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 65 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 M2HVdnBzd2yrZnXyZZRqd25iYYPzZZk> NGrmcnpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN M{\MdFE3PDh|N{ey
BT474 cell line M1nIN3Bzd2yrZnXyZZRqd25iYYPzZZk> NUPqRpJNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsJIxqdmVuIFnDOVA:OC5yMkWg{txO M1rMXlE3PDh|N{ey
HN5 cell M2D6SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEnkSIJKdmirYnn0bY9vKG:oIFjOOUBk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6xNkDPxE1? M{i4WFE3Pzd5NEGw
BT474 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLJXlhKdmirYnn0bY9vKG:oIFLUOFc1KGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{whUUN3ME2wMlA5KM7:TR?= M2TZXlE3Pzd5NEGw
N87 cell M2XR[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUe4N4RTUW6qaXLpeIlwdiCxZjDOPFch[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP NULmV2tyOTZ5N{e0NVA>
HFF cell NFjmb2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2ns[WlvcGmkaYTpc44hd2ZiSF\GJINmdGxiZ4Lve5RpNCCLQ{WwQVkvQSEQvF2= MmXlNVY4Pzd2MUC=
SKBR3 cells M1TYZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGr3d|BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF5IN88US=> MofMNVkxOjh2MkW=
A431 cells NGDYVVhEgXSxdH;4bYNqfHliYYPzZZk> MlvsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVA1KM7:TR?= NFjxZnMyQTh6OEe2NS=>
SKBR3 cells M2XnU2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnLER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAzQSEQvF2= MYGxPVg5QDd4MR?=
HepG2 cells NH3IdXNRem:uaX\ldoF1cW:wIHHzd4F6 NV;TcI9VSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:Pi5{NzFOwG0> Mn:3NlAyPDN5N{i=
Hep3B2 cells MkL2VJJwdGmoZYLheIlwdiCjc4PhfS=> MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincEPCNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU41QSEQvF2= MYqyNFE1Ozd5OB?=
SKHEP1 cells NHvUZVJRem:uaX\ldoF1cW:wIHHzd4F6 NWTVUGhzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwMzFOwG0> M1TDdFIxOTR|N{e4
MCF7 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 NHLuV3FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvPiEQvF2= M4HBfVIxOTR|N{e4
MDA-MB-231 cells NHi2XGFRem:uaX\ldoF1cW:wIHHzd4F6 NYX1SXM6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME21MlQh|ryP NWL3NHF4OjBzNEO3O|g>
SK-BR-3 cells MnK0VJJwdGmoZYLheIlwdiCjc4PhfS=> MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvODRizszN NHLGXpczODF2M{e3PC=>
A431 cells NFS1[FlHfW6ldHnvckBie3OjeR?= M4T6OWlvcGmkaYTpc44hd2ZiRVfGVkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDNEOxJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMEWyJO69VQ>? NEL2eGQzODN2Nk[1OS=>
N87 cells MlrZSpVv[3Srb36gZZN{[Xl? M4K4UGlvcGmkaYTpc44hd2ZiRYLiRlIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTki3JINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMTFOwG0> MVOyNFM1PjZ3NR?=
MIAPaCa cells NIDVU|dHfW6ldHnvckBie3OjeR?= NXGzSVdqUW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOUUGSYVPhJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwNEOzJO69VQ>? MXOyNFgyPzV{Mx?=
MIAPaCa cells M2PGWmZ2dmO2aX;uJIF{e2G7 MonSTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> MU[yNFgyPzV{Mx?=
CAL27 cells Mn;LR5l1d3SxeHnjbZR6KGG|c3H5 NH\UNVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB5IN88UU4> MnS0NlExQDB4Mkm=
SKOV3 cells NWm3[lM4S3m2b4TvfIlkcXS7IHHzd4F6 MlzZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMhd3[ncnX4dJJme3OrbnegTGVTOiCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2wMlAxOyEQvF2u M2LW[|IyODhyNkK5
CAL27 cells NFzlO5VHfW6ldHnvckBie3OjeR?= NGC1O4QyPiCq MnriTY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4SsJGlEPTB;MD6wN|Ih|ryP MmjSNlExQDB4Mkm=
SK-BR-3 cells NEXOTGNRem:uaX\ldoF1cW:wIHHzd4F6 M{\vZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgSZJjSjJib4\ldoV5eHKnc4PpcochcHWvYX6gV2suSlJvMzDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wN|Ih|ryP MVGyNVU4ODh2Mx?=
BXF T24 cells NEPjbYlEgXSxdH;4bYNqfHliYYPzZZk> MUK0JIRigXN? NWPHTIw2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSliIIGSyOEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:QS54NTFOwG0> NWjWR5I1OjJzNkm2NFE>
CXF 269L cells NWHhbGFPS3m2b4TvfIlkcXS7IHHzd4F6 MnS2OEBl[Xm| NYDabpJTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS1iIIEK2PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRThwM{[g{txO NHq0O2QzOjF4OU[wNS=>
DIFI cells NHrZU2xEgXSxdH;4bYNqfHliYYPzZZk> M{DCXVQh\GG7cx?= NGL0Uo9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFUU[LIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlI{PSEQvF2= MoX3NlIyPjl4MEG=
HT-29 cells MkXFR5l1d3SxeHnjbZR6KGG|c3H5 M3e4dlQh\GG7cx?= NXy0UVNOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVQvPjJizszN NXHzfI5UOjJzNkm2NFE>
RKO cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= MXy0JIRigXN? NFfkUWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTU09iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUWuN|Uh|ryP MWWyNlE3QTZyMR?=
GXF251L cells NVf6Ro02S3m2b4TvfIlkcXS7IHHzd4F6 MYC0JIRigXN? Mn7pR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS3hHOjVzTDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9NU41QCEQvF2= M{DqOlIzOTZ7NkCx
LIXF 575L cells M2fEcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3HicFQh\GG7cx?= M1TqfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxKYEZiNUe1UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py5zODFOwG0> MkP0NlIyPjl4MEG=
LXFA 289L cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= NFTsNI41KGSjeYO= MojVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHSSB{OEnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF02Njd7IN88US=> NXnrNZJUOjJzNkm2NFE>
LXFA 526L MmTGR5l1d3SxeHnjbZR6KGG|c3H5 M2jnVFQh\GG7cx?= NU[zWFE2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC1NlZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkKxJO69VQ>? Ml7ZNlIyPjl4MEG=
LXFA 629L cells M1nJT2N6fG:2b4jpZ4l1gSCjc4PhfS=> MUO0JIRigXN? M3XhTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiNkK5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Oi56NzFOwG0> MUeyNlE3QTZyMR?=
LXFL 1121L cells MkXxR5l1d3SxeHnjbZR6KGG|c3H5 MYC0JIRigXN? NX;NSnZGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDCxNVIyVCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nz63N{DPxE1? MoPVNlIyPjl4MEG=
LXFL 529L cells M4CwVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NVjo[4RjPCCmYYnz NH72fHREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[OIEWyPWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTNwNUGg{txO NHfpZnczOjF4OU[wNS=>
MCF7 cells MXfDfZRwfG:6aXPpeJkh[XO|YYm= NX\5fFJxPCCmYYnz NVux[JVTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE45OyEQvF2= MoT2NlIyPjl4MEG=
MDA231 cells NUT3Xm5sS3m2b4TvfIlkcXS7IHHzd4F6 M3rTdlQh\GG7cx?= M3\uPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTJ|MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9O{44KM7:TR?= NXz2VG1JOjJzNkm2NFE>
OVXF 899L NX7sXZR7S3m2b4TvfIlkcXS7IHHzd4F6 NEHaWZY1KGSjeYO= NVjGeHVES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[[RjC4PVlNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkO1JO69VQ>? MXWyNlE3QTZyMR?=
PAXF 546L cells MnTpR5l1d3SxeHnjbZR6KGG|c3H5 NH;KbYM1KGSjeYO= MkmxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFZTiB3NE\MJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF03NjF{IN88US=> MVuyNlE3QTZyMR?=
PANC1 cells Mo\tR5l1d3SxeHnjbZR6KGG|c3H5 MVi0JIRigXN? M4rTfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME24MlEzKM7:TR?= M2DEW|IzOTZ7NkCx
22Rv1 cell MYTDfZRwfG:6aXPpeJkh[XO|YYm= M3e2PFQh\GG7cx?= NEnJSnBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAzOlK4MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok4xPiEQvF2= MWWyNlE3QTZyMR?=
DU145 cells M1nHN2N6fG:2b4jpZ4l1gSCjc4PhfS=> NW\vXXNpPCCmYYnz NYLheXY3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVIvQTlizszN MV[yNlE3QTZyMR?=
LNCAP cells NInM[2pEgXSxdH;4bYNqfHliYYPzZZk> M1\kfFQh\GG7cx?= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Mz62PEDPxE1? NYrFeGdNOjJzNkm2NFE>
PC3M cells NHLXNoVEgXSxdH;4bYNqfHliYYPzZZk> MV20JIRigXN? NYrtOo5FS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|TTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE42PSEQvF2= MlS4NlIyPjl4MEG=
NIH/3T3 cells NWHxWlNbWHKxbHnm[ZJifGmxbjDhd5NigQ>? NX3jVIRKPzJiaB?= NXnyXZp7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDOTWgwO1R|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OE4{KM7:TR?= NYXreo1pOjJ3OUWxO|c>
NCI-H1648 cell NF7HSHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLlT2ZIUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCyOVQ1KM7:TR?= NUXH[5ZzW0GQR1XS
NMC-G1 cell NYXOZ217T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoKyTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlU1PTBzIN88US=> NGTReXhUSU6JRWK=
NTERA-S-cl-D1 cell NG\mc4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEX1cJFKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlI3PTZzIN88US=> NWH5N|NnW0GQR1XS
OCUB-M cell MmfCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPTXWwzUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2XCMW0h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB3N{Sg{txO M4XNPXNCVkeHUh?=
OS-RC-2 cell MojoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLCOGViUW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57OUG5PUDPxE1? NIC0UXVUSU6JRWK=
OVCAR-4 cell NGPTS2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlEyPjd3IN88US=> MYHTRW5ITVJ?
RL95-2 cell MlzxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKGi3bXHuJHJNQTVvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVU3PyEQvF2= MkXRV2FPT0WU
SW954 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Moq4TY5pcWKrdHnvckBw\iCqdX3hckBUXzl3NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|kzPDVizszN NULYcZNzW0GQR1XS
SW962 cell NF70dnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXGeHVtUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl{NEWg{txO MnTIV2FPT0WU
TE-1 cell M1HUPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlKwTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6wNlE2QSEQvF2= MnfBV2FPT0WU
A253 cell MkHoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLz[WRYUW6qaXLpeIlwdiCxZjDoeY1idiCDMkWzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPDh|IN88US=> MnrIV2FPT0WU
A388 cell MmDKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP NX63bIoxW0GQR1XS
BB30-HNC cell M4D1eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3nZfWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl5M{O1JO69VQ>? M1r3NHNCVkeHUh?=
TE-12 cell NWT6cot3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHXNR4ZKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjJ3ODFOwG0> NH:3[GhUSU6JRWK=
TE-5 cell NHfqW5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= NI\TNpdUSU6JRWK=
TE-6 cell NGTkVGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn72TY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVA2PyEQvF2= Ml\SV2FPT0WU
TE-8 cell NFzOOHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrFfFVYUW6qaXLpeIlwdiCxZjDoeY1idiCWRT24JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOzd|IN88US=> NEThTmRUSU6JRWK=
TE-9 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mm[1TY5pcWKrdHnvckBw\iCqdX3hckBVTS17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OVIxOSEQvF2= MnzuV2FPT0WU
TK10 cell M2nxPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2OVIzKM7:TR?= NF25S|VUSU6JRWK=
DSH1 cell Mn2wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofsTY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVM6PiEQvF2= NVTh[2lxW0GQR1XS
ECC12 cell M3;RZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NILvfFJKdmirYnn0bY9vKG:oIHj1cYFvKEWFQ{GyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTJ|MTFOwG0> MUfTRW5ITVJ?
EKVX cell M2fObGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXSN3ZKdmirYnn0bY9vKG:oIHj1cYFvKEWNVmigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDd2IN88US=> NFi3UZVUSU6JRWK=
HCC2218 cell MojWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3v1V2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkKxPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV|Mk[g{txO MnnmV2FPT0WU
LB2241-RCC cell M4D6Rmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MneyTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zNUSwN{DPxE1? MV3TRW5ITVJ?
LB996-RCC cell NVnjTnBxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnrhTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? M3;Qc3NCVkeHUh?=
LC-1F cell M124UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjTOHVnUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO NHS5R4RUSU6JRWK=
LS-513 cell Ml;vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFAxPDFizszN MVnTRW5ITVJ?

... 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

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:

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Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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