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.

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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 M3HHfXBzd2yrZnXyZZRqd25iYYPzZZk> MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxtKGyrbnWsJGlEPTB;MD6wNlUh|ryP M4DQPFE3PDh|N{ey
BT474 cell line NEHPfnVRem:uaX\ldoF1cW:wIHHzd4F6 NWDJSmpkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsJIxqdmVuIFnDOVA:OC5yMkWg{txO M1O5NFE3PDh|N{ey
HN5 cell M2jMNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\2VGF3UW6qaXLpeIlwdiCxZjDIUlUh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNVIh|ryP M3HiOVE3Pzd5NEGw
BT474 cell NVH5[ZBET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKEKWNEe0JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkC4JO69VQ>? NIHRNIEyPjd5N{SxNC=>
N87 cell M4PsNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnvwTY5pcWKrdHnvckBw\iCQOEegZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEig{txO NH;lT3cyPjd5N{SxNC=>
HFF cell M2LXPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEPZSHVKdmirYnn0bY9vKG:oIFjGSkBk\WyuIHfyc5d1cCxiSVO1NF06NjlizszN MmjKNVY4Pzd2MUC=
SKBR3 cells MoHJR5l1d3SxeHnjbZR6KGG|c3H5 NVL2UFdnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzNzFOwG0> NU\qTJI3OTlyMki0NlU>
A431 cells MkjtR5l1d3SxeHnjbZR6KGG|c3H5 M13uXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlExPCEQvF2= MWixPVg5QDd4MR?=
SKBR3 cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFI6KM7:TR?= MXWxPVg5QDd4MR?=
HepG2 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M3jrSmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvOjdizszN NWnjRZNXOjBzNEO3O|g>
Hep3B2 cells NGjlZYVRem:uaX\ldoF1cW:wIHHzd4F6 MnLGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYCzRlIh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVUvPDlizszN NWrkbmNWOjBzNEO3O|g>
SKHEP1 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 M{L2XWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjNizszN MX2yNFE1Ozd5OB?=
MCF7 cells M2TZOHBzd2yrZnXyZZRqd25iYYPzZZk> MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPU[uOkDPxE1? NF;NTnczODF2M{e3PC=>
MDA-MB-231 cells NF7CXFdRem:uaX\ldoF1cW:wIHHzd4F6 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNDFOwG0> MUCyNFE1Ozd5OB?=
SK-BR-3 cells M{Djd3Bzd2yrZnXyZZRqd25iYYPzZZk> NIPhOXVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMWJTNTNiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTBwMESg{txO M{PPUFIxOTR|N{e4
A431 cells NIi3T2hHfW6ldHnvckBie3OjeR?= Mli5TY5pcWKrdHnvckBw\iCHR1\SJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEF2M{GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5yNUKg{txO NWDRfpRROjB|NE[2OVU>
N87 cells NWfWOnc6TnWwY4Tpc44h[XO|YYm= NEfWXolKdmirYnn0bY9vKG:oIFXyZmIzKGmwdILhZ4VtdHWuYYKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF64O{Bk\WyuczDifUBGVEmVQTygTWM2OD1yLkGg{txO MmDqNlA{PDZ4NUW=
MIAPaCa cells Mkn0SpVv[3Srb36gZZN{[Xl? NEDvWlRKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO NHzsNmUzODhzN{WyNy=>
MIAPaCa cells M2HqZWZ2dmO2aX;uJIF{e2G7 Mm\CTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> NEDrUFEzODhzN{WyNy=>
CAL27 cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= NEfXW|JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB5IN88UU4> MV[yNVA5ODZ{OR?=
SKOV3 cells M4nMSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVTyN2pHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNib4\ldoV5eHKnc4PpcochUEWUMjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByMzFOwG0v NYS5OmFuOjFyOEC2Nlk>
CAL27 cells NI\YdJZHfW6ldHnvckBie3OjeR?= M1LnbFE3KGh? M3XvSWlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0MEBKSzVyPUCuNFMzKM7:TR?= NHPXeJUzOTB6ME[yPS=>
SK-BR-3 cells NYXHVlZiWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXyZmIzKG:4ZYLlfJBz\XO|aX7nJIh2dWGwIGPLMWJTNTNiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEOyJO69VQ>? NH3GN|YzOTV5MEi0Ny=>
BXF T24 cells MV3DfZRwfG:6aXPpeJkh[XO|YYm= M2\4cVQh\GG7cx?= NF3mdpNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDYEZiVEK0JINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF06NjZ3IN88US=> MXyyNlE3QTZyMR?=
CXF 269L cells MnfNR5l1d3SxeHnjbZR6KGG|c3H5 MkTSOEBl[Xm| M1XZSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNZTiB{NknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF05NjN4IN88US=> NVnkXXQyOjJzNkm2NFE>
DIFI cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NGn5c5M1KGSjeYO= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDETWZKKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1yLkKzOUDPxE1? NWPFPGN1OjJzNkm2NFE>
HT-29 cells NV;zc2JYS3m2b4TvfIlkcXS7IHHzd4F6 M{L1[|Qh\GG7cx?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND62NkDPxE1? MoPjNlIyPjl4MEG=
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LIXF 575L cells NFPW[XVEgXSxdH;4bYNqfHliYYPzZZk> MYq0JIRigXN? NHuzdJVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNUViIIEW3OWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwMUig{txO NFjweo8zOjF4OU[wNS=>
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OVXF 899L MmXhR5l1d3SxeHnjbZR6KGG|c3H5 M3vqZlQh\GG7cx?= NEP1eXVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXliIIEi5PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTNwM{Wg{txO M33TeFIzOTZ7NkCx
PAXF 546L cells M4XmRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MXW0JIRigXN? MkDDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFZTiB3NE\MJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF03NjF{IN88US=> NHT1RYYzOjF4OU[wNS=>
PANC1 cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= Mle5OEBl[Xm| MnXoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFPSzFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUiuNVIh|ryP NFv5UVIzOjF4OU[wNS=>
22Rv1 cell M2\5VGN6fG:2b4jpZ4l1gSCjc4PhfS=> M37SWVQh\GG7cx?= M1\j[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFIzWnZzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME22MlA3KM7:TR?= MUiyNlE3QTZyMR?=
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PC3M cells MlzyR5l1d3SxeHnjbZR6KGG|c3H5 MXK0JIRigXN? MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|NOKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkW1JO69VQ>? MlP2NlIyPjl4MEG=
NIH/3T3 cells M{HLN3Bzd2yrZnXyZZRqd25iYYPzZZk> NXfMSGgyPzJiaB?= NW\DUFh6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDOTWgwO1R|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OE4{KM7:TR?= MnLHNlI2QTVzN{e=
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OCUB-M cell Ml;GS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGDkdJBKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV5NDFOwG0> NG\tS4FUSU6JRWK=
OS-RC-2 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NITrXoFKdmirYnn0bY9vKG:oIHj1cYFvKE:VLWLDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl7MUm5JO69VQ>? MYPTRW5ITVJ?
OVCAR-4 cell NXHkXpdCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYPJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlEyPjd3IN88US=> MXrTRW5ITVJ?
RL95-2 cell NYHBRYV2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NG\V[YxKdmirYnn0bY9vKG:oIHj1cYFvKFKOOUWtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTV4NzFOwG0> NHXSPWpUSU6JRWK=
SW954 cell NE\1SXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXnJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= MoT0V2FPT0WU
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A388 cell NYrRcXY4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlX4TY5pcWKrdHnvckBw\iCqdX3hckBCOzh6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NIjpOIZUSU6JRWK=
BB30-HNC cell NVq2cI9pT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDiTY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTd|M{Wg{txO MnewV2FPT0WU
TE-12 cell NXzHTmptT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nPb2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczOjV6IN88US=> NYrjeJdlW0GQR1XS
TE-5 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PC[GlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQ3PTRizszN NFzBW|dUSU6JRWK=
TE-6 cell M1HsTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5NFU4KM7:TR?= M3XoOXNCVkeHUh?=
TE-8 cell M2m1[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jZ[2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNFM4OyEQvF2= M3[5ZnNCVkeHUh?=
TE-9 cell MnHIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLu[opKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU2OjBzIN88US=> NYLxSGFjW0GQR1XS
TK10 cell NFiwVmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NULsWJRQUW6qaXLpeIlwdiCxZjDoeY1idiCWS{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yPjV{MjFOwG0> NVnPRZU6W0GQR1XS
DSH1 cell MlH0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGRUUDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5N|k3KM7:TR?= NX;zclBvW0GQR1XS
ECC12 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1e4UmlvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA6OjNzIN88US=> NEHqN4tUSU6JRWK=
EKVX cell M4DzOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJGVMXlhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS0PFc1KM7:TR?= MU\TRW5ITVJ?
HCC2218 cell MmOzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1LjVGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkKxPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV|Mk[g{txO NUf6flE3W0GQR1XS
LB2241-RCC cell NEHBdldIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1fBNGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMUW0NFMh|ryP NV7h[Zo3W0GQR1XS
LB996-RCC cell Ml;MS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGxDQTl4LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ{Mkig{txO MXXTRW5ITVJ?
LC-1F cell NIHyTVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4K1RWlvcGmkaYTpc44hd2ZiaIXtZY4hVENvMV[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlM5OjR2IN88US=> M2jvfnNCVkeHUh?=
LS-513 cell M1jhVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFAxPDFizszN M{HGTXNCVkeHUh?=

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

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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