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 NF\3fHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPlO2hJUUN3ME2wMlAzPTR2IN88US=> NXXHPJpVW0GQR1XS
HCC2218 NG\rSmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfDUldWUUN3ME2wMlA2OzJ4IN88US=> M4XnRnNCVkeHUh?=
OCUB-M MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnZTWM2OD1yLkC1O|Qh|ryP NWHue5M4W0GQR1XS
ECC12 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfvXnhKSzVyPUCuNFkzOzFizszN NFW4[XJUSU6JRWK=
DSH1 NHj2WJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwMEmzPVYh|ryP MX\TRW5ITVJ?
BT-474 MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\vOYRMUUN3ME2wMlIyOzF3IN88US=> Mn\aV2FPT0WU
BB30-HNC M3jCS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwMkS2OVQh|ryP M{nKb3NCVkeHUh?=
EKVX MlSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nMdGlEPTB;MD60OFg4PCEQvF2= M4jFfXNCVkeHUh?=
TE-12 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XNNWlEPTB;MD60PVA2PyEQvF2= NXWwbY1lW0GQR1XS
A388 NVvyS5lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnMTWM2OD1yLkeyNlU5KM7:TR?= NHjPfGNUSU6JRWK=
TE-9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MniwTWM2OD1yLke0OFU{KM7:TR?= M{jub3NCVkeHUh?=
LB2241-RCC Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHYT2ZKSzVyPUGuNVU1ODNizszN M3vzVnNCVkeHUh?=
LB996-RCC NVX2OJVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHBd3hiUUN3ME2xMlM3OjJ6IN88US=> NE\QUY1USU6JRWK=
LC-1F M4fLfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvpTWM2OD1zLkO4NlQ1KM7:TR?= Mn7mV2FPT0WU
TE-6 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFwNUWyNFEh|ryP M37PRXNCVkeHUh?=
A253 M1uzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;hd4N[UUN3ME2xMlk4OzN3IN88US=> MUHTRW5ITVJ?
OS-RC-2 M4myfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3wR3NIUUN3ME2xMlk6OTl7IN88US=> NWPxXGw5W0GQR1XS
TE-1 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJwMES4N{DPxE1? Ml;KV2FPT0WU
RL95-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;OS3JKSzVyPUOuNVU3PyEQvF2= M3rBVnNCVkeHUh?=
LS-513 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTNwNECwOFEh|ryP MX7TRW5ITVJ?
DJM-1 NYfjN5JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnpd21QUUN3ME2zMlQ3QTd3IN88US=> NEjU[llUSU6JRWK=
NMC-G1 NYXQdo1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnyNIV2UUN3ME2zMlU1PTBzIN88US=> MknIV2FPT0WU
TE-10 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH5b|lQUUN3ME2zMlU2OzV4IN88US=> MXvTRW5ITVJ?
TE-5 M4\TVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTRwMEO3N{DPxE1? NV;K[5dnW0GQR1XS
TK10 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPYPYNKSzVyPUSuNVY2OjJizszN MkXtV2FPT0WU
UACC-812 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm2SpVKSzVyPUSuOVYyPTNizszN NX7Re3JjW0GQR1XS
SW962 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[1bFA1UUN3ME21MlAzOTV7IN88US=> MmX1V2FPT0WU
SW954 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTVwM{myOFUh|ryP Ml3HV2FPT0WU
COLO-668 NHrQcVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7ZTWM2OD13LkeyOlY4KM7:TR?= NGLkU5lUSU6JRWK=
LB1047-RCC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nTS2lEPTB;NT64NFA1PiEQvF2= MkK5V2FPT0WU
NB5 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTZwMkGwNFEh|ryP NX3HZWdXW0GQR1XS
NTERA-S-cl-D1 M4HoV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrrcGY2UUN3ME22MlI3PTZzIN88US=> NUTOSZJlW0GQR1XS
IST-MEL1 NWfReVU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTkO3dlUUN3ME22MlQ{Pjl2IN88US=> NIK1UXJUSU6JRWK=
GI-1 NFrFN2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jwVmlEPTB;Nj61NVY5OiEQvF2= M37rT3NCVkeHUh?=
TGBC1TKB MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TRUWlEPTB;Nz6wO|E5OyEQvF2= M{KzOnNCVkeHUh?=
GT3TKB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCxc|cyUUN3ME23MlIzPzR2IN88US=> NIrFOldUSU6JRWK=
EVSA-T NXXZS5E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHnbpdKSzVyPUeuOFI5OTFizszN M{G5XXNCVkeHUh?=
D-502MG M1XqfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTdwNEi4PVQh|ryP MUDTRW5ITVJ?
TE-8 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv4WHFKSzVyPUeuO|YyPTlizszN NIDCfXJUSU6JRWK=
OVCAR-4 NVL3e5ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXaZ5BzUUN3ME25MlEyPjd3IN88US=> NVW1XnBuW0GQR1XS
D-336MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jUXmlEPTB;OT60O|M6PSEQvF2= M{Hpd3NCVkeHUh?=
GCIY MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr0SIFEUUN3ME25MlU4PDJizszN NUTpd4E2W0GQR1XS
KS-1 MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPVTWM2OD17Lk[2Nlg4KM7:TR?= NHjJ[YFUSU6JRWK=
HCC2998 M{D2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTlwOU[zNFch|ryP Ml\lV2FPT0WU
D-247MG NGGzcGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXiSJdbUUN3ME25Mlk5OjlzIN88US=> NGjjOnhUSU6JRWK=
TE-15 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1njRWlEPTB;MUCuNlQ2KM7:TR?= M1;LZnNCVkeHUh?=
IST-MES1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFyLkK1OlUh|ryP Mnr2V2FPT0WU
ETK-1 M4jjNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrJfXZlUUN3ME2xNE43OjNizszN Mmj6V2FPT0WU
RCC10RGB NWXyeFRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTmTmlKSzVyPUGwMlk3OSEQvF2= NVz5OpM4W0GQR1XS
KNS-42 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj2UZRKSzVyPUGxMlczPTVizszN MYnTRW5ITVJ?
LB771-HNC NE\2fXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\0VIhkUUN3ME2xNk4yPzF{IN88US=> MWPTRW5ITVJ?
SR MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnUTWM2OD1zMj6yNFY1KM7:TR?= M{LwOXNCVkeHUh?=
NCI-H1355 NXTUNnlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDvZZFjUUN3ME2xNk45QTh3IN88US=> NXXFWpBZW0GQR1XS
ES6 M3zKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DVWGlEPTB;MUOuNFc5KM7:TR?= MoftV2FPT0WU
SK-NEP-1 MnfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[5OlRrUUN3ME2xN{4zPTd5IN88US=> MnfTV2FPT0WU
D-392MG MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHQTWM2OD1zMz62OFI5KM7:TR?= MmDmV2FPT0WU
NB7 MkTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF2LkKzO|Qh|ryP M1\EPHNCVkeHUh?=
SK-LMS-1 NVH2fVRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF2LkWxOFUh|ryP NWfafm9OW0GQR1XS
SK-UT-1 NVLvVm4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF2Lke4PFkh|ryP MY\TRW5ITVJ?
CA46 NXPSPY86T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\BcmlEPTB;MUWuNFU5PiEQvF2= NHnGUo5USU6JRWK=
IST-SL2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDaTWM2OD1zNT6xPVAyKM7:TR?= NU\vSGM{W0GQR1XS
BC-1 MkPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnMR5JKSzVyPUG1MlM{OTRizszN NEmycZJUSU6JRWK=
LS-123 NEHqeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP6TWM2OD1zNT64NVc{KM7:TR?= M{PvVHNCVkeHUh?=
Ramos-2G6-4C10 NUTlZ2RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\uTWM2OD1zNj6wPVI1KM7:TR?= MULTRW5ITVJ?
MZ1-PC NGC2[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTFXYc4UUN3ME2xOk44OzF|IN88US=> M{LZeHNCVkeHUh?=
LB647-SCLC M2DqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW5eFVKSzVyPUG2Mlk{PzJizszN M3vDW3NCVkeHUh?=
NCI-H1694 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTF5LkG1Nlkh|ryP MWPTRW5ITVJ?
NCI-H322M MlLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljnTWM2OD1zNz60N|Y3KM7:TR?= NVrSXXhnW0GQR1XS
ES7 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH2TWM2OD1zOD6zPVE1KM7:TR?= M{\MNHNCVkeHUh?=
LC-2-ad NYjMSldjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTF6LkSzPFYh|ryP NXfRUo1WW0GQR1XS
SF268 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Pye2lEPTB;MUiuO|QxQSEQvF2= MmHlV2FPT0WU
RPMI-8402 MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzpU5RzUUN3ME2xPU4xPzR{IN88US=> NFT4[HFUSU6JRWK=
HCE-T NX7NTVRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJyLkKzOFQh|ryP NYrCcZI6W0GQR1XS
A101D MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTZU3NKSzVyPUKwMlg2QDdizszN MlW0V2FPT0WU
MRK-nu-1 M4TX[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXTTWM2OD1{MD65NVMh|ryP M3\CcnNCVkeHUh?=
LXF-289 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJzLkCzPEDPxE1? MY\TRW5ITVJ?
NALM-6 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zoc2lEPTB;MkGuNVk3PyEQvF2= M4jWbnNCVkeHUh?=
DOHH-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny3TWM2OD1{MT60PFE{KM7:TR?= NEOyT5BUSU6JRWK=
EW-16 NVrRPHJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJ{LkG0NFIh|ryP NFXHV3NUSU6JRWK=
A4-Fuk M4\ES2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnFcIFCUUN3ME2yNk4zOTR7IN88US=> MmPVV2FPT0WU
HD-MY-Z M1fC[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPzcFJKSzVyPUKyMlM6PjVizszN NUXN[W1jW0GQR1XS
SKM-1 M2nvPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDFWJVMUUN3ME2yNk44OzVzIN88US=> NXzmZ5lNW0GQR1XS
DMS-153 M1jpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH65e2pKSzVyPUKzMlQzODRizszN M{HOSXNCVkeHUh?=
LB373-MEL-D M1HFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTUclhNUUN3ME2yN{42PDV{IN88US=> NGjNXmZUSU6JRWK=
LP-1 Mn7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;qfmlEPTB;MkOuPFA6PyEQvF2= MXzTRW5ITVJ?
GI-ME-N M{fjOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYew[YdpUUN3ME2yOE4zQTJizszN M1nJOHNCVkeHUh?=
MPP-89 M2njfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT1N|h6UUN3ME2yOU4zODN4IN88US=> NW\FTIVkW0GQR1XS
U-698-M NHrBXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7D[|hKSzVyPUK1MlI2ODNizszN NUPoc5RRW0GQR1XS
HC-1 MnzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnSfY5WUUN3ME2yOU43PDF6IN88US=> MXPTRW5ITVJ?
HCC2157 M1H3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L3NGlEPTB;MkWuOlc{KM7:TR?= MWXTRW5ITVJ?
MOLT-4 M1WzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:wb2lEPTB;Mk[uNlc{KM7:TR?= MoOxV2FPT0WU
LS-411N NEOzXXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;mTWM2OD1{Nj6zN|Y6KM7:TR?= NYjHWldJW0GQR1XS
Becker NGf5S5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ4LkWxPFEh|ryP M1nzVHNCVkeHUh?=
NCI-H23 M1LEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr0TWM2OD1{Nj63OVc2KM7:TR?= NIn4WZlUSU6JRWK=
IST-SL1 M2naNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvlbplKSzVyPUK3MlM5PjdizszN MnHyV2FPT0WU
MZ2-MEL MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLGTWM2OD1{Nz60OVY3KM7:TR?= M2[1PXNCVkeHUh?=
RKO MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLvXJVXUUN3ME2yPE4yPDR4IN88US=> MYTTRW5ITVJ?
TE-441-T MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXBUYs2UUN3ME2yPE44QDlizszN NYLXdZNMW0GQR1XS
EW-24 M2O3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTJ7LkGyOVkh|ryP NGPSeWpUSU6JRWK=
no-10 M{GzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXENFI{UUN3ME2yPU4yPjNzIN88US=> NUS1NXJvW0GQR1XS
D-542MG NIP6TpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJ7LkmyNlEh|ryP M3ztV3NCVkeHUh?=
ST486 NF63[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrITWM2OD1|MD62OFUyKM7:TR?= MmHBV2FPT0WU
KURAMOCHI MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7QTWM2OD1|MD64NFU4KM7:TR?= NULGRldNW0GQR1XS
ES8 MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHmTWM2OD1|MT61PVczKM7:TR?= NXezU|RYW0GQR1XS
BL-41 NW\DSGJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzFZ4xKSzVyPUOyMlExPTRizszN NV;yWlNtW0GQR1XS
NB6 M1TtN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13lbGlEPTB;M{KuN|g2PSEQvF2= NVT4e4x3W0GQR1XS
NCI-H1304 NHfIZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3BWVZKSzVyPUOyMlQ6PjdizszN NGXWcFBUSU6JRWK=
MS-1 MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHqxeGpKSzVyPUOyMlc4PTFizszN M2\4WHNCVkeHUh?=
MFH-ino NYSwU4J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOwVJFOUUN3ME2zOE4{OjJ2IN88US=> M3i3[XNCVkeHUh?=
NOS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDjTGVCUUN3ME2zOE43PzR6IN88US=> NFnld3JUSU6JRWK=
HUTU-80 M2Lnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLFTWM2OD1|NT6zOlY4KM7:TR?= MlfUV2FPT0WU
EB2 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nyWmlEPTB;M{[uOlE5QSEQvF2= MUfTRW5ITVJ?
L-540 NYTSb4R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfFO3lKSzVyPUO3MlI{ODhizszN M2fRUnNCVkeHUh?=
NCI-H747 NGrLbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTN6Lki4OFYh|ryP NWXhSXk2W0GQR1XS
NCI-H446 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\xTWM2OD1|OT65OlUyKM7:TR?= NUTSSnhsW0GQR1XS
MOLT-16 Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR{LkSxOUDPxE1? NUixZ2FNW0GQR1XS
BC-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTR3LkS4PVYh|ryP MXLTRW5ITVJ?
SJSA-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUP1cm5PUUN3ME20OU42PDd2IN88US=> NE\YdndUSU6JRWK=
BB65-RCC NV3wfpNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjETYF4UUN3ME20OU43PjZizszN NIrIPVNUSU6JRWK=
SNB75 NYTpWIc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTR4LkCxPEDPxE1? NH3Qc|JUSU6JRWK=

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
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 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

相関EGFR製品

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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