5zODFOwG0> NWXhU|dDOjJzNkm2NFE>
LXFA 289L cells NHHVdopEgXSxdH;4bYNqfHliYYPzZZk> MmHxOEBl[Xm| MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZCKDJ6OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVUvPzlizszN MVeyNlE3QTZyMR?=
LXFA 526L MXHDfZRwfG:6aXPpeJkh[XO|YYm= NUn3N2kzPCCmYYnz NVLWSFZyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC1NlZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkKxJO69VQ>? NYnZZ2RwOjJzNkm2NFE>
LXFA 629L cells M1vpeGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFH2[lk1KGSjeYO= M2TlNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiNkK5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Oi56NzFOwG0> NEniXXYzOjF4OU[wNS=>
LXFL 1121L cells NX\aW4FES3m2b4TvfIlkcXS7IHHzd4F6 M{K0U|Qh\GG7cx?= MorGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHVCBzMUKxUEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py55MzFOwG0> NHPPPIIzOjF4OU[wNS=>
LXFL 529L cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NW\IUIRRPCCmYYnz MkPaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHVCB3MknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjVzIN88US=> M4HRUVIzOTZ7NkCx
MCF7 cells M4PiS2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGPVVVk1KGSjeYO= NFvy[IJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20Mlg{KM7:TR?= M1jvNFIzOTZ7NkCx
MDA231 cells M2TUW2N6fG:2b4jpZ4l1gSCjc4PhfS=> Mnm0OEBl[Xm| M2m4WWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTJ|MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9O{44KM7:TR?= M3;5WVIzOTZ7NkCx
OVXF 899L NIK2WVhEgXSxdH;4bYNqfHliYYPzZZk> M2n2ZlQh\GG7cx?= Ml6zR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZZTiB6OUnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjN3IN88US=> MVuyNlE3QTZyMR?=
PAXF 546L cells M13Rb2N6fG:2b4jpZ4l1gSCjc4PhfS=> MkPoOEBl[Xm| M4XUR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCYEZiNUS2UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi5zMjFOwG0> NVLFXGRWOjJzNkm2NFE>
PANC1 cells Ml7vR5l1d3SxeHnjbZR6KGG|c3H5 M4PvPFQh\GG7cx?= MnjVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFPSzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUiuNVIh|ryP MVeyNlE3QTZyMR?=
22Rv1 cell NYnBeHV2S3m2b4TvfIlkcXS7IHHzd4F6 NWrmc2ZrPCCmYYnz MmPTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNlJTfjFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPU[uNFYh|ryP MonjNlIyPjl4MEG=
DU145 cells M3nO[GN6fG:2b4jpZ4l1gSCjc4PhfS=> NUS5O2tCPCCmYYnz MmDnR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUKuPVkh|ryP MUmyNlE3QTZyMR?=
LNCAP cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= NXXrU5VbPCCmYYnz NGTZdlNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9N{43QCEQvF2= NF2yfY0zOjF4OU[wNS=>
PC3M cells NV;5ZZZYS3m2b4TvfIlkcXS7IHHzd4F6 M1e1[lQh\GG7cx?= M3fwWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEO01iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOVUh|ryP MkLhNlIyPjl4MEG=
NIH/3T3 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 Mn:1O|IhcA>? MnLzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;ND6zJO69VQ>? MYGyNlU6PTF5Nx?=
NCI-H1648 cell M4ewOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEPSWpNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEK1OFQh|ryP NV\KTGRpW0GQR1XS
NMC-G1 cell NWTWO3BDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{HDWWlvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42PDVyMTFOwG0> NVjaVY05W0GQR1XS
NTERA-S-cl-D1 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnzNTY5pcWKrdHnvckBw\iCqdX3hckBPXEWUQT3TMYNtNURzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6yOlU3OSEQvF2= MYLTRW5ITVJ?
OCUB-M cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NI\VblFKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV5NDFOwG0> M2DTd3NCVkeHUh?=
OS-RC-2 cell NYLJRnJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVjJcohq[mm2aX;uJI9nKGi3bXHuJG9UNVKFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk6OTl7IN88US=> NX3KRoN2W0GQR1XS
OVCAR-4 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13LdWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO NFPrXIFUSU6JRWK=
RL95-2 cell MnjlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHnlbYdKdmirYnn0bY9vKG:oIHj1cYFvKFKOOUWtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTV4NzFOwG0> NFS1e21USU6JRWK=
SW954 cell M2XVPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1[1ZmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6OjR3IN88US=> MlqyV2FPT0WU
SW962 cell M4L4fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrDU3VKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> MlW1V2FPT0WU
TE-1 cell NVjUXmlLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7kbXluUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4xOjF3OTFOwG0> NVnVcZZsW0GQR1XS
A253 cell NVqz[pJoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\yTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NISwclNUSU6JRWK=
A388 cell NEXmXIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkDzTY5pcWKrdHnvckBw\iCqdX3hckBCOzh6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NXy4[3hiW0GQR1XS
BB30-HNC cell Mm\VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk[xTY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTd|M{Wg{txO NHn0VmRUSU6JRWK=
TE-12 cell Mnf2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVns[plVUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ{NUig{txO MlHoV2FPT0WU
TE-5 cell MkL1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= MnjFV2FPT0WU
TE-6 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX[5dok5UW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QTB3NzFOwG0> M36wUnNCVkeHUh?=
TE-8 cell MknMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHoTY5pcWKrdHnvckBw\iCqdX3hckBVTS16IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6wN|c{KM7:TR?= M{DieXNCVkeHUh?=
TE-9 cell MmXaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37YXmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVUzODFizszN NHfHdWxUSU6JRWK=
TK10 cell NUTLVolxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nLOmlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN MlPiV2FPT0WU
DSH1 cell M1;PbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHjZ5lKdmirYnn0bY9vKG:oIHj1cYFvKESVSEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6Ozl4IN88US=> M37YbHNCVkeHUh?=
ECC12 cell NYHabIVqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2\2R2lvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6OjNzIN88US=> NWLiOlJ{W0GQR1XS
EKVX cell MkOxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= NUTKfpFkW0GQR1XS
HCC2218 cell MnrpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{PZcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkKxPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV|Mk[g{txO NEjGe|FUSU6JRWK=
LB2241-RCC cell M3;2eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jNd2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMUW0NFMh|ryP MmHVV2FPT0WU
LB996-RCC cell M1zx[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDlTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? MlHMV2FPT0WU
LC-1F cell M{PmWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnF[mM6UW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO NHHhbW1USU6JRWK=
LS-513 cell NFPXO2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlTUTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQxODRzIN88US=> MVPTRW5ITVJ?

... 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]
+ 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

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:

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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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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