Lapatinib (GW-572016) Ditosylate

For research use only.

Catalog No.S1028

98 publications

Lapatinib (GW-572016) Ditosylate Chemical Structure

CAS No. 388082-77-7

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.

Selleck's Lapatinib (GW-572016) Ditosylate has been cited by 98 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 MonQVJJwdGmoZYLheIlwdiCjc4PhfS=> NEfVV2lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NYLSd4F5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0PFM4PzJpPkG2OFg{Pzd{PD;hQi=>
BT474 cell line MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NWfXXGlCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsJIxqdmVuIFnDOVA:OC5yMkWg{txO NXuzc2F2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0PFM4PzJpPkG2OFg{Pzd{PD;hQi=>
HN5 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2Lk[GlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjd5N{SxNEc,OTZ5N{e0NVA9N2F-
BT474 cell NIfFT|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHPQepdKdmirYnn0bY9vKG:oIFLUOFc1KGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{whUUN3ME2wMlA5KM7:TR?= NX6wVWx5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[3O|c1OTBpPkG2O|c4PDFyPD;hQi=>
N87 cell NWO0UpI5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\xTY5pcWKrdHnvckBw\iCQOEegZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEig{txO Mor2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ5N{e0NVAoRjF4N{e3OFExRC:jPh?=
HFF cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MojPTY5pcWKrdHnvckBw\iCKRl[gZ4VtdCCpcn;3eIgtKEmFNUC9PU46KM7:TR?= NYPU[VBFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[3O|c1OTBpPkG2O|c4PDFyPD;hQi=>
BT474 M{nwXmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NH;ER5RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHzzJI93\XKneIDy[ZN{cW6pIFXyRlItKEmFNUC9NE4xOjYQvF2= NGCxNWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[1N|M{Oyd-MUi2OVM{OzN:L3G+
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Hep3B2 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NFuz[YhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52Od88US=> Mnv2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzNEO3O|goRjJyMUSzO|c5RC:jPh?=
HepG2 NXi1OGVVSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2DXcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvOjgQvF2= NVPaWJRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOFM4PzhpPkKwNVQ{Pzd6PD;hQi=>
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OS-RC-2 cell M3z3VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIi1S2lKdmirYnn0bY9vKG:oIHj1cYFvKE:VLWLDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl7MUm5JO69VQ>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
OVCAR-4 cell NUjZcVB3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3X1XWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO MlfoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
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SW954 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= NEi0d4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
SW962 cell M2LnZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLFTY5pcWKrdHnvckBw\iCqdX3hckBUXzl4MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|kzPDVizszN Mn\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
TE-1 cell MmfzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvRS4V{UW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4xOjF3OTFOwG0> M4r0R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
A253 cell M1rrcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkDRTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= M3SzPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
A388 cell MoTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
BB30-HNC cell M4faN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEG4RlRKdmirYnn0bY9vKG:oIHj1cYFvKEKEM{CtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57N{OzOUDPxE1? MnLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
TE-12 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1HmemlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczOjV6IN88US=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TE-5 cell NFy3V5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= M{HXU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
TE-6 cell MoPYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HOd2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFkxPTdizszN NHXJXpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
TE-8 cell NYm2bWFlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkCzO|Mh|ryP NX;LV3hlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
TE-9 cell NEfZbFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4PnOWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVUzODFizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TK10 cell M2OwNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\oXVdKdmirYnn0bY9vKG:oIHj1cYFvKFSNMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE3PTJ{IN88US=> NYDmZ2N2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
DSH1 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnWzTY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVM6PiEQvF2= NXjmd2drRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
ECC12 cell NHzXWZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fGZWlvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6OjNzIN88US=> MnjtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
EKVX cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHz4eWhKdmirYnn0bY9vKG:oIHj1cYFvKEWNVmigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDd2IN88US=> NEnEWmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
HCC2218 cell NGPpfolIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXjt[IVvUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNlE5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNUOyOkDPxE1? NIfqOlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
LB2241-RCC cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF3NECzJO69VQ>? MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
LB996-RCC cell NX;oXFMzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVfQTolGUW6qaXLpeIlwdiCxZjDoeY1idiCOQkm5Ok1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkO2NlI5KM7:TR?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
LC-1F cell NVixc5JQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXHUYFKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUHGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{QDJ2NDFOwG0> NV6yblJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
LS-513 cell MlXHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mli1TY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQxODRzIN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-

... 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]
- Collapse
  • 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+40% PEG 300+5% Tween 80+53% ddH2O
For best results, use promptly after mixing.
1.25 mg/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.CC1=CC=C(C=C1)S(=O)(=O)O.CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

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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
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / 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
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / 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
NCT04608409 Recruiting Drug: Lapatinib and Paclitaxel Ovarian Cancer Frederick R. Ueland M.D.|University of Kentucky November 16 2020 Phase 1
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
NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie September 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