Lapatinib (GW-572016)

Catalog No.S2111 Synonyms: GSK572016, GW2016

For research use only.

Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

Lapatinib (GW-572016) Chemical Structure

CAS No. 231277-92-2

Selleck's Lapatinib (GW-572016) has been cited by 421 publications

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Biological Activity

Description Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
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 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 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 inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib 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 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
LB2241-RCC M4TuO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TLWmlEPTB;MT6xOVQxOyEQvF2= NWPvSXBuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
TE-9 MlGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S4NmlEPTB;MD63OFQ2OyEQvF2= NHLuT3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
A388 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PYTmlEPTB;MD63NlI2QCEQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TE-12 M4\HO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkX1TWM2OD1yLkS5NFU4KM7:TR?= NHHyNmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
EKVX NEjFN2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[yTY9yUUN3ME2wMlQ1QDd2IN88US=> NUXCS4JHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
BB30-HNC Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELISFdKSzVyPUCuNlQ3PTRizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
BT-474 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDNSm5KSzVyPUCuNlE{OTVizszN NVrMelRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
DSH1 M3\kVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPoWHZKSzVyPUCuNFk{QTZizszN NHe3[|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
ECC12 M3jMSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LaSmlEPTB;MD6wPVI{OSEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
OCUB-M NXnqUFd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H3V2lEPTB;MD6wOVc1KM7:TR?= NW\CbGJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
HCC2218 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX75c4tEUUN3ME2wMlA2OzJ4IN88US=> Mo\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
NCI-H1648 NIXZfZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv4TWM2OD1yLkCyOVQ1KM7:TR?= NF:zXZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
LB996-RCC NF3zb3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jFU2lEPTB;MT6zOlIzQCEQvF2= M2nI[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
LC-1F M33Jfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwM{iyOFQh|ryP NF75bZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
TE-6 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwNUWyNFEh|ryP NH[5[Xo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
A253 NGKzUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\UemlEPTB;MT65O|M{PSEQvF2= NV7uTGtNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
OS-RC-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFwOUmxPVkh|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TE-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPXNFNKSzVyPUKuNFQ5OyEQvF2= MlzhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
RL95-2 Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTNwMUW2O{DPxE1? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
LS-513 NYS5OWlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf2c5B6UUN3ME2zMlQxODRzIN88US=> M1jJSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
DJM-1 NF\keW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTNwNE[5O|Uh|ryP NIPFW5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
NMC-G1 MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HJTWlEPTB;Mz61OFUxOSEQvF2= M4n3c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
TE-10 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXxOngxUUN3ME2zMlU2OzV4IN88US=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TE-5 M3HLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHje2ZKSzVyPUSuNFM4OyEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TK10 NHP1Z3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC0TWM2OD12LkG2OVIzKM7:TR?= NVPwTlVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
UACC-812 M{D3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTRwNU[xOVMh|ryP M1HRfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
SW962 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnJTWM2OD13LkCyNVU6KM7:TR?= M130[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
SW954 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTVwM{myOFUh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
COLO-668 M2LDcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnDXW9uUUN3ME21MlczPjZ5IN88US=> M3zJOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
LB1047-RCC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTVwOECwOFYh|ryP M3vhT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
NB5 NXO1VINqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTZwMkGwNFEh|ryP MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
NTERA-S-cl-D1 MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTZwMk[1OlEh|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
IST-MEL1 MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;ITWM2OD14LkSzOlk1KM7:TR?= NYixcXRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
GI-1 M4fqdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\CcopKSzVyPU[uOVE3QDJizszN MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TGBC1TKB NE\rcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTdwMEexPFMh|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
GT3TKB MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTdwMkK3OFQh|ryP M2K4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
EVSA-T NXzRcHV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfYTWM2OD15LkSyPFEyKM7:TR?= M4G2eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
D-502MG NXW2bFNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W1SmlEPTB;Nz60PFg6PCEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TE-8 NHL1S2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTdwN{[xOVkh|ryP NGfnR3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
OVCAR-4 NX;UZ21tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W2VGlEPTB;OT6xNVY4PSEQvF2= NHHnWWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
D-336MG NVe0eFFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2SySGlEPTB;OT60O|M6PSEQvF2= M{\O[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
GCIY M2j0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXxfpplUUN3ME25MlU4PDJizszN MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
KS-1 NVnZfJcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrFTWM2OD17Lk[2Nlg4KM7:TR?= NUixUJZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
HCC2998 NF\vSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS1VJJjUUN3ME25Mlk3OzB5IN88US=> M4faPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
D-247MG M3P4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjibVFKSzVyPUmuPVgzQTFizszN MlG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
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Assay
Methods Test Index PMID
Western blot ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP ; p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1 29799521 28938602 22853430
Immunofluorescence LC3 ; Vimentin / E-cadherin 26637440 28243326
Growth inhibition assay Cell viability (OE19) ; Cell viability (A431 cells) 25350844 28243326
In vivo Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. [1]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
  • 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.
Animal Research:[1]
  • 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

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(172.09 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+5% Tween 80+ddH2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 581.06
Formula

C29H26ClFN4O4S

CAS No. 231277-92-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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
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
NCT01782651 Completed Drug: Lapatinib plus capecitabine Neoplasms Breast GlaxoSmithKline August 2014 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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Frequently Asked Questions

Question 1:
If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

Answer:
For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

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