Lapatinib (GW-572016) Ditosylate

For research use only.

Catalog No.S1028

74 publications

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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Selleck's Lapatinib (GW-572016) Ditosylate has been cited by 74 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 Mn\VVJJwdGmoZYLheIlwdiCjc4PhfS=> M{DJfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= MojjNVY1QDN5N{K=
BT474 cell line M2m1XnBzd2yrZnXyZZRqd25iYYPzZZk> MlfKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NUXXVW5WOTZ2OEO3O|I>
HN5 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M37kR2lvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? MoHaNVY4Pzd2MUC=
BT474 cell NUXpVJV7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2DrfmlvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP MWmxOlc4PzRzMB?=
N87 cell NYD6V2htT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjNWmJKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? MnzUNVY4Pzd2MUC=
HFF cell NX\OSoNLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M13FcWlvcGmkaYTpc44hd2ZiSF\GJINmdGxiZ4Lve5RpNCCLQ{WwQVkvQSEQvF2= NFTtfmIyPjd5N{SxNC=>
SKBR3 cells NGXKV2VEgXSxdH;4bYNqfHliYYPzZZk> M2Pk[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOTdizszN M4rISVE6ODJ6NEK1
A431 cells MlzXR5l1d3SxeHnjbZR6KGG|c3H5 MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6xNFQh|ryP M{\hV|E6QDh6N{[x
SKBR3 cells Mnf1R5l1d3SxeHnjbZR6KGG|c3H5 NYPnepNIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB{OTFOwG0> NGLpbFkyQTh6OEe2NS=>
HepG2 cells NV7XTYxGWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH7NbIpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjJ5IN88US=> NWjX[HpxOjBzNEO3O|g>
Hep3B2 cells NV;pXnF{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NH;IW|BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52OTFOwG0> MViyNFE1Ozd5OB?=
SKHEP1 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MlnURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVUvOyEQvF2= MlW1NlAyPDN5N{i=
MCF7 cells M3nrOXBzd2yrZnXyZZRqd25iYYPzZZk> NHrxVVBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvPiEQvF2= NFfaRZMzODF2M{e3PC=>
MDA-MB-231 cells NES3NWFRem:uaX\ldoF1cW:wIHHzd4F6 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNDFOwG0> MXmyNFE1Ozd5OB?=
SK-BR-3 cells M1\VeXBzd2yrZnXyZZRqd25iYYPzZZk> M4jsbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utRnIuOyClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:OC5yNDFOwG0> NVH5bnRxOjBzNEO3O|g>
A431 cells M3XXS2Z2dmO2aX;uJIF{e2G7 NXf0NJMzUW6qaXLpeIlwdiCxZjDFS2ZTKGmwdILhZ4VtdHWuYYKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFG0N|Eh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wOVIh|ryP NE[wSY4zODN2Nk[1OS=>
N87 cells NXvWOIk6TnWwY4Tpc44h[XO|YYm= MlfFTY5pcWKrdHnvckBw\iCHcnLCNkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCQOEegZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zIN88US=> MV[yNFM1PjZ3NR?=
MIAPaCa cells MVXGeY5kfGmxbjDhd5NigQ>? NXG5PGNiUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOUUGSYVPhJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwNEOzJO69VQ>? NHfFeVQzODhzN{WyNy=>
MIAPaCa cells MYPGeY5kfGmxbjDhd5NigQ>? MkfFTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> M4eyTVIxQDF5NUKz
CAL27 cells NWHZTlFwS3m2b4TvfIlkcXS7IHHzd4F6 NVe3ZpFSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByNzFOwG0v NVTH[YRtOjFyOEC2Nlk>
SKOV3 cells NH;mUm9EgXSxdH;4bYNqfHliYYPzZZk> NF7OOYtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJTVJ{IHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB|IN88UU4> NXTGb2FPOjFyOEC2Nlk>
CAL27 cells NFPpZW5HfW6ldHnvckBie3OjeR?= MoPINVYhcA>? MnntTY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4SsJGlEPTB;MD6wN|Ih|ryP NV3iSFdUOjFyOEC2Nlk>
SK-BR-3 cells Mn\QVJJwdGmoZYLheIlwdiCjc4PhfS=> M{KzfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSZJjSjJib4\ldoV5eHKnc4PpcochcHWvYX6gV2suSlJvMzDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wN|Ih|ryP NW[5c3pzOjF3N{C4OFM>
BXF T24 cells NI\4cXdEgXSxdH;4bYNqfHliYYPzZZk> M2XhNlQh\GG7cx?= M4nYOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJZTiCWMkSgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPjVizszN NWfRbFZIOjJzNkm2NFE>
CXF 269L cells NF3ZbZlEgXSxdH;4bYNqfHliYYPzZZk> NUTFVI5DPCCmYYnz NF\ISlREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEYEZiMk[5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:QC5|NjFOwG0> NELUTnUzOjF4OU[wNS=>
DIFI cells Mke5R5l1d3SxeHnjbZR6KGG|c3H5 NYLTZ2F6PCCmYYnz M2XEb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= M1vuXVIzOTZ7NkCx
HT-29 cells M4TTeWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3;MXFQh\GG7cx?= MnvWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOlIh|ryP NXrydVFmOjJzNkm2NFE>
RKO cells MnjjR5l1d3SxeHnjbZR6KGG|c3H5 M13GO|Qh\GG7cx?= NF:4c2xEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUWuN|Uh|ryP NETsV3AzOjF4OU[wNS=>
GXF251L cells NYnEZWlSS3m2b4TvfIlkcXS7IHHzd4F6 MU[0JIRigXN? NHHz[YhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIYEZ{NUHMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0yNjR6IN88US=> NEnGcpUzOjF4OU[wNS=>
LIXF 575L cells MYXDfZRwfG:6aXPpeJkh[XO|YYm= NVe0PYpSPCCmYYnz M2LlOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxKYEZiNUe1UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py5zODFOwG0> MUiyNlE3QTZyMR?=
LXFA 289L cells NVHmdI1bS3m2b4TvfIlkcXS7IHHzd4F6 NIfMcVU1KGSjeYO= MnTOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHSSB{OEnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF02Njd7IN88US=> MmDzNlIyPjl4MEG=
LXFA 526L MkjIR5l1d3SxeHnjbZR6KGG|c3H5 NG\wNlM1KGSjeYO= NFzmVJREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEWyOmwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTRwMkGg{txO NF:yVoozOjF4OU[wNS=>
LXFA 629L cells NIrkbndEgXSxdH;4bYNqfHliYYPzZZk> NETnVXY1KGSjeYO= NXTEbVZ7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC2NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1{Lki3JO69VQ>? NF3pNHMzOjF4OU[wNS=>
LXFL 1121L cells MXTDfZRwfG:6aXPpeJkh[XO|YYm= NVrwPFFtPCCmYYnz M2q5fmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkxiMUGyNWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwN{Og{txO M{PpNlIzOTZ7NkCx
LXFL 529L cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= MU[0JIRigXN? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZNKDV{OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPTFizszN M4\HZ|IzOTZ7NkCx
MCF7 cells M4HnV2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWCyS4ZQPCCmYYnz MkLVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND64N{DPxE1? NWLHOFVJOjJzNkm2NFE>
MDA231 cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= M3joVFQh\GG7cx?= NEK1cYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF{M{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvPyEQvF2= NUfyWZBoOjJzNkm2NFE>
OVXF 899L M1PuW2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmrJOEBl[Xm| MoLXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZZTiB6OUnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjN3IN88US=> MkG5NlIyPjl4MEG=
PAXF 546L cells NVfRcYVyS3m2b4TvfIlkcXS7IHHzd4F6 Mo[5OEBl[Xm| NX2xVZEyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEG[RjC1OFZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD14LkGyJO69VQ>? MnzBNlIyPjl4MEG=
PANC1 cells NYi3Z4U1S3m2b4TvfIlkcXS7IHHzd4F6 NY\GOHFDPCCmYYnz M2WwNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME24MlEzKM7:TR?= MWqyNlE3QTZyMR?=
22Rv1 cell M1HSN2N6fG:2b4jpZ4l1gSCjc4PhfS=> NVH5eW44PCCmYYnz M4fSU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFIzWnZzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME22MlA3KM7:TR?= MVWyNlE3QTZyMR?=
DU145 cells NVvmVXNXS3m2b4TvfIlkcXS7IHHzd4F6 MUe0JIRigXN? MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Mj65PUDPxE1? NEDCfmozOjF4OU[wNS=>
LNCAP cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= M1LXcVQh\GG7cx?= Mli0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUOuOlgh|ryP MkniNlIyPjl4MEG=
PC3M cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= NWDBXm5RPCCmYYnz MnzlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{VSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND61OUDPxE1? NG\wd|YzOjF4OU[wNS=>
NIH/3T3 cells NHi3TZJRem:uaX\ldoF1cW:wIHHzd4F6 MkizO|IhcA>? M4ntU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuN{DPxE1? M1zSXlIzPTl3MUe3
NCI-H1648 cell M1XySmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\5TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB{NUS0JO69VQ>? MmDyV2FPT0WU
NMC-G1 cell NF\NdIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVQ2ODFizszN NE\SeGtUSU6JRWK=
NTERA-S-cl-D1 cell NH\UbWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXG2[ZNtUW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPjV4MTFOwG0> NXe3NoRVW0GQR1XS
OCUB-M cell NHPTUHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUT6SI9XUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB3N{Sg{txO NELCXIJUSU6JRWK=
OS-RC-2 cell NVju[5NMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4H0cGlvcGmkaYTpc44hd2ZiaIXtZY4hV1NvUlOtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTlzOUmg{txO NUe4OJhiW0GQR1XS
OVCAR-4 cell NU\Pb5ZRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXuVoZJUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk01KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS5zMU[3OUDPxE1? Mn\jV2FPT0WU
RL95-2 cell NHixSXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEexTmhKdmirYnn0bY9vKG:oIHj1cYFvKFKOOUWtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTV4NzFOwG0> MV;TRW5ITVJ?
SW954 cell M1LJSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYCyO2E3UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl{NEWg{txO NE[xcZhUSU6JRWK=
SW962 cell NEX4O|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NES0fI5KdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> M37CfHNCVkeHUh?=
TE-1 cell MmTOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\Ud3pKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlAzOTV7IN88US=> MmTjV2FPT0WU
A253 cell MnrKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;ZTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= MlzpV2FPT0WU
A388 cell M4LGeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvPdZRKdmirYnn0bY9vKG:oIHj1cYFvKEF|OEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA1QDNizszN NYrQPFBpW0GQR1XS
BB30-HNC cell NIrsTYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TjSmlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl5M{O1JO69VQ>? MYDTRW5ITVJ?
TE-12 cell NF7LWW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnfZTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|IzPThizszN MXzTRW5ITVJ?
TE-5 cell M3HzdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= NF3GZ5hUSU6JRWK=
TE-6 cell NV;CZ2JWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XNOmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFkxPTdizszN NHjFe5dUSU6JRWK=
TE-8 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NILSdHVKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{PzNizszN M4\M[HNCVkeHUh?=
TE-9 cell NWG2VnpkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml3DTY5pcWKrdHnvckBw\iCqdX3hckBVTS17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OVIxOSEQvF2= MUTTRW5ITVJ?
TK10 cell MkixS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2OVIzKM7:TR?= NXGye41yW0GQR1XS
DSH1 cell NVLjeIVVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYD2emd6UW6qaXLpeIlwdiCxZjDoeY1idiCGU1ixJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTN7NjFOwG0> NIGwTFVUSU6JRWK=
ECC12 cell M4ixZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3BOJpKdmirYnn0bY9vKG:oIHj1cYFvKEWFQ{GyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTJ|MTFOwG0> MnLtV2FPT0WU
EKVX cell NEjRVINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFvBbIRKdmirYnn0bY9vKG:oIHj1cYFvKEWNVmigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDd2IN88US=> MnLDV2FPT0WU
HCC2218 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEOweJpKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{KyNVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB3M{K2JO69VQ>? NG\IcGNUSU6JRWK=
LB2241-RCC cell NHX4UHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGjw[5VKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkK0NU1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkG1OFA{KM7:TR?= NID4WZpUSU6JRWK=
LB996-RCC cell M{i0O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUS4Xpo5UW6qaXLpeIlwdiCxZjDoeY1idiCOQkm5Ok1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkO2NlI5KM7:TR?= M4DGT3NCVkeHUh?=
LC-1F cell M4XNVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHhTY5pcWKrdHnvckBw\iCqdX3hckBNSy1zRjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|gzPDRizszN MkHxV2FPT0WU
LS-513 cell M{TTbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHSxT5BKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDByNEGg{txO NEX2XnlUSU6JRWK=

... 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
  • 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
Smiles CC1=CC=C(C=C1)[S](O)(=O)=O.CC2=CC=C(C=C2)[S](O)(=O)=O.C[S](=O)(=O)CCNCC3=CC=C(O3)C4=CC=C5N=CN=C(NC6=CC=C(OCC7=CC=CC(=C7)F)C(=C6)Cl)C5=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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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 (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:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment 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 Completed 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.

  • * 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