Lapatinib

Catalog No.S2111 Synonyms: GW-572016, GSK572016

Lapatinib Chemical Structure

Molecular Weight(MW): 581.06

Lapatinib, 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.

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Cited by 38 Publications

7 Customer Reviews

  • Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).

    Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck.

    Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies.

    Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck.

  • Inhibition of HER2 using siRNAs show a similar response measured by induced apoptosis, decreased proliferation and decreased phospho-p70-S6K staining as Lapatinib mono-treatment and combinatorial treatment with Lapatinib and trastuzumab. Trastuzumab mono-treatment is less efficient than siHER2.

    Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck.

    Lapatinib effectively inhibits EGFR activation, leading to a reduc- tion in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 μM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck.

  •  

    Endogenous associations between STAT1, EGFR, and p-STAT3 expression in breast cancer cells. (B) Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 uM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck.

    Combination treatment with lapatinib and CZ0775 significantly induces pro-apoptotic BIM proteins in H195 cells. HCC827 (a) and H1975 (b) cells were treated with either 1 μM lapatinib alone or the combination of 1 μM lapatinib plus 1 μM AZD6244 or CZ0775 for 24 h. Cell lysates were analyzed by Western blotting using the indicated antibodies. The levels of β -actin served as a loading control

    Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck.

  •  

    EGF and TGF-α-induced CD44 expression is reduced by EGFR inhibitors in SKBR3 breast cancer cells. After serum-starvation for 24 h, the cells were pretreated with EGFR inhibitors, AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then, treated with EGF (A) or TGF-α (B) for 24 h. The level of CD44 mRNA expression was analyzed by real-time PCR. After serum-starvation for 24 h, the cells were pretreated with AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then treated with EGF for 24 h (C). The levels of CD44, EGFR, ERK, and β-actin protein expression were analyzed by Western blotting.

    Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Lapatinib, 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.
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
NCI-H1648 NYq3XJVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[3b2lEPTB;MD6wNlU1PCEQvF2= MULTRW5ITVJ?
HCC2218 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvGb2lMUUN3ME2wMlA2OzJ4IN88US=> NEW0S|lUSU6JRWK=
OCUB-M NIGwTphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TS[GlEPTB;MD6wOVc1KM7:TR?= MWDTRW5ITVJ?
ECC12 NUfCN2NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMEmyN|Eh|ryP NVfNNlZvW0GQR1XS
DSH1 M{j4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHDUHdnUUN3ME2wMlA6Ozl4IN88US=> M33DNXNCVkeHUh?=
BT-474 M2S0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDze|ZoUUN3ME2wMlIyOzF3IN88US=> M4W2TXNCVkeHUh?=
BB30-HNC NULpeVlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwMkS2OVQh|ryP MYfTRW5ITVJ?
EKVX Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL3TWM2OD1yLkS0PFc1KM7:TR?= M{L0T3NCVkeHUh?=
TE-12 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXETWM2OD1yLkS5NFU4KM7:TR?= NVfoZZBGW0GQR1XS
A388 Mn\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwN{KyOVgh|ryP NETGXW9USU6JRWK=
TE-9 MnnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwN{S0OVMh|ryP NVnyZ|lnW0GQR1XS
LB2241-RCC MljjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwMUW0NFMh|ryP NYP3VVlRW0GQR1XS
LB996-RCC NI[xTWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV23cXBYUUN3ME2xMlM3OjJ6IN88US=> M1T1O3NCVkeHUh?=
LC-1F NYTPXY5uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fPemlEPTB;MT6zPFI1PCEQvF2= M2j0RnNCVkeHUh?=
TE-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwNUWyNFEh|ryP MYLTRW5ITVJ?
A253 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrZTWM2OD1zLkm3N|M2KM7:TR?= MkfuV2FPT0WU
OS-RC-2 MljpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD2TXA3UUN3ME2xMlk6OTl7IN88US=> NHzHXmlUSU6JRWK=
TE-1 NGrKdHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJwMES4N{DPxE1? NVTWdWFOW0GQR1XS
RL95-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjYXnZ6UUN3ME2zMlE2PjdizszN NWnL[5o6W0GQR1XS
LS-513 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;HfnM4UUN3ME2zMlQxODRzIN88US=> MWHTRW5ITVJ?
DJM-1 MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;X[oFKSzVyPUOuOFY6PzVizszN NFq3cJNUSU6JRWK=
NMC-G1 NGD3SINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\Ld|JiUUN3ME2zMlU1PTBzIN88US=> M3nFZXNCVkeHUh?=
TE-10 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTyTWM2OD1|LkW1N|U3KM7:TR?= M3fncHNCVkeHUh?=
TE-5 M1zTN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHFO2RKSzVyPUSuNFM4OyEQvF2= MX7TRW5ITVJ?
TK10 NELOfVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTRwMU[1NlIh|ryP M3HuS3NCVkeHUh?=
UACC-812 M2\lcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCwN3lKSzVyPUSuOVYyPTNizszN Mnm1V2FPT0WU
SW962 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nH[mlEPTB;NT6wNlE2QSEQvF2= NFrUSYpUSU6JRWK=
SW954 NWPUTmtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjSTWM2OD13LkO5NlQ2KM7:TR?= NFPvNWFUSU6JRWK=
COLO-668 NWC5TWlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTVwN{K2Olch|ryP NYLDNI1jW0GQR1XS
LB1047-RCC NULlV5dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX6b5dEUUN3ME21MlgxODR4IN88US=> MX3TRW5ITVJ?
NB5 M4DrOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHDTGlKSzVyPU[uNlExODFizszN NW\E[nFlW0GQR1XS
NTERA-S-cl-D1 NYm5dHB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjUTWM2OD14LkK2OVYyKM7:TR?= Ml:zV2FPT0WU
IST-MEL1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XOfGlEPTB;Nj60N|Y6PCEQvF2= NIL1U5ZUSU6JRWK=
GI-1 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTZwNUG2PFIh|ryP MX;TRW5ITVJ?
TGBC1TKB M3;5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTdwMEexPFMh|ryP MWfTRW5ITVJ?
GT3TKB NWPiXXNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzTOVlKSzVyPUeuNlI4PDRizszN MnfEV2FPT0WU
EVSA-T NFXz[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{CwXWlEPTB;Nz60NlgyOSEQvF2= NF3rbZpUSU6JRWK=
D-502MG NULz[WM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTScFZKSzVyPUeuOFg5QTRizszN NY\kSlhRW0GQR1XS
TE-8 M2LvZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVToT5NkUUN3ME23Mlc3OTV7IN88US=> M2fyPHNCVkeHUh?=
OVCAR-4 MoXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\1cGlEPTB;OT6xNVY4PSEQvF2= NXHBbmpYW0GQR1XS
D-336MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTlwNEezPVUh|ryP MYPTRW5ITVJ?
GCIY NV3hO|JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:yVW5KSzVyPUmuOVc1OiEQvF2= NWf3dotuW0GQR1XS
KS-1 NFm1V4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTGOXlzUUN3ME25MlY3Ojh5IN88US=> NGDaUXBUSU6JRWK=
HCC2998 MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTlwOU[zNFch|ryP NEDrNVFUSU6JRWK=
D-247MG M4ewPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nCUGlEPTB;OT65PFI6OSEQvF2= M{f2OXNCVkeHUh?=
TE-15 MmizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGni[FBKSzVyPUGwMlI1PSEQvF2= MlvhV2FPT0WU
IST-MES1 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[1TWM2OD1zMD6yOVY2KM7:TR?= NIe3coxUSU6JRWK=
ETK-1 M{TDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nLcWlEPTB;MUCuOlI{KM7:TR?= M17LR3NCVkeHUh?=
RCC10RGB MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDMVlJUUUN3ME2xNE46PjFizszN NGHyZ4RUSU6JRWK=
KNS-42 Mm\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHrTWM2OD1zMT63NlU2KM7:TR?= NGnudnZUSU6JRWK=
LB771-HNC M4nWemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTF{LkG3NVIh|ryP NHfXVpFUSU6JRWK=
SR MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvtOIxQUUN3ME2xNk4zODZ2IN88US=> M37L[HNCVkeHUh?=
NCI-H1355 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDlSnFIUUN3ME2xNk45QTh3IN88US=> NUjJWWE6W0GQR1XS
ES6 NWnqRXhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTQTWM2OD1zMz6wO|gh|ryP NF7xOWVUSU6JRWK=
SK-NEP-1 NWjNfWxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTjXW1KSzVyPUGzMlI2PzdizszN NXvjfHU2W0GQR1XS
D-392MG MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfuTWM2OD1zMz62OFI5KM7:TR?= NVqwUGg3W0GQR1XS
NB7 MmPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLFTWM2OD1zND6yN|c1KM7:TR?= NVPBOmF3W0GQR1XS
SK-LMS-1 M1HBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTF2LkWxOFUh|ryP NFnDZ5FUSU6JRWK=
SK-UT-1 M4X5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zKdWlEPTB;MUSuO|g5QSEQvF2= NFvwT5hUSU6JRWK=
CA46 NFKxUINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF3LkC1PFYh|ryP M{LUbXNCVkeHUh?=
IST-SL2 NYPRXJVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF3LkG5NFEh|ryP NYDtfHRtW0GQR1XS
BC-1 M2LnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXaTXVtUUN3ME2xOU4{OzF2IN88US=> MWHTRW5ITVJ?
LS-123 NH7hSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTF3LkixO|Mh|ryP M1L4dHNCVkeHUh?=
Ramos-2G6-4C10 NEPqT|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPMTWM2OD1zNj6wPVI1KM7:TR?= MmrLV2FPT0WU
MZ1-PC MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ubmlEPTB;MU[uO|MyOyEQvF2= NYHJTnFJW0GQR1XS
LB647-SCLC MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7aN2RKSzVyPUG2Mlk{PzJizszN NHL1ZVdUSU6JRWK=
NCI-H1694 M1rIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\iTWM2OD1zNz6xOVI6KM7:TR?= NX\RNHRXW0GQR1XS
NCI-H322M MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO5RlViUUN3ME2xO{41OzZ4IN88US=> M2LvcHNCVkeHUh?=
ES7 NUXDNYVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n3VWlEPTB;MUiuN|kyPCEQvF2= NVnKcpBpW0GQR1XS
LC-2-ad MnroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT5elR[UUN3ME2xPE41Ozh4IN88US=> NXjLbZJnW0GQR1XS
SF268 NID3fVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PHdmlEPTB;MUiuO|QxQSEQvF2= NY\UW3ZJW0GQR1XS
RPMI-8402 M{TnbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF7LkC3OFIh|ryP NVHxeHdRW0GQR1XS
HCE-T MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fC[GlEPTB;MkCuNlM1PCEQvF2= NY\GcIdWW0GQR1XS
A101D M3\UNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJyLki1PFch|ryP NUKwS283W0GQR1XS
MRK-nu-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH2wUIVKSzVyPUKwMlkyOyEQvF2= MXXTRW5ITVJ?
LXF-289 NFfEOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT5TWM2OD1{MT6wN|gh|ryP NIrQd2hUSU6JRWK=
NALM-6 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn4TWM2OD1{MT6xPVY4KM7:TR?= NH\kVmFUSU6JRWK=
DOHH-2 NGnvZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvaSXVKSzVyPUKxMlQ5OTNizszN MoXMV2FPT0WU
EW-16 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJ{LkG0NFIh|ryP MmG5V2FPT0WU
A4-Fuk MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u0c2lEPTB;MkKuNlE1QSEQvF2= M3zV[HNCVkeHUh?=
HD-MY-Z Mk[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXwTWM2OD1{Mj6zPVY2KM7:TR?= M3;uZnNCVkeHUh?=
SKM-1 NF\1cJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTZOI9KSzVyPUKyMlc{PTFizszN NVzOWHhLW0GQR1XS
DMS-153 NFLZOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTUPHJkUUN3ME2yN{41OjB2IN88US=> NV;oNINXW0GQR1XS
LB373-MEL-D M3G0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnLSJNMUUN3ME2yN{42PDV{IN88US=> MVrTRW5ITVJ?
LP-1 NFP6S4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkWwTWM2OD1{Mz64NFk4KM7:TR?= MYjTRW5ITVJ?
GI-ME-N M1;kNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLnSItKSzVyPUK0MlI6OiEQvF2= M1vpV3NCVkeHUh?=
MPP-89 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3ncIxKSzVyPUK1MlIxOzZizszN Ml\4V2FPT0WU
U-698-M NGHLN5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DUVmlEPTB;MkWuNlUxOyEQvF2= MXjTRW5ITVJ?
HC-1 M1[4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\nS2lEPTB;MkWuOlQyQCEQvF2= MXjTRW5ITVJ?
HCC2157 M33JTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHtb3l3UUN3ME2yOU43PzNizszN NWn3XFRbW0GQR1XS
MOLT-4 NGXBc3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HkdGlEPTB;Mk[uNlc{KM7:TR?= NVyzZ|V3W0GQR1XS
LS-411N NGTxVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K4fGlEPTB;Mk[uN|M3QSEQvF2= M2rn[HNCVkeHUh?=
Becker MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkeyTWM2OD1{Nj61NVgyKM7:TR?= NUO1UHZpW0GQR1XS
NCI-H23 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr4TWM2OD1{Nj63OVc2KM7:TR?= MVHTRW5ITVJ?
IST-SL1 NImyWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV63fmpbUUN3ME2yO{4{QDZ5IN88US=> M2\3NHNCVkeHUh?=
MZ2-MEL MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIKyOFVKSzVyPUK3MlQ2PjZizszN Ml;QV2FPT0WU
RKO M2PkXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJ6LkG0OFYh|ryP MUnTRW5ITVJ?
TE-441-T NXrWPHo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJ6Lke4PUDPxE1? NX;IOVJlW0GQR1XS
EW-24 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTNV5NKSzVyPUK5MlEzPTlizszN NFLuOVZUSU6JRWK=
no-10 NIK2[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVewV4dKUUN3ME2yPU4yPjNzIN88US=> MnjoV2FPT0WU
D-542MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPVTWM2OD1{OT65NlIyKM7:TR?= M3foO3NCVkeHUh?=
ST486 MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTNyLk[0OVEh|ryP Mkn1V2FPT0WU
KURAMOCHI NHPTbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfQPY9ZUUN3ME2zNE45ODV5IN88US=> NIXPSlFUSU6JRWK=
ES8 NWTpXXVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTNzLkW5O|Ih|ryP NEfxXXlUSU6JRWK=
BL-41 NVTJXYFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1u4RWlEPTB;M{KuNVA2PCEQvF2= MVTTRW5ITVJ?
NB6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN{LkO4OVUh|ryP M3rPdHNCVkeHUh?=
NCI-H1304 NYm2SYVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTN{LkS5Olch|ryP M1ewTHNCVkeHUh?=
MS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr4V2h7UUN3ME2zNk44PzVzIN88US=> M3HnPXNCVkeHUh?=
MFH-ino MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTmOYZKSzVyPUO0MlMzOjRizszN MX7TRW5ITVJ?
NOS-1 NYLxOWhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTN2Lk[3OFgh|ryP M3TtPXNCVkeHUh?=
HUTU-80 NUXIbYhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrMOFVrUUN3ME2zOU4{PjZ5IN88US=> M{TUO3NCVkeHUh?=
EB2 NYTHPZpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH0SoRHUUN3ME2zOk43OTh7IN88US=> NFq5O5VUSU6JRWK=
L-540 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX3[XZIUUN3ME2zO{4zOzB6IN88US=> M3fYN3NCVkeHUh?=
NCI-H747 MoTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG0cohbUUN3ME2zPE45QDR4IN88US=> MVrTRW5ITVJ?
NCI-H446 NF[wZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fsNmlEPTB;M{muPVY2OSEQvF2= NGe0dFVUSU6JRWK=
MOLT-16 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInqO5NKSzVyPUSyMlQyPSEQvF2= NFHnOGtUSU6JRWK=
BC-3 MkO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7FTWM2OD12NT60PFk3KM7:TR?= M4LNNHNCVkeHUh?=
SJSA-1 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljJTWM2OD12NT61OFc1KM7:TR?= NYLnbIV3W0GQR1XS
BB65-RCC M3TZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvpTnE4UUN3ME20OU43PjZizszN NGnHeVRUSU6JRWK=
SNB75 NF;H[VVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDuTWM2OD12Nj6wNVgh|ryP Mnf3V2FPT0WU

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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 (172.09 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+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 581.06
Formula

C29H26ClFN4O4S

CAS No. 231277-92-2
Storage powder
Synonyms GW-572016, GSK572016

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 (g) = Concentration (mol/L) × Volume (L) × 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 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
    V1
    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 Conditions Sponsor/Collaborators Start Date Phases
NCT00107003 Completed Glioma|Brain Tumor|Glioblastoma Multiforme|GBM|Gliosarcoma|GS National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 30, 2005 Phase 2
NCT00251433 Active, not recruiting Neoplasms, Breast Novartis Pharmaceuticals|Novartis September 26, 2005 Phase 1
NCT01306045 Recruiting Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 21, 2011 Phase 2
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|Phase 2
NCT02836847 Recruiting Cholangiocarcinoma of the Extrahepatic Bile Duct|Gallbladder Cancer Shanghai Jiao Tong University School of Medicine|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Ruijin Hospital|RenJi Hospital|Eastern Hepatobiliary Surgery Hospital|Huashan Hospital July 2016 Phase 2
NCT02650752 Recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 2016 Phase 1

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 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID