Lapatinib

For research use only. Not for use in humans.

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) 在庫  
10mM (1mL in DMSO) JPY 25700 あり
JPY 20200 あり
JPY 46800 あり
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(315)

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 NH;uRnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7MTWM2OD1yLkCyOVQ1KM7:TR?= MoeyV2FPT0WU
HCC2218 NYDiTG5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TrZ2lEPTB;MD6wOVMzPiEQvF2= NE[1N4hUSU6JRWK=
OCUB-M NHXFdohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XGS2lEPTB;MD6wOVc1KM7:TR?= MUjTRW5ITVJ?
ECC12 M2nWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwMEmyN|Eh|ryP MXjTRW5ITVJ?
DSH1 NFXBb3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrlSlBKSzVyPUCuNFk{QTZizszN MWjTRW5ITVJ?
BT-474 NWrNS5FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHlTWM2OD1yLkKxN|E2KM7:TR?= M{HKWnNCVkeHUh?=
BB30-HNC M{PkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjiXHBDUUN3ME2wMlI1PjV2IN88US=> NX:1SZlUW0GQR1XS
EKVX M4ezTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEf2OodKSzVyPUCuOFQ5PzRizszN M2DP[nNCVkeHUh?=
TE-12 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Lp[2lEPTB;MD60PVA2PyEQvF2= NFrtPFFUSU6JRWK=
A388 NYLa[49GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fSe2lEPTB;MD63NlI2QCEQvF2= MnXZV2FPT0WU
TE-9 M4TieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwN{S0OVMh|ryP M{\2OnNCVkeHUh?=
LB2241-RCC MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH2NFlKSzVyPUGuNVU1ODNizszN MlvkV2FPT0WU
LB996-RCC NWWxOYJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGn3XJZKSzVyPUGuN|YzOjhizszN NV20cHRsW0GQR1XS
LC-1F NYLWbXl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHU[4JtUUN3ME2xMlM5OjR2IN88US=> M{PKT3NCVkeHUh?=
TE-6 NFPEclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYWwcHlJUUN3ME2xMlU2OjBzIN88US=> NUnkVHpqW0GQR1XS
A253 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnVTWM2OD1zLkm3N|M2KM7:TR?= NHrwTXlUSU6JRWK=
OS-RC-2 NF3RdVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjEZlM2UUN3ME2xMlk6OTl7IN88US=> NUXTeWRlW0GQR1XS
TE-1 NHPxRm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHiU|VKSzVyPUKuNFQ5OyEQvF2= NUnBR5BwW0GQR1XS
RL95-2 NV7QfI5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLsVGNKSzVyPUOuNVU3PyEQvF2= M17ub3NCVkeHUh?=
LS-513 MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNwNECwOFEh|ryP M2TX[3NCVkeHUh?=
DJM-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjaeoRKSzVyPUOuOFY6PzVizszN MknKV2FPT0WU
NMC-G1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTNwNUS1NFEh|ryP MVHTRW5ITVJ?
TE-10 Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjPTWM2OD1|LkW1N|U3KM7:TR?= NX35VlYxW0GQR1XS
TE-5 NXzUfHNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTRwMEO3N{DPxE1? Mmf1V2FPT0WU
TK10 NWHWSYNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\uRmlEPTB;ND6xOlUzOiEQvF2= MYjTRW5ITVJ?
UACC-812 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW0TWM2OD12LkW2NVU{KM7:TR?= NUmzZlFvW0GQR1XS
SW962 NWPjeGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknwTWM2OD13LkCyNVU6KM7:TR?= MWPTRW5ITVJ?
SW954 MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTVwM{myOFUh|ryP M4XrUHNCVkeHUh?=
COLO-668 M4jibGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjBTWM2OD13LkeyOlY4KM7:TR?= M2nqOHNCVkeHUh?=
LB1047-RCC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTVwOECwOFYh|ryP NXTHXHVyW0GQR1XS
NB5 NWS0ZWNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfJV2hKSzVyPU[uNlExODFizszN MXnTRW5ITVJ?
NTERA-S-cl-D1 Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPRXGN5UUN3ME22MlI3PTZzIN88US=> MUTTRW5ITVJ?
IST-MEL1 NH\0NHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fMS2lEPTB;Nj60N|Y6PCEQvF2= Mn;KV2FPT0WU
GI-1 NYr0Z2JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTZwNUG2PFIh|ryP NUDQe482W0GQR1XS
TGBC1TKB Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTdwMEexPFMh|ryP MYXTRW5ITVJ?
GT3TKB NGm4NGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jrcmlEPTB;Nz6yNlc1PCEQvF2= NYL6[GdxW0GQR1XS
EVSA-T MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\pPJZ1UUN3ME23MlQzQDFzIN88US=> MV\TRW5ITVJ?
D-502MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnBTWM2OD15LkS4PFk1KM7:TR?= NHH1W5ZUSU6JRWK=
TE-8 NYjtVI9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zpSmlEPTB;Nz63OlE2QSEQvF2= MlvGV2FPT0WU
OVCAR-4 MoPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTlwMUG2O|Uh|ryP MUfTRW5ITVJ?
D-336MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXEd4RKSzVyPUmuOFc{QTVizszN MoH5V2FPT0WU
GCIY NFPlOHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DhPGlEPTB;OT61O|QzKM7:TR?= Mlr2V2FPT0WU
KS-1 M4\SXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:1d4JKSzVyPUmuOlYzQDdizszN MnvRV2FPT0WU
HCC2998 NYnxU2lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTlwOU[zNFch|ryP NV;Bco9TW0GQR1XS
D-247MG MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrkTWM2OD17Lkm4NlkyKM7:TR?= M4HLSXNCVkeHUh?=
TE-15 NXTI[ZNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvXXox5UUN3ME2xNE4zPDVizszN NH\TenlUSU6JRWK=
IST-MES1 NEX2fVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\EN5dKSzVyPUGwMlI2PjVizszN MVjTRW5ITVJ?
ETK-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17ZXWlEPTB;MUCuOlI{KM7:TR?= MV3TRW5ITVJ?
RCC10RGB NWG1WJhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W5Z2lEPTB;MUCuPVYyKM7:TR?= MmTPV2FPT0WU
KNS-42 M4[3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;HTWM2OD1zMT63NlU2KM7:TR?= MmfDV2FPT0WU
LB771-HNC MnXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHVTWM2OD1zMj6xO|EzKM7:TR?= MXvTRW5ITVJ?
SR NIj3TXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3zTWM2OD1zMj6yNFY1KM7:TR?= NUjDZYpjW0GQR1XS
NCI-H1355 Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHVU3JoUUN3ME2xNk45QTh3IN88US=> NGHQVFJUSU6JRWK=
ES6 NF20dG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j0[WlEPTB;MUOuNFc5KM7:TR?= MW\TRW5ITVJ?
SK-NEP-1 NF6zfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D3VGlEPTB;MUOuNlU4PyEQvF2= M{nqd3NCVkeHUh?=
D-392MG NXT5R5h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPrTWM2OD1zMz62OFI5KM7:TR?= NGDMR5dUSU6JRWK=
NB7 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF2LkKzO|Qh|ryP MYnTRW5ITVJ?
SK-LMS-1 MomwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTF2LkWxOFUh|ryP NFHrNo9USU6JRWK=
SK-UT-1 NGXTTWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nzRmlEPTB;MUSuO|g5QSEQvF2= NYfSb3lYW0GQR1XS
CA46 MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nIdWlEPTB;MUWuNFU5PiEQvF2= NV\oU3NZW0GQR1XS
IST-SL2 MkPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX32SXh2UUN3ME2xOU4yQTBzIN88US=> MUTTRW5ITVJ?
BC-1 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m3W2lEPTB;MUWuN|MyPCEQvF2= NHPKXJRUSU6JRWK=
LS-123 NX:xT4VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrjTWM2OD1zNT64NVc{KM7:TR?= NVG4dpJpW0GQR1XS
Ramos-2G6-4C10 M3zPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUSyWGo3UUN3ME2xOk4xQTJ2IN88US=> M1;LPXNCVkeHUh?=
MZ1-PC M{Xqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfqWJdKSzVyPUG2Mlc{OTNizszN MYPTRW5ITVJ?
LB647-SCLC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF4LkmzO|Ih|ryP NIjCUoVUSU6JRWK=
NCI-H1694 NEnRcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LoSWlEPTB;MUeuNVUzQSEQvF2= NEPMdppUSU6JRWK=
NCI-H322M M3LKUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDZUWdKSzVyPUG3MlQ{PjZizszN M4K3XHNCVkeHUh?=
ES7 NGDCN3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTF6LkO5NVQh|ryP MnHzV2FPT0WU
LC-2-ad NYnLOI5IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnwPJhKSzVyPUG4MlQ{QDZizszN M4\PPXNCVkeHUh?=
SF268 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrRNolKSzVyPUG4Mlc1ODlizszN M1flb3NCVkeHUh?=
RPMI-8402 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17E[mlEPTB;MUmuNFc1OiEQvF2= M2PBXnNCVkeHUh?=
HCE-T NG\0PJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXnTWM2OD1{MD6yN|Q1KM7:TR?= NE\XTHhUSU6JRWK=
A101D MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPhTXczUUN3ME2yNE45PTh5IN88US=> NXvhNpNuW0GQR1XS
MRK-nu-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJyLkmxN{DPxE1? NVXXSYFDW0GQR1XS
LXF-289 NF7PcpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJzLkCzPEDPxE1? M3TxU3NCVkeHUh?=
NALM-6 NH32fJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJzLkG5Olch|ryP MU\TRW5ITVJ?
DOHH-2 NV3mS5ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELk[ohKSzVyPUKxMlQ5OTNizszN Mln6V2FPT0WU
EW-16 NYTNbWN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nUTGlEPTB;MkKuNVQxOiEQvF2= NF;O[49USU6JRWK=
A4-Fuk MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf2VnJNUUN3ME2yNk4zOTR7IN88US=> MnriV2FPT0WU
HD-MY-Z NI\5UppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrVTWM2OD1{Mj6zPVY2KM7:TR?= Mnz6V2FPT0WU
SKM-1 NVjqO29vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TkfmlEPTB;MkKuO|M2OSEQvF2= M4LmcHNCVkeHUh?=
DMS-153 NH;ZSHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37xPGlEPTB;MkOuOFIxPCEQvF2= M4fEN3NCVkeHUh?=
LB373-MEL-D Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7jeoVxUUN3ME2yN{42PDV{IN88US=> MnHxV2FPT0WU
LP-1 M17EO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFKwVGpKSzVyPUKzMlgxQTdizszN NHL2NI9USU6JRWK=
GI-ME-N NGrpW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknxTWM2OD1{ND6yPVIh|ryP NX3yeXV4W0GQR1XS
MPP-89 NUfQRW1ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3sW2NSUUN3ME2yOU4zODN4IN88US=> NWDwUlBYW0GQR1XS
U-698-M MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13KfWlEPTB;MkWuNlUxOyEQvF2= NU\McHRmW0GQR1XS
HC-1 M4Hke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHmS5FoUUN3ME2yOU43PDF6IN88US=> Ml3BV2FPT0WU
HCC2157 M3vpW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn5TlVKSzVyPUK1MlY4OyEQvF2= MVXTRW5ITVJ?
MOLT-4 NWHpNG9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:2eJI1UUN3ME2yOk4zPzNizszN NUDnS2xUW0GQR1XS
LS-411N NYfTVXh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zpfGlEPTB;Mk[uN|M3QSEQvF2= Mo\6V2FPT0WU
Becker M2\EeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr5ZXR3UUN3ME2yOk42OThzIN88US=> M4HFTHNCVkeHUh?=
NCI-H23 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvEV|Y2UUN3ME2yOk44PTd3IN88US=> M376UHNCVkeHUh?=
IST-SL1 M2\6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvRTWM2OD1{Nz6zPFY4KM7:TR?= NUDyWWRrW0GQR1XS
MZ2-MEL NXTvZ4MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITrWmdKSzVyPUK3MlQ2PjZizszN MoTZV2FPT0WU
RKO NUjrN2xvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDSVohKSzVyPUK4MlE1PDZizszN M2nQSHNCVkeHUh?=
TE-441-T NWj0OVk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfmTWM2OD1{OD63PFkh|ryP NF7GXoxUSU6JRWK=
EW-24 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7n[YFFUUN3ME2yPU4yOjV7IN88US=> MWnTRW5ITVJ?
no-10 NGDuflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJ7LkG2N|Eh|ryP NWC0dYxjW0GQR1XS
D-542MG NGrCPYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\1TWM2OD1{OT65NlIyKM7:TR?= NYnzbYRxW0GQR1XS
ST486 NWS5[lUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO2dYVQUUN3ME2zNE43PDVzIN88US=> NGHrcIhUSU6JRWK=
KURAMOCHI MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXzV|E{UUN3ME2zNE45ODV5IN88US=> MYLTRW5ITVJ?
ES8 MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTNzLkW5O|Ih|ryP MYPTRW5ITVJ?
BL-41 M2r4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3qTWM2OD1|Mj6xNFU1KM7:TR?= NVLEXndYW0GQR1XS
NB6 NVXheZYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULl[JNEUUN3ME2zNk4{QDV3IN88US=> MXzTRW5ITVJ?
NCI-H1304 NVKzWXBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjm[nRKSzVyPUOyMlQ6PjdizszN MUTTRW5ITVJ?
MS-1 NHjlbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\jZYZKSzVyPUOyMlc4PTFizszN MXPTRW5ITVJ?
MFH-ino MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TzbmlEPTB;M{SuN|IzPCEQvF2= NVTFW2Z6W0GQR1XS
NOS-1 NETXSoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPmTWM2OD1|ND62O|Q5KM7:TR?= NHj4TlVUSU6JRWK=
HUTU-80 Mkf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTN3LkO2Olch|ryP MY\TRW5ITVJ?
EB2 NY\FXYY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN4Lk[xPFkh|ryP M4XKV3NCVkeHUh?=
L-540 NIfoUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDFTWM2OD1|Nz6yN|A5KM7:TR?= NVnzO5ZEW0GQR1XS
NCI-H747 MkLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTN6Lki4OFYh|ryP NXfSeYJoW0GQR1XS
NCI-H446 MmTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv0V|Z{UUN3ME2zPU46PjVzIN88US=> MVrTRW5ITVJ?
MOLT-16 MoroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7uVZBKSzVyPUSyMlQyPSEQvF2= MmH1V2FPT0WU
BC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TTbWlEPTB;NEWuOFg6PiEQvF2= NHqyTWtUSU6JRWK=
SJSA-1 M2e5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTR3LkW0O|Qh|ryP NWnlW|JxW0GQR1XS
BB65-RCC MofXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H2XmlEPTB;NEWuOlY3KM7:TR?= Ml;hV2FPT0WU
SNB75 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR4LkCxPEDPxE1? MV\TRW5ITVJ?

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]
- 合併

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]
- 合併
  • 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]
- 合併
  • 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
  • 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
Smiles C[S](=O)(=O)CCNCC1=CC=C(O1)C2=CC=C3N=CN=C(NC4=CC=C(OCC5=CC=CC(=C5)F)C(=C4)Cl)C3=C2

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(余分な消耗を考慮し動物一匹分の量を用意することをお勧めします。)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロットごとに組成が異なるため、セレックから完全に溶解できる組成をお求めください。)
% DMSO % % Tween 80 % ddH2O
計算リセット

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 (mg) = 濃度 (mM) x 体積 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03075995 Unknown status Other: hight-fat breakfast Breast Cancer Sun Yat-sen University April 12 2017 Not Applicable
NCT02338245 Completed Drug: ASLAN001|Drug: Lapatinib|Drug: Capecitabine Metastatic Breast Cancer Aslan Pharmaceuticals December 29 2014 Phase 2
NCT02294786 Terminated Drug: Lapatinib|Drug: Capecitabine|Drug: Octreotide Cancer Novartis Pharmaceuticals|Novartis December 17 2014 Phase 2
NCT02213042 Completed Drug: Lapatinib|Biological: Trastuzumab Neoplasms Breast Novartis Pharmaceuticals|Novartis October 24 2014 Phase 2
NCT01782651 Completed Drug: Lapatinib plus capecitabine Neoplasms Breast GlaxoSmithKline August 2014 --
NCT02158507 Active not recruiting Drug: Combination of Veliparib + Lapatinib Metastatic Triple Negative Breast Cancer University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie July 2014 Not Applicable

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