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
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

文献中Selleckの製品使用例(63)

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 NUXZNJVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\oSZpOUUN3ME2wMlAzPTR2IN88US=> M3z2OXNCVkeHUh?=
HCC2218 MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMEWzNlYh|ryP Moq0V2FPT0WU
OCUB-M NI\idIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMEW3OEDPxE1? M4i4dXNCVkeHUh?=
ECC12 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmryTWM2OD1yLkC5NlMyKM7:TR?= NH3TeVVUSU6JRWK=
DSH1 MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS5fWY1UUN3ME2wMlA6Ozl4IN88US=> NFzwfVRUSU6JRWK=
BT-474 MlnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHntOFhKSzVyPUCuNlE{OTVizszN NVPQdZMyW0GQR1XS
BB30-HNC M1HtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrsTWM2OD1yLkK0OlU1KM7:TR?= M1GxW3NCVkeHUh?=
EKVX M4qweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT2c|J{UUN3ME2wMlQ1QDd2IN88US=> MljtV2FPT0WU
TE-12 M4WyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rOe2lEPTB;MD60PVA2PyEQvF2= NHLGTnZUSU6JRWK=
A388 M2K1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrwTWM2OD1yLkeyNlU5KM7:TR?= MUTTRW5ITVJ?
TE-9 NX;penl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:4TWM2OD1yLke0OFU{KM7:TR?= MmHmV2FPT0WU
LB2241-RCC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwMUW0NFMh|ryP MkXyV2FPT0WU
LB996-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrOXIdvUUN3ME2xMlM3OjJ6IN88US=> NYn3W5d5W0GQR1XS
LC-1F NUG2O2FlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwM{iyOFQh|ryP NXi4VXR1W0GQR1XS
TE-6 MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL3cXdKSzVyPUGuOVUzODFizszN M4fXOHNCVkeHUh?=
A253 NFz6NldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwOUezN|Uh|ryP M1jBTnNCVkeHUh?=
OS-RC-2 NIXPN|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwOUmxPVkh|ryP M4L2dHNCVkeHUh?=
TE-1 MkDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzGTZdCUUN3ME2yMlA1QDNizszN NYDRVnB5W0GQR1XS
RL95-2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;xPGg6UUN3ME2zMlE2PjdizszN MXHTRW5ITVJ?
LS-513 NXvEVYdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLmTWM2OD1|LkSwNFQyKM7:TR?= M{PJOHNCVkeHUh?=
DJM-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTNwNE[5O|Uh|ryP MYrTRW5ITVJ?
NMC-G1 NVLZ[lk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL2NJFKSzVyPUOuOVQ2ODFizszN NUO1THdIW0GQR1XS
TE-10 NEXRTFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG1Vpl[UUN3ME2zMlU2OzV4IN88US=> M4ixS3NCVkeHUh?=
TE-5 NYDLOph1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXhZpU4UUN3ME20MlA{PzNizszN MkPXV2FPT0WU
TK10 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTRwMU[1NlIh|ryP MWjTRW5ITVJ?
UACC-812 M1zRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[4R4xKSzVyPUSuOVYyPTNizszN NXHBXlZ5W0GQR1XS
SW962 NIDBZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvrTWM2OD13LkCyNVU6KM7:TR?= M2n3ZnNCVkeHUh?=
SW954 M17zemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD4TWM2OD13LkO5NlQ2KM7:TR?= NUH3fVVbW0GQR1XS
COLO-668 MnrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTVwN{K2Olch|ryP M1vHcHNCVkeHUh?=
LB1047-RCC NWC1cGIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDnO4dtUUN3ME21MlgxODR4IN88US=> M4[2THNCVkeHUh?=
NB5 NIXzUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPPTWM2OD14LkKxNFAyKM7:TR?= MkKwV2FPT0WU
NTERA-S-cl-D1 M{HxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHLdWptUUN3ME22MlI3PTZzIN88US=> NHz6VHBUSU6JRWK=
IST-MEL1 NIPwdoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDnRndKSzVyPU[uOFM3QTRizszN M3;FWHNCVkeHUh?=
GI-1 M17uT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zkdWlEPTB;Nj61NVY5OiEQvF2= NGrsSIZUSU6JRWK=
TGBC1TKB NYf2U|dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XLVWlEPTB;Nz6wO|E5OyEQvF2= MWTTRW5ITVJ?
GT3TKB NXHSbno4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjSRZlKSzVyPUeuNlI4PDRizszN NIHYVVZUSU6JRWK=
EVSA-T NIHCWXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TDdWlEPTB;Nz60NlgyOSEQvF2= NF3LTZZUSU6JRWK=
D-502MG M4nwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTdwNEi4PVQh|ryP MmDuV2FPT0WU
TE-8 NV6wSGZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2POOGlEPTB;Nz63OlE2QSEQvF2= M{C4WHNCVkeHUh?=
OVCAR-4 NHnFW3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPES2VpUUN3ME25MlEyPjd3IN88US=> Mo\JV2FPT0WU
D-336MG Mkf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTlwNEezPVUh|ryP MmjyV2FPT0WU
GCIY M37kW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL2SHZKSzVyPUmuOVc1OiEQvF2= M{PONXNCVkeHUh?=
KS-1 M{jyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTlwNk[yPFch|ryP MXvTRW5ITVJ?
HCC2998 MoP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\DTWM2OD17Lkm2N|A4KM7:TR?= NX6zZ2xCW0GQR1XS
D-247MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33KfmlEPTB;OT65PFI6OSEQvF2= MWXTRW5ITVJ?
TE-15 NX3QSmdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFyLkK0OUDPxE1? MYHTRW5ITVJ?
IST-MES1 MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17SfmlEPTB;MUCuNlU3PSEQvF2= MmjSV2FPT0WU
ETK-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Dod2lEPTB;MUCuOlI{KM7:TR?= NV[3NplxW0GQR1XS
RCC10RGB NH72bJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G0NWlEPTB;MUCuPVYyKM7:TR?= MlLCV2FPT0WU
KNS-42 M3m4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFzLkeyOVUh|ryP NHHuW2hUSU6JRWK=
LB771-HNC NX\NWGUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF{LkG3NVIh|ryP M2XnTXNCVkeHUh?=
SR NWHEUnMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF{LkKwOlQh|ryP MmHOV2FPT0WU
NCI-H1355 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXVTWM2OD1zMj64PVg2KM7:TR?= M2\GOnNCVkeHUh?=
ES6 NYX0UmZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vqbmlEPTB;MUOuNFc5KM7:TR?= NEG1[m1USU6JRWK=
SK-NEP-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF|LkK1O|ch|ryP Ml7JV2FPT0WU
D-392MG NX;YNnJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTF|Lk[0Nlgh|ryP NF7yO3dUSU6JRWK=
NB7 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfFR4ZKSzVyPUG0MlI{PzRizszN MWLTRW5ITVJ?
SK-LMS-1 M1LPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3MTWM2OD1zND61NVQ2KM7:TR?= NWniXmIyW0GQR1XS
SK-UT-1 NYHLVmVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfrTWM2OD1zND63PFg6KM7:TR?= MoO5V2FPT0WU
CA46 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzBUHlKSzVyPUG1MlA2QDZizszN Ml7JV2FPT0WU
IST-SL2 M1T1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF3LkG5NFEh|ryP Mln0V2FPT0WU
BC-1 M2L3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVntPZA3UUN3ME2xOU4{OzF2IN88US=> MmS4V2FPT0WU
LS-123 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1za[WlEPTB;MUWuPFE4OyEQvF2= NHPpS4dUSU6JRWK=
Ramos-2G6-4C10 Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfDOpF[UUN3ME2xOk4xQTJ2IN88US=> MV;TRW5ITVJ?
MZ1-PC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK2V|llUUN3ME2xOk44OzF|IN88US=> NVyyUFRrW0GQR1XS
LB647-SCLC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF4LkmzO|Ih|ryP NH\tVo1USU6JRWK=
NCI-H1694 M3f6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Xt[GlEPTB;MUeuNVUzQSEQvF2= M1fVTnNCVkeHUh?=
NCI-H322M MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF5LkSzOlYh|ryP M4T3b3NCVkeHUh?=
ES7 NUnPTodLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W1PWlEPTB;MUiuN|kyPCEQvF2= NGe1XGNUSU6JRWK=
LC-2-ad NFvERnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\mTmlEPTB;MUiuOFM5PiEQvF2= MX7TRW5ITVJ?
SF268 M3joWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvFTWM2OD1zOD63OFA6KM7:TR?= MUHTRW5ITVJ?
RPMI-8402 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHKTWM2OD1zOT6wO|QzKM7:TR?= MWLTRW5ITVJ?
HCE-T MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rmV2lEPTB;MkCuNlM1PCEQvF2= NVjI[WhGW0GQR1XS
A101D NF7r[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInsSFFKSzVyPUKwMlg2QDdizszN Mk\jV2FPT0WU
MRK-nu-1 NUW1fWo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;lclJrUUN3ME2yNE46OTNizszN M17PXXNCVkeHUh?=
LXF-289 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJzLkCzPEDPxE1? NUXOfFlOW0GQR1XS
NALM-6 NITDOY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TPb2lEPTB;MkGuNVk3PyEQvF2= NGjSZVNUSU6JRWK=
DOHH-2 NGDXVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L6[WlEPTB;MkGuOFgyOyEQvF2= MWTTRW5ITVJ?
EW-16 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X0[WlEPTB;MkKuNVQxOiEQvF2= MX3TRW5ITVJ?
A4-Fuk M2rGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHSeYhKSzVyPUKyMlIyPDlizszN NXm5b4NpW0GQR1XS
HD-MY-Z MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fieGlEPTB;MkKuN|k3PSEQvF2= MWLTRW5ITVJ?
SKM-1 NVH0e5NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr4dYRzUUN3ME2yNk44OzVzIN88US=> NX7me4N4W0GQR1XS
DMS-153 NWr6T5JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13hW2lEPTB;MkOuOFIxPCEQvF2= NYLhdmhXW0GQR1XS
LB373-MEL-D NH[zN4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G1W2lEPTB;MkOuOVQ2OiEQvF2= MY\TRW5ITVJ?
LP-1 NEDyNGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ|LkiwPVch|ryP M1\2S3NCVkeHUh?=
GI-ME-N NWL3eHF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJ2LkK5NkDPxE1? NHvqO2xUSU6JRWK=
MPP-89 M17Qfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T6eWlEPTB;MkWuNlA{PiEQvF2= MVLTRW5ITVJ?
U-698-M MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEixXmdKSzVyPUK1MlI2ODNizszN NXTHU|l[W0GQR1XS
HC-1 M1rUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPBTlNKSzVyPUK1MlY1OThizszN M3\jSHNCVkeHUh?=
HCC2157 MkPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljqTWM2OD1{NT62O|Mh|ryP M4DscHNCVkeHUh?=
MOLT-4 NW\EUohVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjMU|l7UUN3ME2yOk4zPzNizszN MX3TRW5ITVJ?
LS-411N NFfpXlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHvWndUUUN3ME2yOk4{OzZ7IN88US=> M2K2[nNCVkeHUh?=
Becker MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH6xepVKSzVyPUK2MlUyQDFizszN MlmyV2FPT0WU
NCI-H23 Mne2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3flWmlEPTB;Mk[uO|U4PSEQvF2= NIHGfGZUSU6JRWK=
IST-SL1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PDSGlEPTB;MkeuN|g3PyEQvF2= M3T5enNCVkeHUh?=
MZ2-MEL M3fEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjGb4NDUUN3ME2yO{41PTZ4IN88US=> M17xdHNCVkeHUh?=
RKO M3PBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ziPWlEPTB;MkiuNVQ1PiEQvF2= NWrEfYpQW0GQR1XS
TE-441-T NFLJbplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ6Lke4PUDPxE1? NIS0WGZUSU6JRWK=
EW-24 NV7KW2dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJ7LkGyOVkh|ryP MVHTRW5ITVJ?
no-10 NYDMenp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TXO2lEPTB;MkmuNVY{OSEQvF2= MkPxV2FPT0WU
D-542MG NWLkWWUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3D[5NUUUN3ME2yPU46OjJzIN88US=> M1jFRnNCVkeHUh?=
ST486 NWjSdGRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fCZWlEPTB;M{CuOlQ2OSEQvF2= MWTTRW5ITVJ?
KURAMOCHI MmHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEj3TJNKSzVyPUOwMlgxPTdizszN MX\TRW5ITVJ?
ES8 MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XxTmlEPTB;M{GuOVk4OiEQvF2= MnfaV2FPT0WU
BL-41 NWnLZYpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfHPIFKSzVyPUOyMlExPTRizszN NH25PZNUSU6JRWK=
NB6 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLVTWM2OD1|Mj6zPFU2KM7:TR?= NXHaeGhpW0GQR1XS
NCI-H1304 NFfFOpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIntdJdKSzVyPUOyMlQ6PjdizszN NFzDSllUSU6JRWK=
MS-1 NIfVWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH6TWM2OD1|Mj63O|UyKM7:TR?= MXfTRW5ITVJ?
MFH-ino MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jqOWlEPTB;M{SuN|IzPCEQvF2= NHTmb4lUSU6JRWK=
NOS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH2ySnBKSzVyPUO0MlY4PDhizszN NXHue2lNW0GQR1XS
HUTU-80 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTN3LkO2Olch|ryP MUfTRW5ITVJ?
EB2 NHjqfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTN4Lk[xPFkh|ryP M1vje3NCVkeHUh?=
L-540 NV20UHNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTN5LkKzNFgh|ryP NFfNVnhUSU6JRWK=
NCI-H747 NF6zbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnKU4NvUUN3ME2zPE45QDR4IN88US=> NYLOcpBEW0GQR1XS
NCI-H446 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHmTWM2OD1|OT65OlUyKM7:TR?= NWrsVmJsW0GQR1XS
MOLT-16 M{nid2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTR{LkSxOUDPxE1? MoTlV2FPT0WU
BC-3 M{\Rdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TjWGlEPTB;NEWuOFg6PiEQvF2= M2PObXNCVkeHUh?=
SJSA-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\5emlEPTB;NEWuOVQ4PCEQvF2= NGraPXVUSU6JRWK=
BB65-RCC NXzndZN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR3Lk[2OkDPxE1? M16zVXNCVkeHUh?=
SNB75 M2\4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR4LkCxPEDPxE1? MlPSV2FPT0WU

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

アッセイ
Methods Test Index PMID
Western blot
ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; 

PubMed: 29799521     


Downregulation of HSF1, mutp53, and Mdm2 in lapatinib-sensitive parental BT474, but not in lapatinib-resistant BT474R cells, treated with indicated lapatinib concentrations for 24 h.

pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP ; 

PubMed: 28938602     


SKBR3 and 78617 cells were treated with lapatinib as in panel A, then the expression of phospho-ErbB2 (Tyr1221/1222), ErbB2, phospho-EGFR (Tyr1068), EGFR, phospho-Akt (Ser473), Akt, phospho-Erk1/2 (Thr202/Tyr204), Erk2, phospho-mTOR (Ser2448), and mTOR were analyzed using Western blotting. 

p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1; 

PubMed: 22853430     


A panel of HER2-amplified breast cancer cells were treated with 200nM lapatinib for up to 72 hours to detect the initial downregulation and subsequent upregulation of HER2-HER3 and downstream signaling. Immunoblots were performed using the indicated antibodies.

29799521 28938602 22853430
Immunofluorescence
LC3 ; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 6 days and UACC893 GFP-LC3 cells were cultured for 7 days with 5 μM EZN3046 or EZN4150 .

Vimentin / E-cadherin; 

PubMed: 28243326     


Cells treated with lapatinib (5µM) increased the expression of E-cadherin and inhibited the expression of Vimentin by immunofluorescence. (Magnification: 1000×).

26637440 28243326
Growth inhibition assay
Cell viability (OE19); 

PubMed: 25350844     


Dose-response curves from escalated dose of lapatinib in the presence of 1 µM concentration of saracatinib. The calculated values of IC50 for lapatinib were following; 207.3 nM and 145 nM, respectively, after lapatinib alone and in the presence of saracatinib for parental OE19; >1,000 nM after lapatinib alone for LR2A and LR2B; 91.66 nM and 224.0 nM in the presence of saracatinib in LR2A and LR2B, respectively. Values were presented as relative cellular viability relative to vehicle-treated controls with the mean ± S.E. of quadruplicate from a representative experiment. The p values calculated by two-way ANOVA were <0.0001 comparing lapatinib alone with lapatinib plus saracatinib both in the LR2A and LR2B.

Cell viability (A431 cells); 

PubMed: 28243326     


The MTT assay was performed on the viability of A431 cells by lapatinib at different concentrations (0.1-50μM) and IC50 value was analyzed as indicated on the plot (t-test).

25350844 28243326
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
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID