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.

Size Price Stock Quantity  
In DMSO USD 143 In stock
USD 110 In stock
USD 270 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 42 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 MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwMEK1OFQh|ryP M4jtU3NCVkeHUh?=
HCC2218 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHTW|RKSzVyPUCuNFU{OjZizszN M3O1[nNCVkeHUh?=
OCUB-M NEfVR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jaV2lEPTB;MD6wOVc1KM7:TR?= NHKyeXNUSU6JRWK=
ECC12 NWHv[I9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrsd252UUN3ME2wMlA6OjNzIN88US=> M4DDS3NCVkeHUh?=
DSH1 NUj5Zo1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwMEmzPVYh|ryP NVPLOY1pW0GQR1XS
BT-474 M1LZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nJfmlEPTB;MD6yNVMyPSEQvF2= MmnhV2FPT0WU
BB30-HNC M3qyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoixTWM2OD1yLkK0OlU1KM7:TR?= MYfTRW5ITVJ?
EKVX NX7RXW5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe5[VFKSzVyPUCuOFQ5PzRizszN NU[0Z|U{W0GQR1XS
TE-12 NIfuWZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLDTWM2OD1yLkS5NFU4KM7:TR?= MmXEV2FPT0WU
A388 NFvx[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjzUVJKSzVyPUCuO|IzPThizszN M4n5TnNCVkeHUh?=
TE-9 NXvEW5FjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37ocWlEPTB;MD63OFQ2OyEQvF2= M{OySnNCVkeHUh?=
LB2241-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwMUW0NFMh|ryP MoPZV2FPT0WU
LB996-RCC NYLaeok3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTFwM{[yNlgh|ryP MXvTRW5ITVJ?
LC-1F Mk\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHDWIxIUUN3ME2xMlM5OjR2IN88US=> M{TNOHNCVkeHUh?=
TE-6 NFfmTnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon5TWM2OD1zLkW1NlAyKM7:TR?= NE\TOmpUSU6JRWK=
A253 M1jYTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFwOUezN|Uh|ryP NF\nSlZUSU6JRWK=
OS-RC-2 NHSwR|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4TWM2OD1zLkm5NVk6KM7:TR?= M3z0NnNCVkeHUh?=
TE-1 M4rBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTJwMES4N{DPxE1? MV3TRW5ITVJ?
RL95-2 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNwMUW2O{DPxE1? NFPOVVlUSU6JRWK=
LS-513 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNwNECwOFEh|ryP M2rSfHNCVkeHUh?=
DJM-1 M1H5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu4em9rUUN3ME2zMlQ3QTd3IN88US=> MoPTV2FPT0WU
NMC-G1 NW\ITlRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTNwNUS1NFEh|ryP M2DKb3NCVkeHUh?=
TE-10 NHzpOoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7sTWM2OD1|LkW1N|U3KM7:TR?= NVzIXFhrW0GQR1XS
TE-5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXflU2FrUUN3ME20MlA{PzNizszN MmflV2FPT0WU
TK10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzzTWM2OD12LkG2OVIzKM7:TR?= NEKzRXBUSU6JRWK=
UACC-812 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH5UYZKSzVyPUSuOVYyPTNizszN NG\XPZlUSU6JRWK=
SW962 M13vVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjafYRKSzVyPUWuNFIyPTlizszN NI[zR4xUSU6JRWK=
SW954 NXXaOVZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTVwM{myOFUh|ryP MVTTRW5ITVJ?
COLO-668 NXnkdoR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrFbnBpUUN3ME21MlczPjZ5IN88US=> NEe4OoFUSU6JRWK=
LB1047-RCC NWnTOXVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3QTWM2OD13LkiwNFQ3KM7:TR?= NGjmfGJUSU6JRWK=
NB5 NYDaWmRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPj[W1KSzVyPU[uNlExODFizszN NGC0c2pUSU6JRWK=
NTERA-S-cl-D1 M2\l[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTZwMk[1OlEh|ryP NHjSW4dUSU6JRWK=
IST-MEL1 NGLPfZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTZwNEO2PVQh|ryP NW\aT5RoW0GQR1XS
GI-1 NETSZW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HadGlEPTB;Nj61NVY5OiEQvF2= M{LC[HNCVkeHUh?=
TGBC1TKB NI[wR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;2Z2lEPTB;Nz6wO|E5OyEQvF2= NXHUdZNzW0GQR1XS
GT3TKB NWPvOJpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fjTWlEPTB;Nz6yNlc1PCEQvF2= NInEbmdUSU6JRWK=
EVSA-T MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrvXXdKSzVyPUeuOFI5OTFizszN NH74WIJUSU6JRWK=
D-502MG MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW1TFhwUUN3ME23MlQ5QDl2IN88US=> MXHTRW5ITVJ?
TE-8 NY\ZZ3hpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTDSppjUUN3ME23Mlc3OTV7IN88US=> Mo\DV2FPT0WU
OVCAR-4 NFPsVYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXncJFKSzVyPUmuNVE3PzVizszN MWHTRW5ITVJ?
D-336MG Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW3TWM2OD17LkS3N|k2KM7:TR?= NIrVNJNUSU6JRWK=
GCIY MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\TZmhKSzVyPUmuOVc1OiEQvF2= MnTCV2FPT0WU
KS-1 M{m5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTlwNk[yPFch|ryP MWPTRW5ITVJ?
HCC2998 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvSTWM2OD17Lkm2N|A4KM7:TR?= MWjTRW5ITVJ?
D-247MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3LPZhKSzVyPUmuPVgzQTFizszN NFPX[ZVUSU6JRWK=
TE-15 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DpdWlEPTB;MUCuNlQ2KM7:TR?= NF7pUYNUSU6JRWK=
IST-MES1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\hVFZKSzVyPUGwMlI2PjVizszN NH3MW|JUSU6JRWK=
ETK-1 NEfyT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ae2lEPTB;MUCuOlI{KM7:TR?= NFLURopUSU6JRWK=
RCC10RGB NIfqOGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFyLkm2NUDPxE1? MVzTRW5ITVJ?
KNS-42 MoPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7QTmVKSzVyPUGxMlczPTVizszN NEXYN4tUSU6JRWK=
LB771-HNC MoDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITKeY5KSzVyPUGyMlE4OTJizszN NIH5dINUSU6JRWK=
SR MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\4N|FKSzVyPUGyMlIxPjRizszN NWXTcVRjW0GQR1XS
NCI-H1355 NHHVUXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF{Lki5PFUh|ryP M{O1PXNCVkeHUh?=
ES6 NFrYT|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PyeWlEPTB;MUOuNFc5KM7:TR?= M2j6UXNCVkeHUh?=
SK-NEP-1 NXL6R3I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\WV2lEPTB;MUOuNlU4PyEQvF2= MWLTRW5ITVJ?
D-392MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHCXXdKSzVyPUGzMlY1OjhizszN MXzTRW5ITVJ?
NB7 NFjL[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHET2hKSzVyPUG0MlI{PzRizszN M2iySnNCVkeHUh?=
SK-LMS-1 M1XkUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF2LkWxOFUh|ryP NGr2U|JUSU6JRWK=
SK-UT-1 M13JVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrSTWM2OD1zND63PFg6KM7:TR?= NEPUWYpUSU6JRWK=
CA46 MoThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF3LkC1PFYh|ryP NGL2OWdUSU6JRWK=
IST-SL2 NYHE[ol4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF3LkG5NFEh|ryP NEPsO21USU6JRWK=
BC-1 NHrGVJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln3TWM2OD1zNT6zN|E1KM7:TR?= NIP5VnFUSU6JRWK=
LS-123 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPMTWM2OD1zNT64NVc{KM7:TR?= NHrvZnNUSU6JRWK=
Ramos-2G6-4C10 MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDDeIhyUUN3ME2xOk4xQTJ2IN88US=> M1H3WnNCVkeHUh?=
MZ1-PC NILpWGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D4OWlEPTB;MU[uO|MyOyEQvF2= NHL2OWdUSU6JRWK=
LB647-SCLC NHPQT3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfvN3BKSzVyPUG2Mlk{PzJizszN M4HjbHNCVkeHUh?=
NCI-H1694 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PuNmlEPTB;MUeuNVUzQSEQvF2= NH;qdmNUSU6JRWK=
NCI-H322M MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF5LkSzOlYh|ryP NILsNJVUSU6JRWK=
ES7 NWjT[FlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvCV3JKSzVyPUG4MlM6OTRizszN NEfnT3dUSU6JRWK=
LC-2-ad M4\kV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF6LkSzPFYh|ryP NH76NJJUSU6JRWK=
SF268 M2LDfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjs[GRmUUN3ME2xPE44PDB7IN88US=> M2\HSnNCVkeHUh?=
RPMI-8402 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK3WoRSUUN3ME2xPU4xPzR{IN88US=> NXfIbHUxW0GQR1XS
HCE-T MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XSW2lEPTB;MkCuNlM1PCEQvF2= Mn\aV2FPT0WU
A101D MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXwWpNRUUN3ME2yNE45PTh5IN88US=> MlfTV2FPT0WU
MRK-nu-1 NEDMc4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJyLkmxN{DPxE1? M{DMbXNCVkeHUh?=
LXF-289 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHDTWM2OD1{MT6wN|gh|ryP MVTTRW5ITVJ?
NALM-6 MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJzLkG5Olch|ryP NID6PYlUSU6JRWK=
DOHH-2 NFzTdlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHnRlRKSzVyPUKxMlQ5OTNizszN MmnqV2FPT0WU
EW-16 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PVOWlEPTB;MkKuNVQxOiEQvF2= NFvY[XdUSU6JRWK=
A4-Fuk NHzJTZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHIXWJKSzVyPUKyMlIyPDlizszN MlXGV2FPT0WU
HD-MY-Z M3[x[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6yTWM2OD1{Mj6zPVY2KM7:TR?= NFP2PVFUSU6JRWK=
SKM-1 M321VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfsTWM2OD1{Mj63N|UyKM7:TR?= NWDSVW1IW0GQR1XS
DMS-153 M2GzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfoSINZUUN3ME2yN{41OjB2IN88US=> NF3rTmRUSU6JRWK=
LB373-MEL-D MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj0dFJKSzVyPUKzMlU1PTJizszN MYnTRW5ITVJ?
LP-1 NHrJVolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfu[3lKSzVyPUKzMlgxQTdizszN NXfTc5Y{W0GQR1XS
GI-ME-N M3;1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjlfWFKSzVyPUK0MlI6OiEQvF2= M163eXNCVkeHUh?=
MPP-89 NX\rOZJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfzTWM2OD1{NT6yNFM3KM7:TR?= NYXo[JVuW0GQR1XS
U-698-M NF;KOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJ3LkK1NFMh|ryP NVm0THNoW0GQR1XS
HC-1 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJ3Lk[0NVgh|ryP NHfifIZUSU6JRWK=
HCC2157 M321cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ3Lk[3N{DPxE1? Ml;oV2FPT0WU
MOLT-4 M1zubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DSd2lEPTB;Mk[uNlc{KM7:TR?= NXjZ[JMzW0GQR1XS
LS-411N MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP6TWM2OD1{Nj6zN|Y6KM7:TR?= NHi3SphUSU6JRWK=
Becker MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi5XmRGUUN3ME2yOk42OThzIN88US=> MYTTRW5ITVJ?
NCI-H23 Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ4Lke1O|Uh|ryP MULTRW5ITVJ?
IST-SL1 NHToXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzrR2xKSzVyPUK3MlM5PjdizszN NEPafm1USU6JRWK=
MZ2-MEL M13QOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjTPHJKSzVyPUK3MlQ2PjZizszN MnXZV2FPT0WU
RKO NYmw[3o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPYTZdWUUN3ME2yPE4yPDR4IN88US=> NUTySXFwW0GQR1XS
TE-441-T MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvCTWM2OD1{OD63PFkh|ryP NXLUNIdjW0GQR1XS
EW-24 M2nXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv0R5BKSzVyPUK5MlEzPTlizszN M{[5cHNCVkeHUh?=
no-10 M1frZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH0TWM2OD1{OT6xOlMyKM7:TR?= MlnjV2FPT0WU
D-542MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJ7LkmyNlEh|ryP NY\OdndXW0GQR1XS
ST486 M3rGdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHEPGZKSzVyPUOwMlY1PTFizszN NEfRXJVUSU6JRWK=
KURAMOCHI MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfB[Y1KSzVyPUOwMlgxPTdizszN M4fiTHNCVkeHUh?=
ES8 NXLHXVFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:zTWM2OD1|MT61PVczKM7:TR?= NYewZZVXW0GQR1XS
BL-41 M4j5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\wTWM2OD1|Mj6xNFU1KM7:TR?= M2flbHNCVkeHUh?=
NB6 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\5TWM2OD1|Mj6zPFU2KM7:TR?= MY\TRW5ITVJ?
NCI-H1304 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVixcmJjUUN3ME2zNk41QTZ5IN88US=> NGPNT2VUSU6JRWK=
MS-1 MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDSTWM2OD1|Mj63O|UyKM7:TR?= Ml3FV2FPT0WU
MFH-ino MoPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3mSFdKSzVyPUO0MlMzOjRizszN NWLSS3BkW0GQR1XS
NOS-1 NGTueXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN2Lk[3OFgh|ryP MWHTRW5ITVJ?
HUTU-80 NXnkXoVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUP5SnA6UUN3ME2zOU4{PjZ5IN88US=> NF7pbG9USU6JRWK=
EB2 M1LUT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHkOVhKSzVyPUO2MlYyQDlizszN NYfRe4N6W0GQR1XS
L-540 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPMUIVKSzVyPUO3MlI{ODhizszN NYmyeXFnW0GQR1XS
NCI-H747 MnzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTN6Lki4OFYh|ryP M{nHbXNCVkeHUh?=
NCI-H446 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULyNHFCUUN3ME2zPU46PjVzIN88US=> MnPlV2FPT0WU
MOLT-16 Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3WcZJVUUN3ME20Nk41OTVizszN NWrie3lzW0GQR1XS
BC-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO5VHVKSzVyPUS1MlQ5QTZizszN NHfTN4hUSU6JRWK=
SJSA-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXyNmZKSzVyPUS1MlU1PzRizszN M{e2O3NCVkeHUh?=
BB65-RCC NFrnS4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TPfmlEPTB;NEWuOlY3KM7:TR?= MUfTRW5ITVJ?
SNB75 NHnhNYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTR4LkCxPEDPxE1? MVPTRW5ITVJ?

... 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(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

* 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
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
    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
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2

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.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

Related EGFR Products4

Tags: buy Lapatinib | Lapatinib supplier | purchase Lapatinib | Lapatinib cost | Lapatinib manufacturer | order Lapatinib | Lapatinib distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID