Lapatinib (GW-572016) Ditosylate

製品コードS1028

Lapatinib (GW-572016) Ditosylate化学構造

分子量(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.

サイズ 価格(税別)  
JPY 31722.00
JPY 24402.00
JPY 66400.00

文献中Selleckの製品使用例(54)

カスタマーフィードバック(7)

  • 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.

製品安全説明書

HER2阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HN5 cell line MUPQdo9tcW[ncnH0bY9vKGG|c3H5 M3;qbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF61JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= NXXvSXRZOTZ2OEO3O|I>
BT474 cell line MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NF7ocmhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> MmHqNVY1QDN5N{K=
HN5 cell NUHwVGc5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{ntN2lvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? Mn;wNVY4Pzd2MUC=
BT474 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7WW3dKdmirYnn0bY9vKG:oIFLUOFc1KGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{whUUN3ME2wMlA5KM7:TR?= MYGxOlc4PzRzMB?=
N87 cell M2q5Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnuO2NNUW6qaXLpeIlwdiCxZjDOPFch[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP MmPDNVY4Pzd2MUC=
HFF cell MlHDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKEiIRjDj[YxtKGe{b4f0bEwhUUN3ME25Mlkh|ryP M{X4[VE3Pzd5NEGw
SKBR3 cells MmfmR5l1d3SxeHnjbZR6KGG|c3H5 NILhZWxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF5IN88US=> M4LCSlE6ODJ6NEK1
A431 cells M{XMbmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHe0RY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4yODRizszN M{njRlE6QDh6N{[x
SKBR3 cells NFPU[IVEgXSxdH;4bYNqfHliYYPzZZk> NXe5[3lMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB{OTFOwG0> NV7mO2x7OTl6OEi3OlE>
HepG2 cells NF3heVNRem:uaX\ldoF1cW:wIHHzd4F6 MnPqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= MoLzNlAyPDN5N{i=
Hep3B2 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 NWf2[JRKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SjJiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNEmg{txO MUCyNFE1Ozd5OB?=
SKHEP1 cells MlLrVJJwdGmoZYLheIlwdiCjc4PhfS=> M1fnZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjNizszN MmnCNlAyPDN5N{i=
MCF7 cells MnLMVJJwdGmoZYLheIlwdiCjc4PhfS=> MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPU[uOkDPxE1? NGS5[pozODF2M{e3PC=>
MDA-MB-231 cells M1XxbnBzd2yrZnXyZZRqd25iYYPzZZk> MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNDFOwG0> M3y2ZVIxOTR|N{e4
SK-BR-3 cells NV2y[4lrWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3rpNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utRnIuOyClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:OC5yNDFOwG0> NIn0enAzODF2M{e3PC=>
A431 cells M2PGRmZ2dmO2aX;uJIF{e2G7 NYPGOHNsUW6qaXLpeIlwdiCxZjDFS2ZTKGmwdILhZ4VtdHWuYYKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFG0N|Eh[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6wOVIh|ryP NWLiSlU4OjB|NE[2OVU>
N87 cells NGXJd5VHfW6ldHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKEW{YlKyJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE56NzDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjFizszN NW[1R2h3OjB|NE[2OVU>
MIAPaCa cells MoHVSpVv[3Srb36gZZN{[Xl? MojsTY5pcWKrdHnvckBw\iCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNTWFR[UOjIHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVAvPDN|IN88US=> Ml7WNlA5OTd3MkO=
MIAPaCa cells NYfQdYlKTnWwY4Tpc44h[XO|YYm= NIj5[FVKdmirYnn0bY9vKG:oIFXSRoIzKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOUUGSYVPhJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMUSg{txO MYGyNFgyPzV{Mx?=
CAL27 cells NEDoS2FEgXSxdH;4bYNqfHliYYPzZZk> NXjhVGNVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByNzFOwG0v NWLKe4xtOjFyOEC2Nlk>
SKOV3 cells NWLEdpI{S3m2b4TvfIlkcXS7IHHzd4F6 MnHKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMhd3[ncnX4dJJme3OrbnegTGVTOiCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2wMlAxOyEQvF2u M1n2[FIyODhyNkK5
CAL27 cells MnTnSpVv[3Srb36gZZN{[Xl? M2qySlE3KGh? NH[zdFRKdmirYnn0bY9vKG:oIFXHSk1qdmS3Y3XkJGVITlJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEODTEK3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEWJRmKgZYZ1\XJiMU[gbJJ{KGK7IGfld5Rmem5iYnzveEwhUUN3ME2wMlA{OiEQvF2= MWqyNVA5ODZ{OR?=
SK-BR-3 cells NILDWFlRem:uaX\ldoF1cW:wIHHzd4F6 NVXRUpFDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGemKEMjDveoVz\XiycnXzd4lv\yCqdX3hckBUUy2EUj2zJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA{OiEQvF2= NEnS[HIzOTV5MEi0Ny=>
BXF T24 cells M1i3ZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFO1cFU1KGSjeYO= NG\Nc4pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDYEZiVEK0JINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF06NjZ3IN88US=> NHO3Vo4zOjF4OU[wNS=>
CXF 269L cells MnzyR5l1d3SxeHnjbZR6KGG|c3H5 MkK5OEBl[Xm| MlHCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR3hHKDJ4OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVgvOzZizszN NYLnRohDOjJzNkm2NFE>
DIFI cells NUnZdlB4S3m2b4TvfIlkcXS7IHHzd4F6 MYW0JIRigXN? NGHIZWtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFUU[LIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlI{PSEQvF2= NWP3cmx1OjJzNkm2NFE>
HT-29 cells NVHHVXZOS3m2b4TvfIlkcXS7IHHzd4F6 MX20JIRigXN? M3nvPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20MlYzKM7:TR?= NFvzeI4zOjF4OU[wNS=>
RKO cells MmnTR5l1d3SxeHnjbZR6KGG|c3H5 MmHVOEBl[Xm| M{Sz[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJMVyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;NT6zOUDPxE1? MlHTNlIyPjl4MEG=
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LIXF 575L cells M3v2OGN6fG:2b4jpZ4l1gSCjc4PhfS=> MYG0JIRigXN? NH:4PWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNUViIIEW3OWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwMUig{txO M135PFIzOTZ7NkCx
LXFA 289L cells M1LhUWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3LTVlQh\GG7cx?= M1mzR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkFiMki5UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:PS55OTFOwG0> M2rmV|IzOTZ7NkCx
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MCF7 cells M4nwfmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHztNnU1KGSjeYO= M{DjVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuPFMh|ryP MnzENlIyPjl4MEG=
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OVXF 899L NIHTV2REgXSxdH;4bYNqfHliYYPzZZk> NUXWZoZUPCCmYYnz MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWnhHKDh7OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvOzVizszN M1q5Z|IzOTZ7NkCx
PAXF 546L cells NI\ONHNEgXSxdH;4bYNqfHliYYPzZZk> NUfPZ21vPCCmYYnz NF7ZOGVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSViIIEW0Omwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTZwMUKg{txO MWWyNlE3QTZyMR?=
PANC1 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= MmjuOEBl[Xm| NFzRbnNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSU6FMTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4yOiEQvF2= NUnxVppVOjJzNkm2NFE>
22Rv1 cell Mo\0R5l1d3SxeHnjbZR6KGG|c3H5 M3HoVVQh\GG7cx?= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCyNnJ3OSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nj6wOkDPxE1? NGHyW44zOjF4OU[wNS=>
DU145 cells MkHkR5l1d3SxeHnjbZR6KGG|c3H5 MYC0JIRigXN? MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Mj65PUDPxE1? MlfDNlIyPjl4MEG=
LNCAP cells M1:2T2N6fG:2b4jpZ4l1gSCjc4PhfS=> NH;HTnk1KGSjeYO= NYntWXVuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN NYm2OFZ7OjJzNkm2NFE>
PC3M cells MnHiR5l1d3SxeHnjbZR6KGG|c3H5 MUm0JIRigXN? MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|NOKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkW1JO69VQ>? MoX6NlIyPjl4MEG=
NIH/3T3 cells Mo\DVJJwdGmoZYLheIlwdiCjc4PhfS=> M{PneVczKGh? M4jXcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuN{DPxE1? MWeyNlU6PTF5Nx?=
NCI-H1648 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TiW2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yMkW0OEDPxE1? NUTTboZvW0GQR1XS
NMC-G1 cell MnfhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHPldG1KdmirYnn0bY9vKG:oIHj1cYFvKE6PQz3HNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTR3MEGg{txO M{[wTHNCVkeHUh?=
NTERA-S-cl-D1 cell MnH0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH:4W41KdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlI3PTZzIN88US=> NEeySXNUSU6JRWK=
OCUB-M cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHwTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA2PzRizszN MVXTRW5ITVJ?
OS-RC-2 cell NUnPVW9pT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MluzTY5pcWKrdHnvckBw\iCqdX3hckBQWy2UQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46QTF7OTFOwG0> MVHTRW5ITVJ?
OVCAR-4 cell NVT5[YVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoX1TY5pcWKrdHnvckBw\iCqdX3hckBQXkODUj20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yOTZ5NTFOwG0> MnLwV2FPT0WU
RL95-2 cell NFvEXVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmP3TY5pcWKrdHnvckBw\iCqdX3hckBTVDl3LUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2PjdizszN MWPTRW5ITVJ?
SW954 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEj6SmxKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> M1z1RXNCVkeHUh?=
SW962 cell NEDiWopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXVV|dZUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl{NEWg{txO MWnTRW5ITVJ?
TE-1 cell MlXpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLtTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6wNlE2QSEQvF2= NInNdZFUSU6JRWK=
A253 cell MkPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGEzPTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP MonoV2FPT0WU
A388 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHIU293UW6qaXLpeIlwdiCxZjDoeY1idiCDM{i4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPDh|IN88US=> MmDqV2FPT0WU
BB30-HNC cell MnmxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGJDOzBvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PzN|NTFOwG0> Mn7iV2FPT0WU
TE-12 cell NGDxUINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWXDR2VqUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzJ{NUig{txO NHPwXXFUSU6JRWK=
TE-5 cell MlzKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DPSWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQ3PTRizszN M4nwc3NCVkeHUh?=
TE-6 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{PRbWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFkxPTdizszN MmnpV2FPT0WU
TE-8 cell NILyd2RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWXyTXl[UW6qaXLpeIlwdiCxZjDoeY1idiCWRT24JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOzd|IN88US=> MULTRW5ITVJ?
TE-9 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVzqO|RKUW6qaXLpeIlwdiCxZjDoeY1idiCWRT25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTJyMTFOwG0> MX7TRW5ITVJ?
TK10 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\YTY5pcWKrdHnvckBw\iCqdX3hckBVUzFyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlUzOiEQvF2= NF;LcWxUSU6JRWK=
DSH1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFThUodKdmirYnn0bY9vKG:oIHj1cYFvKESVSEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6Ozl4IN88US=> Mn\JV2FPT0WU
ECC12 cell NX[1e5ZzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGVESzF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVI{OSEQvF2= NFv3ZWRUSU6JRWK=
EKVX cell NUS0VlVkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= M4rCOXNCVkeHUh?=
HCC2218 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPHd4tGUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNlE5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNUOyOkDPxE1? M4PVW3NCVkeHUh?=
LB2241-RCC cell NYr1V|M{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF3NECzJO69VQ>? M3XGfXNCVkeHUh?=
LB996-RCC cell M1PRcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnGwTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? MYnTRW5ITVJ?
LC-1F cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGxENTGIIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zPFI1PCEQvF2= NF73TY5USU6JRWK=
LS-513 cell NXf3UHgzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\OTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQxODRzIN88US=> MYPTRW5ITVJ?

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2
  • 濃度: Dissolved in DMSO, final concentrations ~100 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
  • 製剤: Formulated in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
  • 投薬量: ~100 mg/kg
  • 投与方法: Orally twice daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (108.05 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 925.46
化学式

C29H26ClFN4O4S.2C7H8O3S

CAS No. 388082-77-7
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    If I need to use S1028 for treating tumor-bearing mice with injection, how could I prepare the solution?

  • 回答:

    S1028 Lapatinib Ditosylate can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as clear solution.

HER2シグナル伝達経路

HER2 Inhibitors with Unique Features

相関HER2製品

Tags: Lapatinib (GW-572016) Ditosylateを買う | Lapatinib (GW-572016) Ditosylate ic50 | Lapatinib (GW-572016) Ditosylate供給者 | Lapatinib (GW-572016) Ditosylateを購入する | Lapatinib (GW-572016) Ditosylate費用 | Lapatinib (GW-572016) Ditosylate生産者 | オーダーLapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate化学構造 | Lapatinib (GW-572016) Ditosylate分子量 | Lapatinib (GW-572016) Ditosylate代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID