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

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)
C-Raf-1 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM 3.5 μM >10 μM
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 NHXwZ4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMEK1OFQh|ryP NVTpeIY6W0GQR1XS
HCC2218 M3y2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIixS29KSzVyPUCuNFU{OjZizszN NXjEc4hHW0GQR1XS
OCUB-M NFvZdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUC2VXNUUUN3ME2wMlA2PzRizszN M4jBTXNCVkeHUh?=
ECC12 NXnlSmE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTBwMEmyN|Eh|ryP MkfRV2FPT0WU
DSH1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[xN49KSzVyPUCuNFk{QTZizszN MnzHV2FPT0WU
BT-474 NH\vWmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;QTWM2OD1yLkKxN|E2KM7:TR?= M2e1b3NCVkeHUh?=
BB30-HNC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e0[WlEPTB;MD6yOFY2PCEQvF2= M2\NRnNCVkeHUh?=
EKVX Mle2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDBTWM2OD1yLkS0PFc1KM7:TR?= M4PZcnNCVkeHUh?=
TE-12 M1jESGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNEmwOVch|ryP NYiycZppW0GQR1XS
A388 NYHne5VWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwN{KyOVgh|ryP MljJV2FPT0WU
LB2241-RCC M2TGO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmiyTWM2OD1zLkG1OFA{KM7:TR?= MYTTRW5ITVJ?
LB996-RCC MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwM{[yNlgh|ryP M1rkdXNCVkeHUh?=
TE-6 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHjW3QxUUN3ME2xMlU2OjBzIN88US=> M{jxcHNCVkeHUh?=
A253 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFwOUezN|Uh|ryP MVHTRW5ITVJ?
TE-1 NXnCbHZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe5UJVOUUN3ME2yMlA1QDNizszN M2fZNnNCVkeHUh?=
RL95-2 M1rSS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTNwMUW2O{DPxE1? NGXwdIlUSU6JRWK=
LS-513 NF64cFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTNwNECwOFEh|ryP MW\TRW5ITVJ?
DJM-1 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTNwNE[5O|Uh|ryP MmHGV2FPT0WU
NMC-G1 M3jZc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrrTWM2OD1|LkW0OVAyKM7:TR?= MVrTRW5ITVJ?
TE-10 M3rlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHywZmNKSzVyPUOuOVU{PTZizszN M3\PcXNCVkeHUh?=
UACC-812 NES2cJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLMTWM2OD12LkW2NVU{KM7:TR?= NHfqU4xUSU6JRWK=
SW962 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTVwMEKxOVkh|ryP M1nXS3NCVkeHUh?=
SW954 M4fkVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXW[3NiUUN3ME21MlM6OjR3IN88US=> NIHWdFdUSU6JRWK=
COLO-668 NXS1O5dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7ETWM2OD13LkeyOlY4KM7:TR?= MVzTRW5ITVJ?
NB5 M4PoXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnhU2NKSzVyPU[uNlExODFizszN M33NfHNCVkeHUh?=
NTERA-S-cl-D1 Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTZwMk[1OlEh|ryP MXrTRW5ITVJ?
GI-1 M3rKO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTZwNUG2PFIh|ryP NX\lSoE3W0GQR1XS
EVSA-T NX3aXpZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\pUGlEPTB;Nz60NlgyOSEQvF2= M33rO3NCVkeHUh?=
D-502MG NH;WWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;1R4hWUUN3ME23MlQ5QDl2IN88US=> MkK3V2FPT0WU
TE-8 M2nacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT4TWM2OD15Lke2NVU6KM7:TR?= MnTSV2FPT0WU
OVCAR-4 M{LGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\K[pVKSzVyPUmuNVE3PzVizszN MXXTRW5ITVJ?
D-336MG NVL0NY1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTlwNEezPVUh|ryP Mn\DV2FPT0WU
GCIY NEP6S5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\NdmlEPTB;OT61O|QzKM7:TR?= M2LTfnNCVkeHUh?=
KS-1 NFzIW3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HYTWlEPTB;OT62OlI5PyEQvF2= Mlm5V2FPT0WU
HCC2998 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPYTWM2OD17Lkm2N|A4KM7:TR?= M4PsVXNCVkeHUh?=
D-247MG M{HiNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\qTWM2OD17Lkm4NlkyKM7:TR?= NV7uS3dYW0GQR1XS
TE-15 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFyLkK0OUDPxE1? MkfkV2FPT0WU
ETK-1 NUe3eVBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITD[49KSzVyPUGwMlYzOyEQvF2= M1rqWHNCVkeHUh?=
KNS-42 Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHGPIhKSzVyPUGxMlczPTVizszN NF60NmVUSU6JRWK=
SR NHnyZXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF{LkKwOlQh|ryP M1zkb3NCVkeHUh?=
ES6 NGrnfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj2S5NLUUN3ME2xN{4xPzhizszN NX\XfXRRW0GQR1XS
SK-NEP-1 MnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr4T5U3UUN3ME2xN{4zPTd5IN88US=> NVjLZ5VVW0GQR1XS
D-392MG M{j3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvrTWM2OD1zMz62OFI5KM7:TR?= NU\wZ285W0GQR1XS
NB7 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrhUHNIUUN3ME2xOE4zOzd2IN88US=> NEWwRYlUSU6JRWK=
SK-UT-1 M4m3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHJcWNwUUN3ME2xOE44QDh7IN88US=> Mmj5V2FPT0WU
CA46 Mm\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqzTWM2OD1zNT6wOVg3KM7:TR?= MlGzV2FPT0WU
IST-SL2 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;jTVlKSzVyPUG1MlE6ODFizszN NWj3e4pVW0GQR1XS
LS-123 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrGfWZKSzVyPUG1MlgyPzNizszN Ml\jV2FPT0WU
Ramos-2G6-4C10 NFHlNodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\TTWM2OD1zNj6wPVI1KM7:TR?= MX3TRW5ITVJ?
MZ1-PC NIHGXlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF4LkezNVMh|ryP M1rwTHNCVkeHUh?=
LB647-SCLC MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP0Um5KSzVyPUG2Mlk{PzJizszN MnjEV2FPT0WU
NCI-H1694 M33SWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPUTWM2OD1zNz6xOVI6KM7:TR?= MWLTRW5ITVJ?
NCI-H322M MkPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFW3WJhKSzVyPUG3MlQ{PjZizszN Mn;UV2FPT0WU
ES7 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n4NWlEPTB;MUiuN|kyPCEQvF2= M{DZdHNCVkeHUh?=
LC-2-ad MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrzTWM2OD1zOD60N|g3KM7:TR?= NIDScFlUSU6JRWK=
SF268 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvXN5VKSzVyPUG4Mlc1ODlizszN Ml6xV2FPT0WU
RPMI-8402 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUi3Rnl1UUN3ME2xPU4xPzR{IN88US=> MWPTRW5ITVJ?
HCE-T NHzldWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLHfHY{UUN3ME2yNE4zOzR2IN88US=> NVfsS4dNW0GQR1XS
A101D NHvubnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rseWlEPTB;MkCuPFU5PyEQvF2= NICyU2JUSU6JRWK=
MRK-nu-1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHsTWM2OD1{MD65NVMh|ryP M1XSbnNCVkeHUh?=
LXF-289 NYjIV3lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnHSGtpUUN3ME2yNU4xOzhizszN NUT4eWo3W0GQR1XS
NALM-6 M2DaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJzLkG5Olch|ryP M4HKWHNCVkeHUh?=
EW-16 M2\sdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3WWXlKSzVyPUKyMlE1ODJizszN NUXDN|hQW0GQR1XS
A4-Fuk NGjUVlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJ{LkKxOFkh|ryP Ml;PV2FPT0WU
HD-MY-Z NF7WUnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLqTWM2OD1{Mj6zPVY2KM7:TR?= NV[5OnJMW0GQR1XS
SKM-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDrTWM2OD1{Mj63N|UyKM7:TR?= NH3NW|hUSU6JRWK=
DMS-153 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLTTWM2OD1{Mz60NlA1KM7:TR?= NHrGOGFUSU6JRWK=
LB373-MEL-D M2q5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ|LkW0OVIh|ryP MX;TRW5ITVJ?
LP-1 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqwcIhKSzVyPUKzMlgxQTdizszN MYDTRW5ITVJ?
MPP-89 M3W4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHOPZJKSzVyPUK1MlIxOzZizszN MmrjV2FPT0WU
U-698-M MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2POSGlEPTB;MkWuNlUxOyEQvF2= Mn60V2FPT0WU
HC-1 MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm4e45KSzVyPUK1MlY1OThizszN M4HFNHNCVkeHUh?=
HCC2157 NUPtUYVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rXd2lEPTB;MkWuOlc{KM7:TR?= M1;zd3NCVkeHUh?=
MOLT-4 MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33KSWlEPTB;Mk[uNlc{KM7:TR?= MWXTRW5ITVJ?
LS-411N NYT2b3RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zJfGlEPTB;Mk[uN|M3QSEQvF2= M2LYZnNCVkeHUh?=
Becker NETBPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH2TWM2OD1{Nj61NVgyKM7:TR?= Mn2yV2FPT0WU
NCI-H23 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXSPHpYUUN3ME2yOk44PTd3IN88US=> M1TqU3NCVkeHUh?=
IST-SL1 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn6yTWM2OD1{Nz6zPFY4KM7:TR?= Ml\JV2FPT0WU
MZ2-MEL Mm\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T0OGlEPTB;MkeuOFU3PiEQvF2= NULqO2kxW0GQR1XS
TE-441-T M3nhb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvxTWM2OD1{OD63PFkh|ryP NHy2c2tUSU6JRWK=
EW-24 MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[zbW1KSzVyPUK5MlEzPTlizszN Ml:zV2FPT0WU
no-10 MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjIbYRKSzVyPUK5MlE3OzFizszN NXXM[ZNpW0GQR1XS
D-542MG MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu0TWM2OD1{OT65NlIyKM7:TR?= M1[0XHNCVkeHUh?=
ST486 M4TWeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r5bWlEPTB;M{CuOlQ2OSEQvF2= MoXCV2FPT0WU
BL-41 MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M135e2lEPTB;M{KuNVA2PCEQvF2= NVXaRYtOW0GQR1XS
NB6 NFe5U5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG0WJdKSzVyPUOyMlM5PTVizszN MWrTRW5ITVJ?
NCI-H1304 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGe5NGNKSzVyPUOyMlQ6PjdizszN MY\TRW5ITVJ?
MS-1 NInJN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjaTWM2OD1|Mj63O|UyKM7:TR?= NX;WeYhCW0GQR1XS
NOS-1 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDMd3RKSzVyPUO0MlY4PDhizszN NH\6bodUSU6JRWK=
EB2 M17CO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN4Lk[xPFkh|ryP M{HTNHNCVkeHUh?=
L-540 NG\KOJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zGU2lEPTB;M{euNlMxQCEQvF2= M1myNXNCVkeHUh?=
NCI-H747 M4jtcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HydWlEPTB;M{iuPFg1PiEQvF2= M33aTHNCVkeHUh?=
NCI-H446 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3wTWM2OD1|OT65OlUyKM7:TR?= NHi5T2FUSU6JRWK=
SJSA-1 M4LsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\qTWM2OD12NT61OFc1KM7:TR?= MmPhV2FPT0WU
BB65-RCC NHy2eFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXKU5BvUUN3ME20OU43PjZizszN M4H6enNCVkeHUh?=
SNB75 M{XTZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K0b2lEPTB;NE[uNFE5KM7:TR?= M1ntW3NCVkeHUh?=

... 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]


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 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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


CAS No. 231277-92-2
Storage powder
in solvent
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
    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

* 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID