Lapatinib (GW-572016) Ditosylate

For research use only.

Catalog No.S1028

77 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 77 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 M1\GWXBzd2yrZnXyZZRqd25iYYPzZZk> Ml7uRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkWgZ4VtdCCuaX7lMEBKSzVyPUCuNFI2KM7:TR?= M4XtUFE3PDh|N{ey
BT474 cell line MkLZVJJwdGmoZYLheIlwdiCjc4PhfS=> MoHxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN MV2xOlQ5Ozd5Mh?=
HN5 cell NUHGZnY{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVWwTXZ{UW6qaXLpeIlwdiCxZjDIUlUh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNVIh|ryP M{K5ZVE3Pzd5NEGw
BT474 cell NVK1XnhyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDHTY5pcWKrdHnvckBw\iCEVES3OEBk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? NWjidoJ2OTZ5N{e0NVA>
N87 cell NYTCOWVwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jUcGlvcGmkaYTpc44hd2ZiTki3JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkC4JO69VQ>? NXPGdJpzOTZ5N{e0NVA>
HFF cell NX;wfoIzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvxdWZZUW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> M1fPT|E3Pzd5NEGw
SKBR3 cells NFTIcWdEgXSxdH;4bYNqfHliYYPzZZk> NHTjVlBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF5IN88US=> MYWxPVAzQDR{NR?=
A431 cells M3vhPGN6fG:2b4jpZ4l1gSCjc4PhfS=> M2TRfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlExPCEQvF2= MVyxPVg5QDd4MR?=
SKBR3 cells Mn\rR5l1d3SxeHnjbZR6KGG|c3H5 NGDPb2VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODJ7IN88US=> M2O4XlE6QDh6N{[x
HepG2 cells M4K5NHBzd2yrZnXyZZRqd25iYYPzZZk> Ml;lRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= NYjnfGdKOjBzNEO3O|g>
Hep3B2 cells M1nrVXBzd2yrZnXyZZRqd25iYYPzZZk> NHn6bG1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52OTFOwG0> MXWyNFE1Ozd5OB?=
SKHEP1 cells MnG0VJJwdGmoZYLheIlwdiCjc4PhfS=> M4XmTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjNizszN NHroe5YzODF2M{e3PC=>
MCF7 cells MoLZVJJwdGmoZYLheIlwdiCjc4PhfS=> NITTbI5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvPiEQvF2= MV6yNFE1Ozd5OB?=
MDA-MB-231 cells NFmyOmRRem:uaX\ldoF1cW:wIHHzd4F6 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNDFOwG0> MX[yNFE1Ozd5OB?=
SK-BR-3 cells M4jERXBzd2yrZnXyZZRqd25iYYPzZZk> MlHZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3CVk0{KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF0xNjB2IN88US=> NEDUc4szODF2M{e3PC=>
A431 cells M1myPGZ2dmO2aX;uJIF{e2G7 Mn3QTY5pcWKrdHnvckBw\iCHR1\SJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEF2M{GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5yNUKg{txO NGrkfFUzODN2Nk[1OS=>
N87 cells M2\4PGZ2dmO2aX;uJIF{e2G7 NWniU3AzUW6qaXLpeIlwdiCxZjDFdoJDOiCrboTyZYNmdGy3bHHyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOPFch[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6xJO69VQ>? M33Bc|IxOzR4NkW1
MIAPaCa cells NVL1NI5wTnWwY4Tpc44h[XO|YYm= NVnuVnB[UW6qaXLpeIlwdiCxZjDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOUUGSYVPhJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwNEOzJO69VQ>? M3jue|IxQDF5NUKz
MIAPaCa cells Mn3NSpVv[3Srb36gZZN{[Xl? M2HyUGlvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zNDFOwG0> NV62ZXc{OjB6MUe1NlM>
CAL27 cells M4PpSmN6fG:2b4jpZ4l1gSCjc4PhfS=> MmHSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2FNOjdiY3XscJMhd3[ncnX4dJJme3OrbnegSWdHWiCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2wMlAxPyEQvF2u NIm5dJozOTB6ME[yPS=>
SKOV3 cells NIH0TopEgXSxdH;4bYNqfHliYYPzZZk> MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDISXIzKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA{KM7:TT6= NXnOe49mOjFyOEC2Nlk>
CAL27 cells M1zXPGZ2dmO2aX;uJIF{e2G7 MkGzNVYhcA>? M{LoXGlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0MEBKSzVyPUCuNFMzKM7:TR?= MofkNlExQDB4Mkm=
SK-BR-3 cells NWXreXNOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGSwVXdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVz[kJ{IH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJHNMNUKULUOgZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFMzKM7:TR?= M2npSlIyPTdyOESz
BXF T24 cells NV;LOFliS3m2b4TvfIlkcXS7IHHzd4F6 NITIOIY1KGSjeYO= NFfHVoREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDYEZiVEK0JINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF06NjZ3IN88US=> M1fNflIzOTZ7NkCx
CXF 269L cells NYCwNItDS3m2b4TvfIlkcXS7IHHzd4F6 Mo\0OEBl[Xm| NHXTUm9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEYEZiMk[5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:QC5|NjFOwG0> M3HJS|IzOTZ7NkCx
DIFI cells MUXDfZRwfG:6aXPpeJkh[XO|YYm= NEDO[Hc1KGSjeYO= NIjsbFFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFUU[LIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlI{PSEQvF2= NVizfYI2OjJzNkm2NFE>
HT-29 cells Mmr5R5l1d3SxeHnjbZR6KGG|c3H5 NWXvW5N4PCCmYYnz NV7Sd41HS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVQvPjJizszN MWqyNlE3QTZyMR?=
RKO cells NXq2W21HS3m2b4TvfIlkcXS7IHHzd4F6 M13qcFQh\GG7cx?= MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDST28h[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwM{Wg{txO NGqweoYzOjF4OU[wNS=>
GXF251L cells NHXTR2pEgXSxdH;4bYNqfHliYYPzZZk> NIW1cpU1KGSjeYO= NYPFPFU1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT1iIMkWxUEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OS52ODFOwG0> MoexNlIyPjl4MEG=
LIXF 575L cells NHTudXlEgXSxdH;4bYNqfHliYYPzZZk> M3zvWFQh\GG7cx?= MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMTXhHKDV5NVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvOThizszN NY\sbZBWOjJzNkm2NFE>
LXFA 289L cells NIHJ[4pEgXSxdH;4bYNqfHliYYPzZZk> NH\wRZo1KGSjeYO= NF3aeHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEK4PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwN{mg{txO NGfzbZkzOjF4OU[wNS=>
LXFA 526L NYLa[FFES3m2b4TvfIlkcXS7IHHzd4F6 NVjrWFhPPCCmYYnz NHO1SVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEWyOmwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTRwMkGg{txO NFqyS3QzOjF4OU[wNS=>
LXFA 629L cells NWHlV2NiS3m2b4TvfIlkcXS7IHHzd4F6 NH3kbIY1KGSjeYO= Mli0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHSSB4MknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0zNjh5IN88US=> NILOeXYzOjF4OU[wNS=>
LXFL 1121L cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= NIrvd4k1KGSjeYO= NXrzRVNnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDCxNVIyVCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nz63N{DPxE1? NFXYfFczOjF4OU[wNS=>
LXFL 529L cells NV;acGxRS3m2b4TvfIlkcXS7IHHzd4F6 MkGyOEBl[Xm| NYH5[3VHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDC1NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkWxJO69VQ>? M3G4[FIzOTZ7NkCx
MCF7 cells M2\ybmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYK0JIRigXN? NEewZYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20Mlg{KM7:TR?= MYmyNlE3QTZyMR?=
MDA231 cells NUDBUVk1S3m2b4TvfIlkcXS7IHHzd4F6 NWW0fnF7PCCmYYnz NEHkTY9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF{M{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvPyEQvF2= NHnWcVUzOjF4OU[wNS=>
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PAXF 546L cells Mn\NR5l1d3SxeHnjbZR6KGG|c3H5 MXu0JIRigXN? NIT6VYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSViIIEW0Omwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwMUKg{txO M1u4[lIzOTZ7NkCx
PANC1 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= MmDROEBl[Xm| MnfkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFPSzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUiuNVIh|ryP NU\ndIRuOjJzNkm2NFE>
22Rv1 cell MXPDfZRwfG:6aXPpeJkh[XO|YYm= NHHGVoY1KGSjeYO= NIn1VFREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAzOlK4MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok4xPiEQvF2= M2LWXVIzOTZ7NkCx
DU145 cells NWTiW5VKS3m2b4TvfIlkcXS7IHHzd4F6 NG\IPIc1KGSjeYO= NFzuWFVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Nk46QSEQvF2= NYD5O2Y3OjJzNkm2NFE>
LNCAP cells NEHudYxEgXSxdH;4bYNqfHliYYPzZZk> NXyze4hxPCCmYYnz MnvGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUOuOlgh|ryP NYGwdGhGOjJzNkm2NFE>
PC3M cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NITsSZA1KGSjeYO= NXrxU2hVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|TTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE42PSEQvF2= NIWzSo8zOjF4OU[wNS=>
NIH/3T3 cells MljYVJJwdGmoZYLheIlwdiCjc4PhfS=> MWG3NkBp M4DSSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuN{DPxE1? Ml:1NlI2QTVzN{e=
NCI-H1648 cell M2TXNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEe2OINKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEK1OFQh|ryP NIfFVHlUSU6JRWK=
NMC-G1 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPYNXhKdmirYnn0bY9vKG:oIHj1cYFvKE6PQz3HNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTR3MEGg{txO M{HWdHNCVkeHUh?=
NTERA-S-cl-D1 cell NWLnPINoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUfuNJU4UW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPjV4MTFOwG0> NF3zZpZUSU6JRWK=
OCUB-M cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFU4PCEQvF2= M2rXe3NCVkeHUh?=
OS-RC-2 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFnsPVJKdmirYnn0bY9vKG:oIHj1cYFvKE:VLWLDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl7MUm5JO69VQ>? Ml;jV2FPT0WU
OVCAR-4 cell M1LmVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWTKcW8{UW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk01KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS5zMU[3OUDPxE1? MmXyV2FPT0WU
RL95-2 cell NFTsTIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWXaWok{UW6qaXLpeIlwdiCxZjDoeY1idiCUTEm1MVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjF3Nkeg{txO M2fpOXNCVkeHUh?=
SW954 cell NGDTXZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkDITY5pcWKrdHnvckBw\iCqdX3hckBUXzl3NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|kzPDVizszN MX\TRW5ITVJ?
SW962 cell MojVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXHNTHc1UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl{NEWg{txO NFGzTlZUSU6JRWK=
TE-1 cell M1XpV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEWzPWdKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlAzOTV7IN88US=> NH34NXhUSU6JRWK=
A253 cell NITiVlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIjNZo5KdmirYnn0bY9vKG:oIHj1cYFvKEF{NUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA1QDNizszN M2PxfnNCVkeHUh?=
A388 cell NV\ZW5FHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHLESJBKdmirYnn0bY9vKG:oIHj1cYFvKEF|OEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA1QDNizszN MWDTRW5ITVJ?
BB30-HNC cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUKzflRkUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP NFTKdGVUSU6JRWK=
TE-12 cell MkjtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn3ITY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|IzPThizszN M{DBV3NCVkeHUh?=
TE-5 cell NU\mSXBzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLLTY5pcWKrdHnvckBw\iCqdX3hckBVTS13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFY2PCEQvF2= MljIV2FPT0WU
TE-6 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5NFU4KM7:TR?= NWDOW4luW0GQR1XS
TE-8 cell Mnz6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlfBTY5pcWKrdHnvckBw\iCqdX3hckBVTS16IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6wN|c{KM7:TR?= NVn4ZYNmW0GQR1XS
TE-9 cell NI\xbGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml3MTY5pcWKrdHnvckBw\iCqdX3hckBVTS17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OVIxOSEQvF2= NGT3UpJUSU6JRWK=
TK10 cell NYjmXVdxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2OVIzKM7:TR?= MYLTRW5ITVJ?
DSH1 cell NXPiU3ZHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGRUUDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5N|k3KM7:TR?= NYTpUHVqW0GQR1XS
ECC12 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHMR4h{UW6qaXLpeIlwdiCxZjDoeY1idiCHQ1OxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODl{M{Gg{txO MYHTRW5ITVJ?
EKVX cell NFnvV4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= MojYV2FPT0WU
HCC2218 cell MneyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2izVWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkKxPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV|Mk[g{txO MXPTRW5ITVJ?
LB2241-RCC cell M37jVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrGW4JKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkK0NU1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkG1OFA{KM7:TR?= NXKzXmp{W0GQR1XS
LB996-RCC cell MnLnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml;oTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? Mnn5V2FPT0WU
LC-1F cell M1K0TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGxENTGIIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zPFI1PCEQvF2= MXXTRW5ITVJ?
LS-513 cell NXLvO2czT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFAxPDFizszN MmXQV2FPT0WU

... 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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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)

  • Mass
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    Volume
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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):
    C7=C6/X C7: LOG(C7):
    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