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.

Size Price Stock Quantity  
In DMSO USD 191 In stock
USD 147 In stock
USD 400 In stock
Bulk Discount

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

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

Choose Selective HER2 Inhibitors

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 NH6zV2lRem:uaX\ldoF1cW:wIHHzd4F6 NFvC[HhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NIfyfHYyPjR6M{e3Ni=>
BT474 cell line M3y2SnBzd2yrZnXyZZRqd25iYYPzZZk> M3n2b2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS0O|Qh[2WubDDsbY5mNCCLQ{WwQVAvODJ3IN88US=> M4XPNlE3PDh|N{ey
HN5 cell NFXjRpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3j0NGlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? NV7UTZhZOTZ5N{e0NVA>
BT474 cell MknxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkH5TY5pcWKrdHnvckBw\iCEVES3OEBk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? NE\UV5EyPjd5N{SxNC=>
N87 cell M3vl[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrIPXBKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? Mo\oNVY4Pzd2MUC=
HFF cell NXjhTHZET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoXQTY5pcWKrdHnvckBw\iCKRl[gZ4VtdCCpcn;3eIgtKEmFNUC9PU46KM7:TR?= MYWxOlc4PzRzMB?=
SKBR3 cells M{PXVWN6fG:2b4jpZ4l1gSCjc4PhfS=> NHnWTlFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF5IN88US=> NEPkUHQyQTB{OESyOS=>
A431 cells M3zUdGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6xNFQh|ryP M{DDOFE6QDh6N{[x
SKBR3 cells NFXOZWtEgXSxdH;4bYNqfHliYYPzZZk> M4q2WGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOjlizszN MniyNVk5QDh5NkG=
HepG2 cells NWDTfFk3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGTrTopCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF03NjJ5IN88US=> M{f1b|IxOTR|N{e4
Hep3B2 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincEPCNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU41QSEQvF2= NEnFNGszODF2M{e3PC=>
SKHEP1 cells M3O3c3Bzd2yrZnXyZZRqd25iYYPzZZk> M2\1bWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjNizszN NFn6[|AzODF2M{e3PC=>
MCF7 cells NVG4N5NxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPU[uOkDPxE1? M2\zfVIxOTR|N{e4
MDA-MB-231 cells M{DO[3Bzd2yrZnXyZZRqd25iYYPzZZk> M3\1c2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkBpenNiYomgRXRRKGOxboTlcpQh[XO|YYmsJGlEPTB;NT60JO69VQ>? Mn20NlAyPDN5N{i=
SK-BR-3 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 M1LDSmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utRnIuOyClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:OC5yNDFOwG0> MYeyNFE1Ozd5OB?=
A431 cells M1fL[GZ2dmO2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKEWJRmKgbY51emGlZXzseYxieiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hSTR|MTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjB3MjFOwG0> MonUNlA{PDZ4NUW=
N87 cells M4rhVGZ2dmO2aX;uJIF{e2G7 NVf2d5hsUW6qaXLpeIlwdiCxZjDFdoJDOiCrboTyZYNmdGy3bHHyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOPFch[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6xJO69VQ>? Mo[5NlA{PDZ4NUW=
MIAPaCa cells MnPOSpVv[3Srb36gZZN{[Xl? NGLhTHZKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO MnTnNlA5OTd3MkO=
MIAPaCa cells Mor6SpVv[3Srb36gZZN{[Xl? M1f6XGlvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zNDFOwG0> M{L1SlIxQDF5NUKz
CAL27 cells MXTDfZRwfG:6aXPpeJkh[XO|YYm= NYj1e5JqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByNzFOwG0v MnLKNlExQDB4Mkm=
SKOV3 cells MXjDfZRwfG:6aXPpeJkh[XO|YYm= M3HkcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGhGWjJiYomgdoV{[Xq3cnnuJIR6\SC{ZXT1Z5Rqd25iYYPzZZktKEmFNUC9NE4xODNizszNMi=> NHzndFQzOTB6ME[yPS=>
CAL27 cells NGXDe2hHfW6ldHnvckBie3OjeR?= MnjXNVYhcA>? MYnJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? MVGyNVA5ODZ{OR?=
SK-BR-3 cells Mo\KVJJwdGmoZYLheIlwdiCjc4PhfS=> MnnrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDFdoJDOiCxdnXy[ZhxemW|c3nu[{BpfW2jbjDTT{1DWi1|IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCzNkDPxE1? M4S4V|IyPTdyOESz
BXF T24 cells NV\ifZVwS3m2b4TvfIlkcXS7IHHzd4F6 NInlfY41KGSjeYO= NH3xdXBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDYEZiVEK0JINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF06NjZ3IN88US=> M1TvRlIzOTZ7NkCx
CXF 269L cells MmLJR5l1d3SxeHnjbZR6KGG|c3H5 NU\BcnR2PCCmYYnz MkezR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR3hHKDJ4OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVgvOzZizszN NF;WcXgzOjF4OU[wNS=>
DIFI cells Mof2R5l1d3SxeHnjbZR6KGG|c3H5 MWC0JIRigXN? M{jlR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= NFjhXXUzOjF4OU[wNS=>
HT-29 cells NYqzemhIS3m2b4TvfIlkcXS7IHHzd4F6 NVzrcFFCPCCmYYnz MnP6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOlIh|ryP M2rZWlIzOTZ7NkCx
RKO cells MWDDfZRwfG:6aXPpeJkh[XO|YYm= M2jCXlQh\GG7cx?= M2LycWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJMVyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;NT6zOUDPxE1? MWiyNlE3QTZyMR?=
GXF251L cells NGS0VlJEgXSxdH;4bYNqfHliYYPzZZk> M1K2blQh\GG7cx?= MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDHXGYzPTGOIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2xMlQ5KM7:TR?= NGrZ[|QzOjF4OU[wNS=>
LIXF 575L cells MUHDfZRwfG:6aXPpeJkh[XO|YYm= MmjSOEBl[Xm| NWSzfolQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVEm[RjC1O|VNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD15LkG4JO69VQ>? NYPYVINuOjJzNkm2NFE>
LXFA 289L cells NXnTWWNuS3m2b4TvfIlkcXS7IHHzd4F6 MWm0JIRigXN? MlXWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHSSB{OEnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF02Njd7IN88US=> NFfmXm4zOjF4OU[wNS=>
LXFA 526L MUfDfZRwfG:6aXPpeJkh[XO|YYm= M4XHblQh\GG7cx?= NUPJdXA2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC1NlZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkKxJO69VQ>? MkDqNlIyPjl4MEG=
LXFA 629L cells NFrKTFJEgXSxdH;4bYNqfHliYYPzZZk> MlPYOEBl[Xm| M{PVfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiNkK5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Oi56NzFOwG0> NYfiVXhuOjJzNkm2NFE>
LXFL 1121L cells MoXuR5l1d3SxeHnjbZR6KGG|c3H5 MVS0JIRigXN? NH3wRmlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[OIEGxNlFNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD15LkezJO69VQ>? MYOyNlE3QTZyMR?=
LXFL 529L cells NV2yVGM{S3m2b4TvfIlkcXS7IHHzd4F6 NVr6SotVPCCmYYnz NVzWS2dWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDC1NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkWxJO69VQ>? M{jGbVIzOTZ7NkCx
MCF7 cells M2PqTWN6fG:2b4jpZ4l1gSCjc4PhfS=> NF7KXYQ1KGSjeYO= M2rYZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuPFMh|ryP MojMNlIyPjl4MEG=
MDA231 cells NFT6b2JEgXSxdH;4bYNqfHliYYPzZZk> MkXDOEBl[Xm| MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEzOzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUeuO{DPxE1? M{H4U|IzOTZ7NkCx
OVXF 899L MoLnR5l1d3SxeHnjbZR6KGG|c3H5 NWfoVlM2PCCmYYnz M1fRbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XYEZiOEm5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Oy5|NTFOwG0> NV:3eY5zOjJzNkm2NFE>
PAXF 546L cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= NWHKTY9mPCCmYYnz NWfXWYtPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEG[RjC1OFZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD14LkGyJO69VQ>? MWGyNlE3QTZyMR?=
PANC1 cells MVTDfZRwfG:6aXPpeJkh[XO|YYm= NX\zS4FqPCCmYYnz M1q5fWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME24MlEzKM7:TR?= M33kRVIzOTZ7NkCx
22Rv1 cell MYjDfZRwfG:6aXPpeJkh[XO|YYm= NFPndG01KGSjeYO= M3PWdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFIzWnZzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME22MlA3KM7:TR?= MkXPNlIyPjl4MEG=
DU145 cells M4\XO2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWWySFdvPCCmYYnz NE\kS2JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Nk46QSEQvF2= M{XCeVIzOTZ7NkCx
LNCAP cells MoHUR5l1d3SxeHnjbZR6KGG|c3H5 NXjyRoNkPCCmYYnz MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Mz62PEDPxE1? NFzQcYozOjF4OU[wNS=>
PC3M cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= MYm0JIRigXN? MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|NOKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkW1JO69VQ>? NGfiVGwzOjF4OU[wNS=>
NIH/3T3 cells M3nhSXBzd2yrZnXyZZRqd25iYYPzZZk> NV7KcZFWPzJiaB?= M2PKUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuN{DPxE1? MXSyNlU6PTF5Nx?=
NCI-H1648 cell M{n1PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFfGN3pKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEK1OFQh|ryP MWjTRW5ITVJ?
NMC-G1 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Ky[2lvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42PDVyMTFOwG0> MWrTRW5ITVJ?
NTERA-S-cl-D1 cell M1O4RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfXdWxnUW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPjV4MTFOwG0> M1iwTnNCVkeHUh?=
OCUB-M cell Mk\ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3:yTGlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTd2IN88US=> MoDvV2FPT0WU
OS-RC-2 cell NWTZNm5LT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWrsOVBMUW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57OUG5PUDPxE1? MUHTRW5ITVJ?
OVCAR-4 cell M3n0Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2HJUGlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO MULTRW5ITVJ?
RL95-2 cell NYDJbWw2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vDdmlvcGmkaYTpc44hd2ZiaIXtZY4hWkx7NT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yPTZ5IN88US=> NFqxcXpUSU6JRWK=
SW954 cell Mn:5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= MWPTRW5ITVJ?
SW962 cell MlTuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= NGXUb2RUSU6JRWK=
TE-1 cell NGXYeGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkCyNVU6KM7:TR?= M{m2U3NCVkeHUh?=
A253 cell MorzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;ITY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NEnaPItUSU6JRWK=
A388 cell NGfQfYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkOzTY5pcWKrdHnvckBw\iCqdX3hckBCOzh6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= MWTTRW5ITVJ?
BB30-HNC cell NFXr[XpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvEfXI3UW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP MYjTRW5ITVJ?
TE-12 cell NV2zO3BMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63NlI2QCEQvF2= MXPTRW5ITVJ?
TE-5 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M131WWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQ3PTRizszN MVPTRW5ITVJ?
TE-6 cell NWG0c|NoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4iyV2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFkxPTdizszN M2Do[nNCVkeHUh?=
TE-8 cell MofJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHRGNThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkCzO|Mh|ryP MnSwV2FPT0WU
TE-9 cell NGTkTIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjUR4RKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU2OjBzIN88US=> NWO3e3VqW0GQR1XS
TK10 cell MoP6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3nzXWlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN MVHTRW5ITVJ?
DSH1 cell MnfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3X0R2lvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN M4fJfHNCVkeHUh?=
ECC12 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGVESzF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVI{OSEQvF2= NIPoVFVUSU6JRWK=
EKVX cell NYPDb|RmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFmwXo5KdmirYnn0bY9vKG:oIHj1cYFvKEWNVmigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1QDd2IN88US=> M4PZTXNCVkeHUh?=
HCC2218 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoSyTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> NIT3bW9USU6JRWK=
LB2241-RCC cell NWfZRoVuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF3NECzJO69VQ>? MknUV2FPT0WU
LB996-RCC cell MlLxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGxDQTl4LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ{Mkig{txO MmPRV2FPT0WU
LC-1F cell NG\0bmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3nDTWlvcGmkaYTpc44hd2ZiaIXtZY4hVENvMV[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlM5OjR2IN88US=> M1rHOnNCVkeHUh?=
LS-513 cell NX\GPVlqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HlXWlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41ODB2MTFOwG0> NHfsb5NUSU6JRWK=

... 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

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
NCT02015169 Completed HER2-positive Gastric Cancer Patients With Liver Metastasis Samsung Medical Center July 9 2012 Phase 2
NCT00073528 Completed Neoplasms Breast Novartis Pharmaceuticals|Novartis December 9 2003 Phase 3
NCT03418558 Recruiting Metastatic Colorectal Cancer Fondazione del Piemonte per l''Oncologia July 8 2015 Phase 2
NCT01591577 Recruiting Newly Diagnosed Glioblastoma Multiforme Jonsson Comprehensive Cancer Center|GlaxoSmithKline December 7 2012 Phase 2
NCT00667251 Active not recruiting Breast Cancer Novartis Pharmaceuticals|NCIC Clinical Trials Group|Novartis October 7 2008 Phase 3
NCT00367471 Active not recruiting Neoplasms Breast Novartis Pharmaceuticals|Novartis December 7 2006 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 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.

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

Related HER2 Products

Tags: buy Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate supplier | purchase Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate cost | Lapatinib (GW-572016) Ditosylate manufacturer | order Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID