Lapatinib

製品コードS2111 別名:GW-572016, GSK572016

Lapatinib化学構造

分子量(MW):581.06

Lapatinib, used in the form of Lapatinib 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 23738.00
JPY 18260.00
JPY 44820.00

文献中Selleckの製品使用例(42)

カスタマーフィードバック(7)

  • Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).

    Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck.

    Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies.

    Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck.

  • Inhibition of HER2 using siRNAs show a similar response measured by induced apoptosis, decreased proliferation and decreased phospho-p70-S6K staining as Lapatinib mono-treatment and combinatorial treatment with Lapatinib and trastuzumab. Trastuzumab mono-treatment is less efficient than siHER2.

    Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck.

    Lapatinib effectively inhibits EGFR activation, leading to a reduc- tion in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 μM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck.

  •  

    Endogenous associations between STAT1, EGFR, and p-STAT3 expression in breast cancer cells. (B) Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 uM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck.

    Combination treatment with lapatinib and CZ0775 significantly induces pro-apoptotic BIM proteins in H195 cells. HCC827 (a) and H1975 (b) cells were treated with either 1 μM lapatinib alone or the combination of 1 μM lapatinib plus 1 μM AZD6244 or CZ0775 for 24 h. Cell lysates were analyzed by Western blotting using the indicated antibodies. The levels of β -actin served as a loading control

    Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck.

  •  

    EGF and TGF-α-induced CD44 expression is reduced by EGFR inhibitors in SKBR3 breast cancer cells. After serum-starvation for 24 h, the cells were pretreated with EGFR inhibitors, AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then, treated with EGF (A) or TGF-α (B) for 24 h. The level of CD44 mRNA expression was analyzed by real-time PCR. After serum-starvation for 24 h, the cells were pretreated with AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then treated with EGF for 24 h (C). The levels of CD44, EGFR, ERK, and β-actin protein expression were analyzed by Western blotting.

    Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Lapatinib, used in the form of Lapatinib 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 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 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 inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib 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 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
NCI-H1648 NHz1SJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ntZmlEPTB;MD6wNlU1PCEQvF2= M3XIS3NCVkeHUh?=
HCC2218 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnizTWM2OD1yLkC1N|I3KM7:TR?= MXvTRW5ITVJ?
OCUB-M NYnIdlJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jWTmlEPTB;MD6wOVc1KM7:TR?= Mo\4V2FPT0WU
ECC12 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMEmyN|Eh|ryP NGjTT5ZUSU6JRWK=
DSH1 NIHtc|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfzTWM2OD1yLkC5N|k3KM7:TR?= MWnTRW5ITVJ?
BT-474 M{Lre2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf1TWM2OD1yLkKxN|E2KM7:TR?= MULTRW5ITVJ?
BB30-HNC NFHlS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzmPJU5UUN3ME2wMlI1PjV2IN88US=> Mn3GV2FPT0WU
EKVX MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;hTWlEPTB;MD60OFg4PCEQvF2= MXrTRW5ITVJ?
TE-12 NY\aPYRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTQTWM2OD1yLkS5NFU4KM7:TR?= NHnHNFdUSU6JRWK=
A388 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPBTWM2OD1yLkeyNlU5KM7:TR?= MYPTRW5ITVJ?
TE-9 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DkTGlEPTB;MD63OFQ2OyEQvF2= MUnTRW5ITVJ?
LB2241-RCC M{Tm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfCOFlKSzVyPUGuNVU1ODNizszN MkXsV2FPT0WU
LB996-RCC MmDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjiU4RKSzVyPUGuN|YzOjhizszN NUT5fo1yW0GQR1XS
LC-1F NW[wSmYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPPUpQ3UUN3ME2xMlM5OjR2IN88US=> MXTTRW5ITVJ?
TE-6 NYL3fWN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDlW203UUN3ME2xMlU2OjBzIN88US=> M4H2WHNCVkeHUh?=
A253 M1;odWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfKe3RKSzVyPUGuPVc{OzVizszN M3rlTHNCVkeHUh?=
OS-RC-2 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfDXVI4UUN3ME2xMlk6OTl7IN88US=> NF3pfZlUSU6JRWK=
TE-1 NXOybJB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJwMES4N{DPxE1? M2rGWHNCVkeHUh?=
RL95-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNwMUW2O{DPxE1? NF\qZ5NUSU6JRWK=
LS-513 NVjtV|VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwNECwOFEh|ryP MYLTRW5ITVJ?
DJM-1 NGjidm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXmbIE3UUN3ME2zMlQ3QTd3IN88US=> MmDxV2FPT0WU
NMC-G1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEH1O2NKSzVyPUOuOVQ2ODFizszN NFzVZnRUSU6JRWK=
TE-10 NIX3PYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfSTWM2OD1|LkW1N|U3KM7:TR?= MXHTRW5ITVJ?
TE-5 NGrUfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPHXFVGUUN3ME20MlA{PzNizszN M2PaPHNCVkeHUh?=
TK10 NWnSeXZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTRwMU[1NlIh|ryP MkjYV2FPT0WU
UACC-812 M3vSemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4q3dGlEPTB;ND61OlE2OyEQvF2= MYHTRW5ITVJ?
SW962 M4j0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTMTWM2OD13LkCyNVU6KM7:TR?= M2j4XXNCVkeHUh?=
SW954 NF[3V2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTVwM{myOFUh|ryP MkPvV2FPT0WU
COLO-668 MnjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C3cmlEPTB;NT63NlY3PyEQvF2= NYXHflZPW0GQR1XS
LB1047-RCC MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjHTWM2OD13LkiwNFQ3KM7:TR?= MoTmV2FPT0WU
NB5 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3eyVmlEPTB;Nj6yNVAxOSEQvF2= MknaV2FPT0WU
NTERA-S-cl-D1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzKTWM2OD14LkK2OVYyKM7:TR?= NI\xTFBUSU6JRWK=
IST-MEL1 NVKzR49NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLSVll7UUN3ME22MlQ{Pjl2IN88US=> M1vY[HNCVkeHUh?=
GI-1 M3LhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7Z[GxKSzVyPU[uOVE3QDJizszN MoqxV2FPT0WU
TGBC1TKB NE\iTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHKyPZhKSzVyPUeuNFcyQDNizszN MV3TRW5ITVJ?
GT3TKB NHzHfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn74TWM2OD15LkKyO|Q1KM7:TR?= NGXGUlJUSU6JRWK=
EVSA-T MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrtc3dYUUN3ME23MlQzQDFzIN88US=> M2nXfXNCVkeHUh?=
D-502MG MlLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfrOHRVUUN3ME23MlQ5QDl2IN88US=> NV3V[I52W0GQR1XS
TE-8 NEizWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnSeIlKSzVyPUeuO|YyPTlizszN MX\TRW5ITVJ?
OVCAR-4 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzwbGhXUUN3ME25MlEyPjd3IN88US=> MoC1V2FPT0WU
D-336MG NFnSWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nnb2lEPTB;OT60O|M6PSEQvF2= M2rLWHNCVkeHUh?=
GCIY MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTlwNUe0NkDPxE1? MYnTRW5ITVJ?
KS-1 MnvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LGe2lEPTB;OT62OlI5PyEQvF2= M4P5WnNCVkeHUh?=
HCC2998 MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHmzN|VKSzVyPUmuPVY{ODdizszN MmDvV2FPT0WU
D-247MG NGHBZoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jTT2lEPTB;OT65PFI6OSEQvF2= NGewfIJUSU6JRWK=
TE-15 M{DGcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HQcWlEPTB;MUCuNlQ2KM7:TR?= NWmxNFJGW0GQR1XS
IST-MES1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2WxdmlEPTB;MUCuNlU3PSEQvF2= M4j5[3NCVkeHUh?=
ETK-1 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFyLk[yN{DPxE1? MWrTRW5ITVJ?
RCC10RGB M3uwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnkOI9KSzVyPUGwMlk3OSEQvF2= MV;TRW5ITVJ?
KNS-42 M363Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPHTWM2OD1zMT63NlU2KM7:TR?= M3jWeXNCVkeHUh?=
LB771-HNC M3vvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXpU4pKSzVyPUGyMlE4OTJizszN NGe5WXdUSU6JRWK=
SR M17rd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTF{LkKwOlQh|ryP MUPTRW5ITVJ?
NCI-H1355 NELicGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:xc2lEPTB;MUKuPFk5PSEQvF2= NUS3O5RpW0GQR1XS
ES6 NFjIWmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LZNGlEPTB;MUOuNFc5KM7:TR?= MUDTRW5ITVJ?
SK-NEP-1 M3P2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\yd2lEPTB;MUOuNlU4PyEQvF2= M1frRnNCVkeHUh?=
D-392MG Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTF|Lk[0Nlgh|ryP MWrTRW5ITVJ?
NB7 NVLlVol{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHscIs1UUN3ME2xOE4zOzd2IN88US=> NWnFeZplW0GQR1XS
SK-LMS-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HKN2lEPTB;MUSuOVE1PSEQvF2= NE\k[XpUSU6JRWK=
SK-UT-1 MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13jRWlEPTB;MUSuO|g5QSEQvF2= M3;nRXNCVkeHUh?=
CA46 NIrNcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17DPGlEPTB;MUWuNFU5PiEQvF2= MoruV2FPT0WU
IST-SL2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfOdZBKSzVyPUG1MlE6ODFizszN MX7TRW5ITVJ?
BC-1 NHP4dlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3SzXGlEPTB;MUWuN|MyPCEQvF2= NVnIO216W0GQR1XS
LS-123 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfYeIhKSzVyPUG1MlgyPzNizszN NWPqdWNkW0GQR1XS
Ramos-2G6-4C10 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\KcWlEPTB;MU[uNFkzPCEQvF2= Ml3SV2FPT0WU
MZ1-PC MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fBOWlEPTB;MU[uO|MyOyEQvF2= NY\XUIs6W0GQR1XS
LB647-SCLC NET2RVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3i[2U1UUN3ME2xOk46Ozd{IN88US=> MlnMV2FPT0WU
NCI-H1694 Mmr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF5LkG1Nlkh|ryP NELOXIxUSU6JRWK=
NCI-H322M NYnDbXZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILrR5JKSzVyPUG3MlQ{PjZizszN NVSwfIZiW0GQR1XS
ES7 NWKyR5pPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\RTnVKSzVyPUG4MlM6OTRizszN NVTkc45zW0GQR1XS
LC-2-ad MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHGTWM2OD1zOD60N|g3KM7:TR?= MlfpV2FPT0WU
SF268 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXLPVRKSzVyPUG4Mlc1ODlizszN M33FdnNCVkeHUh?=
RPMI-8402 Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S1cGlEPTB;MUmuNFc1OiEQvF2= M1rDNHNCVkeHUh?=
HCE-T M2\RWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTkPYdXUUN3ME2yNE4zOzR2IN88US=> M2H0WXNCVkeHUh?=
A101D NXu0OZFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLSTWM2OD1{MD64OVg4KM7:TR?= MU\TRW5ITVJ?
MRK-nu-1 NUfGOY83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzCTWM2OD1{MD65NVMh|ryP NIfJT2tUSU6JRWK=
LXF-289 M{LHWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T2cWlEPTB;MkGuNFM5KM7:TR?= M1jRSHNCVkeHUh?=
NALM-6 NV7he3JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfObI5XUUN3ME2yNU4yQTZ5IN88US=> NIKyZ5dUSU6JRWK=
DOHH-2 NXrJUYFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{T3VGlEPTB;MkGuOFgyOyEQvF2= M1nyOnNCVkeHUh?=
EW-16 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJ{LkG0NFIh|ryP MV;TRW5ITVJ?
A4-Fuk M3\xdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq4R2xKSzVyPUKyMlIyPDlizszN NHXObmRUSU6JRWK=
HD-MY-Z NYS2U4ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPaclVKSzVyPUKyMlM6PjVizszN NYm2dZR5W0GQR1XS
SKM-1 MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3NVWJvUUN3ME2yNk44OzVzIN88US=> MVrTRW5ITVJ?
DMS-153 NYHQOmFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;ieHRmUUN3ME2yN{41OjB2IN88US=> NHnsVmJUSU6JRWK=
LB373-MEL-D NXy2enU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfOSnVZUUN3ME2yN{42PDV{IN88US=> NYX5eWo4W0GQR1XS
LP-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXhd2UxUUN3ME2yN{45ODl5IN88US=> NHXRTGlUSU6JRWK=
GI-ME-N M2j1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCy[oJKSzVyPUK0MlI6OiEQvF2= MU\TRW5ITVJ?
MPP-89 NYnDV5NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;qN|NKSzVyPUK1MlIxOzZizszN M2jkbXNCVkeHUh?=
U-698-M M2TvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3KTWM2OD1{NT6yOVA{KM7:TR?= NYqzNml5W0GQR1XS
HC-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PKeGlEPTB;MkWuOlQyQCEQvF2= M1e5fnNCVkeHUh?=
HCC2157 NH;KbHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJ3Lk[3N{DPxE1? NVnH[YpMW0GQR1XS
MOLT-4 M4Pjbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ4LkK3N{DPxE1? NYjYb206W0GQR1XS
LS-411N NX\aU4tQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJ4LkOzOlkh|ryP MW\TRW5ITVJ?
Becker NGCyRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rpZWlEPTB;Mk[uOVE5OSEQvF2= M3PoN3NCVkeHUh?=
NCI-H23 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPNNIVKSzVyPUK2Mlc2PzVizszN NGPlfYNUSU6JRWK=
IST-SL1 M1\OfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoToTWM2OD1{Nz6zPFY4KM7:TR?= M{T1bXNCVkeHUh?=
MZ2-MEL MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7FUZdKSzVyPUK3MlQ2PjZizszN MlL0V2FPT0WU
RKO MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe0[4xKSzVyPUK4MlE1PDZizszN M4rh[HNCVkeHUh?=
TE-441-T NXHPUHBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXyemJKSzVyPUK4Mlc5QSEQvF2= NIPsVmNUSU6JRWK=
EW-24 M1XLS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLpXohqUUN3ME2yPU4yOjV7IN88US=> M3;ubXNCVkeHUh?=
no-10 NX36XXBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zufmlEPTB;MkmuNVY{OSEQvF2= MX3TRW5ITVJ?
D-542MG Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[2XZBrUUN3ME2yPU46OjJzIN88US=> NGjEb2xUSU6JRWK=
ST486 M{O5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q3bWlEPTB;M{CuOlQ2OSEQvF2= NVzPV2dKW0GQR1XS
KURAMOCHI M2TSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TxfWlEPTB;M{CuPFA2PyEQvF2= MVnTRW5ITVJ?
ES8 NFHnbHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTR[4djUUN3ME2zNU42QTd{IN88US=> NGDEcXFUSU6JRWK=
BL-41 NFXjOmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvVTWM2OD1|Mj6xNFU1KM7:TR?= Mn76V2FPT0WU
NB6 NIfI[3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTN{LkO4OVUh|ryP NILXTYVUSU6JRWK=
NCI-H1304 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HWOWlEPTB;M{KuOFk3PyEQvF2= NYCySZhiW0GQR1XS
MS-1 MknIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfLSGhYUUN3ME2zNk44PzVzIN88US=> MUDTRW5ITVJ?
MFH-ino MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TEUGlEPTB;M{SuN|IzPCEQvF2= NULhfmxMW0GQR1XS
NOS-1 NVnpUopST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\SZnJRUUN3ME2zOE43PzR6IN88US=> MoqyV2FPT0WU
HUTU-80 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\PSHdrUUN3ME2zOU4{PjZ5IN88US=> M17Bc3NCVkeHUh?=
EB2 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\P[GlEPTB;M{[uOlE5QSEQvF2= MYXTRW5ITVJ?
L-540 MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljpTWM2OD1|Nz6yN|A5KM7:TR?= NYTJ[lk2W0GQR1XS
NCI-H747 M3GzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTN6Lki4OFYh|ryP NVGzfmNwW0GQR1XS
NCI-H446 M1rXOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrYO3JZUUN3ME2zPU46PjVzIN88US=> Mmr6V2FPT0WU
MOLT-16 NVT6d3RpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3mU5Z7UUN3ME20Nk41OTVizszN NUfITIFRW0GQR1XS
BC-3 NH75eHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPQTWM2OD12NT60PFk3KM7:TR?= M4PqfnNCVkeHUh?=
SJSA-1 NIDzVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTR3LkW0O|Qh|ryP M17Gb3NCVkeHUh?=
BB65-RCC NHL1c2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13JdGlEPTB;NEWuOlY3KM7:TR?= NIXRPWtUSU6JRWK=
SNB75 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKyTWM2OD12Nj6wNVgh|ryP NXTVPHY4W0GQR1XS

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 (~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 cells
  • 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 (172.09 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+5% Tween 80+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 581.06
化学式

C29H26ClFN4O4S

CAS No. 231277-92-2
保管
in solvent
別名 GW-572016, GSK572016

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 want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

  • 回答:

    For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

EGFRシグナル伝達経路

EGFR Inhibitors with Unique Features

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Tags: Lapatinibを買う | Lapatinib ic50 | Lapatinib供給者 | Lapatinibを購入する | Lapatinib費用 | Lapatinib生産者 | オーダーLapatinib | Lapatinib化学構造 | Lapatinib分子量 | Lapatinib代理店
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