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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In DMSO USD 191 In stock
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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 M1rqeXBzd2yrZnXyZZRqd25iYYPzZZk> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxtKGyrbnWsJGlEPTB;MD6wNlUh|ryP NUfic3JTOTZ2OEO3O|I>
BT474 cell line MmjRVJJwdGmoZYLheIlwdiCjc4PhfS=> MkPhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN MoLjNVY1QDN5N{K=
HN5 cell NYXFUG16T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmT2TY5pcWKrdHnvckBw\iCKTkWgZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKg{txO NWjoSJlrOTZ5N{e0NVA>
BT474 cell NWXITVMzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\jR25NUW6qaXLpeIlwdiCxZjDCWFQ4PCClZXzsJIdzd3e2aDDh[pRmeiB5MjDodpMtKEmFNUC9NE4xQCEQvF2= M33yO|E3Pzd5NEGw
N87 cell MlTQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\6UYxKdmirYnn0bY9vKG:oIF64O{Bk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? MkLaNVY4Pzd2MUC=
HFF cell M3XaXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUT0RZFFUW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> M1fPVVE3Pzd5NEGw
SKBR3 cells NUP0XGF[S3m2b4TvfIlkcXS7IHHzd4F6 MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFE4KM7:TR?= NFnrd44yQTB{OESyOS=>
A431 cells NFj6SYVEgXSxdH;4bYNqfHliYYPzZZk> NWPlWI0{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR|MTDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTB2IN88US=> MlLVNVk5QDh5NkG=
SKBR3 cells M3rObmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnXjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAzQSEQvF2= MV6xPVg5QDd4MR?=
HepG2 cells Mln1VJJwdGmoZYLheIlwdiCjc4PhfS=> MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME22MlI4KM7:TR?= NXewRlB2OjBzNEO3O|g>
Hep3B2 cells NYLkWHRRWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXLv[mFHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SjJiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNEmg{txO NF7P[2MzODF2M{e3PC=>
SKHEP1 cells Ml7SVJJwdGmoZYLheIlwdiCjc4PhfS=> M2DPOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjNizszN NVjNSFJEOjBzNEO3O|g>
MCF7 cells MkfjVJJwdGmoZYLheIlwdiCjc4PhfS=> M1XXN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok43KM7:TR?= Mm\ONlAyPDN5N{i=
MDA-MB-231 cells NUfuWWZlWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIXqbWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPUWuOEDPxE1? MV:yNFE1Ozd5OB?=
SK-BR-3 cells M16wSXBzd2yrZnXyZZRqd25iYYPzZZk> MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVAvODRizszN M3jUdVIxOTR|N{e4
A431 cells NYDYeHlFTnWwY4Tpc44h[XO|YYm= M3XlTmlvcGmkaYTpc44hd2ZiRVfGVkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDNEOxJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMEWyJO69VQ>? NET6cWMzODN2Nk[1OS=>
N87 cells Mk\aSpVv[3Srb36gZZN{[Xl? NWO1TWdiUW6qaXLpeIlwdiCxZjDFdoJDOiCrboTyZYNmdGy3bHHyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOPFch[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6xJO69VQ>? MkjKNlA{PDZ4NUW=
MIAPaCa cells Mme1SpVv[3Srb36gZZN{[Xl? NFzEeGlKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO NIjRVpMzODhzN{WyNy=>
MIAPaCa cells MVvGeY5kfGmxbjDhd5NigQ>? MmjOTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> Ml3tNlA5OTd3MkO=
CAL27 cells NI\0d5VEgXSxdH;4bYNqfHliYYPzZZk> MnS0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2FNOjdiY3XscJMhd3[ncnX4dJJme3OrbnegSWdHWiCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2wMlAxPyEQvF2u MYKyNVA5ODZ{OR?=
SKOV3 cells M2nT[WN6fG:2b4jpZ4l1gSCjc4PhfS=> M1T2XWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGhGWjJiYomgdoV{[Xq3cnnuJIR6\SC{ZXT1Z5Rqd25iYYPzZZktKEmFNUC9NE4xODNizszNMi=> M1Tn[lIyODhyNkK5
CAL27 cells MnjQSpVv[3Srb36gZZN{[Xl? MlH6NVYhcA>? M3vaR2lvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0MEBKSzVyPUCuNFMzKM7:TR?= M3z5b|IyODhyNkK5
SK-BR-3 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXyZmIzKG:4ZYLlfJBz\XO|aX7nJIh2dWGwIGPLMWJTNTNiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEOyJO69VQ>? NFLpWWszOTV5MEi0Ny=>
BXF T24 cells NWiw[XpqS3m2b4TvfIlkcXS7IHHzd4F6 MXG0JIRigXN? MnTTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnhHKFR{NDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PU43PSEQvF2= NHv5enUzOjF4OU[wNS=>
CXF 269L cells NYL5fnZmS3m2b4TvfIlkcXS7IHHzd4F6 NHHoWnc1KGSjeYO= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDXGYhOjZ7TDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4{PiEQvF2= NX7l[Jc5OjJzNkm2NFE>
DIFI cells NG\CR4dEgXSxdH;4bYNqfHliYYPzZZk> NWjVVHM2PCCmYYnz NVjldWM4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTEmISTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9NE4zOzVizszN MmPZNlIyPjl4MEG=
HT-29 cells NYDjXlRRS3m2b4TvfIlkcXS7IHHzd4F6 MnzZOEBl[Xm| MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND62NkDPxE1? MoHPNlIyPjl4MEG=
RKO cells MnfGR5l1d3SxeHnjbZR6KGG|c3H5 M2nC[FQh\GG7cx?= MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDST28h[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwM{Wg{txO NGDKSZAzOjF4OU[wNS=>
GXF251L cells MlXpR5l1d3SxeHnjbZR6KGG|c3H5 NIDuVXg1KGSjeYO= M1O5V2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN NFrnZm4zOjF4OU[wNS=>
LIXF 575L cells MofBR5l1d3SxeHnjbZR6KGG|c3H5 M3HYTVQh\GG7cx?= M3;yZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxKYEZiNUe1UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Py5zODFOwG0> M2ixeFIzOTZ7NkCx
LXFA 289L cells NUL3S|RzS3m2b4TvfIlkcXS7IHHzd4F6 Mm\5OEBl[Xm| M1fPb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiMki5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:PS55OTFOwG0> MUGyNlE3QTZyMR?=
LXFA 526L NYLDVIM2S3m2b4TvfIlkcXS7IHHzd4F6 MWC0JIRigXN? M1fid2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiNUK2UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:PC5{MTFOwG0> MmnaNlIyPjl4MEG=
LXFA 629L cells MUPDfZRwfG:6aXPpeJkh[XO|YYm= NEHwcIc1KGSjeYO= NU\sfJFJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC2NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1{Lki3JO69VQ>? NVPkPI83OjJzNkm2NFE>
LXFL 1121L cells NIrYZnJEgXSxdH;4bYNqfHliYYPzZZk> NWLyZ5liPCCmYYnz M4rvSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkxiMUGyNWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwN{Og{txO MViyNlE3QTZyMR?=
LXFL 529L cells NIXKdYJEgXSxdH;4bYNqfHliYYPzZZk> NYPaVoZ5PCCmYYnz NXrnVm1DS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDC1NllNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkWxJO69VQ>? NFnaOmEzOjF4OU[wNS=>
MCF7 cells M1HV[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MnHHOEBl[Xm| NU\PRYMzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9OE45OyEQvF2= MnHzNlIyPjl4MEG=
MDA231 cells NWD0TnduS3m2b4TvfIlkcXS7IHHzd4F6 NUHyUlFFPCCmYYnz MmfhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCOjNzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME23Mlch|ryP Mn\KNlIyPjl4MEG=
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... 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:
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
Synonyms N/A

Bio Calculators

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    If I 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