Lapatinib (GW-572016) Ditosylate

Catalog No.S1028

Lapatinib (GW-572016) Ditosylate Chemical Structure

Molecular Weight(MW): 925.46

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.

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Cited by 52 Publications

7 Customer Reviews

  • Combination of NVP-AEW541 and lapatinib cooperatively inhibits the growth of NVP-AEW541 resistant murine rhabdomyosarcoma primary cell cultures with Igf1r/Her2 complexes. Cell viability assay for Naïve, untreated (U20325; A) and NVP-AEW541 innately resistant mouse rhabdomyosarcoma primary culture (U44676; B) treated with varying concentrations of NVP-AEW541, lapatinib, or a combination of both. Naïve cells (U20325) were sensitive to NVP-AEW541, but lapatinib had no cooperativity. In contrast, NVP-AEW541 at moderate doses increased cell growth in resistant cell cultures (U44676). However, this paradoxical effect was reduced by the addition of lapatinib, although lapatinib treatment alone had very little effect. C, the NVP-AEW541 resistant primary tumor cell line (U44676) was treated with DMSO, 5 μmol/L lapatinib, 5 μmol/L NVP-AEW541, and a combination of 5 μmol/L NVP-AEW541+lapatinib for 25 minutes and Western blot analysis was done on lysates for p-Igf1r and p-Her2.

    Mol Cancer Ther 2011 10:697-707. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

    (B-C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.

    Carcinogenesis 2010 31, 1948–1955 . Lapatinib (GW-572016) Ditosylate purchased from Selleck.

  • LNCaP-AI cells were starved in 1% stripped medium for 24 h. The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) for 24 h. Cell culture medium was collected from each sample and subjected to ELISA for sPLA2-IIa. The condition medium samples were diluted 10 times for ELISA. Average of duplicate samples was converted to nanogram per milliliter against standard curve. The data represent one of five repeated experiments.

     

     

    Carcinogenesis 2010 31, 1948–1955. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

    Impact of the TKI erlotinib, lapatinib, dasatinib, and sorafenib on the viability of MDS/AML cells. MOLM-13 (A) and HL-60 (B) cells were incubated with the indicated doses (given in mM below the x-axis) of the 4 TKI, and cellular viability was assessed by MTT assay after 24, 48 and 72 h of incubation. Changes in viability are given as percentage of cells as compared to non-treated control samples. This experiment was repeated at least three times, yielding comparable results. Graphs show representative results of one experiment carried out in duplicates (mean   standard deviation).

     

     

    Biochem Pharmacol 2011 82, 1457-1466. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

  • Capacity of the TKI to overcome the AML-typical differentiation blockage. The myeloid cell lines MOLM-13 and HL-60 were incubated for 6 days with 0.01% DMSO (serving as a negative solvent control), 1 μM of ATRA (serving as a positive control), as well as with the indicated doses of the four TKI. (A) Representative May-Gruenwald-Giemsa staining of MOLM-13 cells, (B) quantitation of the percentage of MOLM-13 cells exhibiting at least two morphological signs of differentiation (that is a decrease in cytoplasmic basophilia, a reduction of the nucleo-cytoplasmic ratio, appearance of nuclear lobulation and/or cytoplasmic granules). Percentages were evaluated by examining at least 100 cells/condition; (C) representative FACS overlays of MOLM-13 cells depicting TKI-induced CD11b expression (black line) as compared to the isotype (shaded grey); (D) quantitation of TKI-induced CD11b-expression in MOLM-13 cells; (E) representative slides depicting morphology/staining of MOLM-13 cells assessed in the NBT-reduction assay; (F) respective quantitative assessment demonstrating the NBT-reducing capacity under the different drugs; (G) representative May-Gruenwald-Giemsa staining of HL-60 cells.

     

     

    Biochem Pharmacol 2011 82, 1457-1466. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

    Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.

    Int J Proteomics 2011 2011, 215496. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

  • After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of Lapatinib for 3h,followed by 20-minute  stimolation of 100ng/ml EGF.

     

     

    Dr. Zhang of Tianjin Medical University. Lapatinib (GW-572016) Ditosylate purchased from Selleck.

Purity & Quality Control

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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 NV3sd2tzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4XFeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= MYmxOlQ5Ozd5Mh?=
BT474 cell line NUXrTGhMWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIL0TXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> NEnLNJgyPjR6M{e3Ni=>
HN5 cell NFvoZZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1HOfmlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? MXexOlc4PzRzMB?=
BT474 cell NITFfW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnlWopKdmirYnn0bY9vKG:oIFLUOFc1KGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{whUUN3ME2wMlA5KM7:TR?= Mkf6NVY4Pzd2MUC=
N87 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TWbWlvcGmkaYTpc44hd2ZiTki3JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkC4JO69VQ>? Mon4NVY4Pzd2MUC=
HFF cell NGDBelBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTtOJdjUW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> MWKxOlc4PzRzMB?=
SKBR3 cells Mni3R5l1d3SxeHnjbZR6KGG|c3H5 M16zZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOTdizszN M{\WV|E6ODJ6NEK1
A431 cells M{i0R2N6fG:2b4jpZ4l1gSCjc4PhfS=> NGPI[pNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4yODRizszN NITNVWQyQTh6OEe2NS=>
SKBR3 cells NInTNHdEgXSxdH;4bYNqfHliYYPzZZk> NYLofGZ4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB{OTFOwG0> NHTDOY4yQTh6OEe2NS=>
HepG2 cells NUnMdGVOWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml6wRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= MkPtNlAyPDN5N{i=
Hep3B2 cells MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 NIi0dWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52OTFOwG0> MXyyNFE1Ozd5OB?=
SKHEP1 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONSFXQNUBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU4{KM7:TR?= MX2yNFE1Ozd5OB?=
MCF7 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 M2XZXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok43KM7:TR?= NGHvNVYzODF2M{e3PC=>
MDA-MB-231 cells NEHXdGZRem:uaX\ldoF1cW:wIHHzd4F6 NWL0OWdSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME21MlQh|ryP NWfVU3BlOjBzNEO3O|g>
SK-BR-3 cells M2nDb3Bzd2yrZnXyZZRqd25iYYPzZZk> NXTRVHB1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{KGGodHXyJIhzeyCkeTDBWHAh[2:wdHXueEBie3OjeTygTWM2OD1yLkC0JO69VQ>? NUC5e|A3OjBzNEO3O|g>
A431 cells MX;GeY5kfGmxbjDhd5NigQ>? NGH2O2dKdmirYnn0bY9vKG:oIFXHSnIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQUSzNUBk\WyuczDifUBGVEmVQTygTWM2OD1yLkC1NkDPxE1? MX6yNFM1PjZ3NR?=
N87 cells NEPOdGxHfW6ldHnvckBie3OjeR?= M4TjW2lvcGmkaYTpc44hd2ZiRYLiRlIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTki3JINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMTFOwG0> NF34cZgzODN2Nk[1OS=>
MIAPaCa cells NFW3WmRHfW6ldHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3JRXBiS2FiY3XscJMh[nliRVzJV2EtKEmFNUC9NE41OzNizszN NVjjXFZROjB6MUe1NlM>
MIAPaCa cells NUL3dm5FTnWwY4Tpc44h[XO|YYm= MkLmTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> NVzjbog2OjB6MUe1NlM>
CAL27 cells MkPPR5l1d3SxeHnjbZR6KGG|c3H5 NGXW[3lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB5IN88UU4> MmnzNlExQDB4Mkm=
SKOV3 cells M17lcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDISXIzKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA{KM7:TT6= MV[yNVA5ODZ{OR?=
CAL27 cells M{\tfWZ2dmO2aX;uJIF{e2G7 MmXMNVYhcA>? MWLJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? MmWyNlExQDB4Mkm=
SK-BR-3 cells Mmq4VJJwdGmoZYLheIlwdiCjc4PhfS=> MmPtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFdoJDOiCxdnXy[ZhxemW|c3nu[{BpfW2jbjDTT{1DWi1|IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCzNkDPxE1? M4fYTVIyPTdyOESz
BXF T24 cells MlTkR5l1d3SxeHnjbZR6KGG|c3H5 M2Lj[VQh\GG7cx?= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCXGYhXDJ2IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME25MlY2KM7:TR?= MmfyNlIyPjl4MEG=
CXF 269L cells NFG5dGdEgXSxdH;4bYNqfHliYYPzZZk> MVy0JIRigXN? MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDXGYhOjZ7TDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4{PiEQvF2= M2nGe|IzOTZ7NkCx
DIFI cells NE\5TIpEgXSxdH;4bYNqfHliYYPzZZk> MXq0JIRigXN? MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDETWZKKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1yLkKzOUDPxE1? NGq0V5QzOjF4OU[wNS=>
HT-29 cells MoXYR5l1d3SxeHnjbZR6KGG|c3H5 Ml;UOEBl[Xm| M3PJdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20MlYzKM7:TR?= M3jiR|IzOTZ7NkCx
RKO cells NHXWSmFEgXSxdH;4bYNqfHliYYPzZZk> NWLOVnZLPCCmYYnz NXTWSIhCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWkuRIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME21MlM2KM7:TR?= MlTKNlIyPjl4MEG=
GXF251L cells NE\OUJNEgXSxdH;4bYNqfHliYYPzZZk> M3jCOlQh\GG7cx?= M1LSNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN MkLMNlIyPjl4MEG=
LIXF 575L cells MmDNR5l1d3SxeHnjbZR6KGG|c3H5 NUnzOlZnPCCmYYnz MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMTXhHKDV5NVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvOThizszN MoHjNlIyPjl4MEG=
LXFA 289L cells M1jWfWN6fG:2b4jpZ4l1gSCjc4PhfS=> MWS0JIRigXN? MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZCKDJ6OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVUvPzlizszN MWmyNlE3QTZyMR?=
LXFA 526L NH36fWREgXSxdH;4bYNqfHliYYPzZZk> MWW0JIRigXN? NFvyWnVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEWyOmwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTRwMkGg{txO Ml7VNlIyPjl4MEG=
LXFA 629L cells NHnoXFJEgXSxdH;4bYNqfHliYYPzZZk> MXu0JIRigXN? NXzVfmo4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC2NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1{Lki3JO69VQ>? NWWwWIwxOjJzNkm2NFE>
LXFL 1121L cells MnjFR5l1d3SxeHnjbZR6KGG|c3H5 MVe0JIRigXN? NWPJSpZXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDCxNVIyVCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nz63N{DPxE1? Ml7uNlIyPjl4MEG=
LXFL 529L cells M4LzcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M{PqVFQh\GG7cx?= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZNKDV{OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPTFizszN M1PLflIzOTZ7NkCx
MCF7 cells NWLxXYpUS3m2b4TvfIlkcXS7IHHzd4F6 MYK0JIRigXN? NYO2Sm03S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE45OyEQvF2= NF6zdpYzOjF4OU[wNS=>
MDA231 cells M4LvV2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWCzTpR1PCCmYYnz NFWxPFREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF{M{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvPyEQvF2= NUDoS|NPOjJzNkm2NFE>
OVXF 899L MnjHR5l1d3SxeHnjbZR6KGG|c3H5 NWG1dFZPPCCmYYnz NGnpS4dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXliIIEi5PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTNwM{Wg{txO NX\FPG53OjJzNkm2NFE>
PAXF 546L cells MYDDfZRwfG:6aXPpeJkh[XO|YYm= MV60JIRigXN? M{G3VmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCYEZiNUS2UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi5zMjFOwG0> NX\FclE5OjJzNkm2NFE>
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OVCAR-4 cell Ml;PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2jtbWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO NHrtO|dUSU6JRWK=
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TE-1 cell NYfMT5EzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnzMTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6wNlE2QSEQvF2= NVziUmdqW0GQR1XS
A253 cell M1TTcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYC0dGdiUW6qaXLpeIlwdiCxZjDoeY1idiCDMkWzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPDh|IN88US=> MXzTRW5ITVJ?
A388 cell NVToVnNkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTFVXpKdmirYnn0bY9vKG:oIHj1cYFvKEF|OEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA1QDNizszN NWC3bmJEW0GQR1XS
BB30-HNC cell MkPhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYjJU|J6UW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP NEfEe|dUSU6JRWK=
TE-12 cell MmnBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYXmWI9TUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ{NUig{txO MWjTRW5ITVJ?
TE-5 cell M13hbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnYZmpPUW6qaXLpeIlwdiCxZjDoeY1idiCWRT21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDZ3NDFOwG0> M2jlSXNCVkeHUh?=
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TE-8 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHrXO3BKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{PzNizszN M1LrUHNCVkeHUh?=
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TK10 cell NG\xe4JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXrJcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2OVIzKM7:TR?= M3nuN3NCVkeHUh?=
DSH1 cell NX;neXc6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmHGTY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVM6PiEQvF2= M1PUNHNCVkeHUh?=
ECC12 cell M{nvNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\yTY5pcWKrdHnvckBw\iCqdX3hckBGS0NzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFkzOzFizszN NHvUcJhUSU6JRWK=
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HCC2218 cell NXz3R4FpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlnPTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> NGjnTo1USU6JRWK=
LB2241-RCC cell NFHnSXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF3NECzJO69VQ>? MUTTRW5ITVJ?
LB996-RCC cell NWGzNGRXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGxDQTl4LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ{Mkig{txO NFTkUGFUSU6JRWK=
LC-1F cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJGxENTGIIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zPFI1PCEQvF2= MkjLV2FPT0WU
LS-513 cell Mn3OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETQXHFKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDByNEGg{txO MVrTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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]
+ 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
  • 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 (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+30% PEG 300+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 925.46
Formula

C29H26ClFN4O4S.2C7H8O3S

CAS No. 388082-77-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*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).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT03080805 Recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co. Ltd. May 3 2017 Phase 3
NCT03084939 Recruiting Breast Cancer Hoffmann-La Roche April 24 2017 Phase 3
NCT03085368 Recruiting HER2-positive Breast Cancer Peking Union Medical College Hospital|EddingPharm Oncology Co. LTD. March 1 2017 Phase 2|Phase 3
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|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 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