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.

サイズ 価格(税別)  
JPY 31722.00
JPY 24402.00
JPY 66400.00

文献中Selleckの製品使用例(54)

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 NV7lSIc{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxtKGyrbnWsJGlEPTB;MD6wNlUh|ryP NYnCXZpxOTZ2OEO3O|I>
BT474 cell line Mk\oVJJwdGmoZYLheIlwdiCjc4PhfS=> NF;ISYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> MW[xOlQ5Ozd5Mh?=
HN5 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlm3TY5pcWKrdHnvckBw\iCKTkWgZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKg{txO NFLlV4oyPjd5N{SxNC=>
BT474 cell M4HzeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DyNGlvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP M2HrR|E3Pzd5NEGw
N87 cell NYK3WnRST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKE56NzDj[YxtKGe{b4f0bEBi\nSncjC3NkBpenNuIFnDOVA:OC5yODFOwG0> MmS5NVY4Pzd2MUC=
HFF cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVzrTJFVUW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> MofPNVY4Pzd2MUC=
SKBR3 cells MYHDfZRwfG:6aXPpeJkh[XO|YYm= NXrt[oFES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzNzFOwG0> NI\zSVgyQTB{OESyOS=>
A431 cells M4[xeGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mm\3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVA1KM7:TR?= NX7PO4RHOTl6OEi3OlE>
SKBR3 cells M{TD[mN6fG:2b4jpZ4l1gSCjc4PhfS=> MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFI6KM7:TR?= MkLUNVk5QDh5NkG=
HepG2 cells NGf0[pFRem:uaX\ldoF1cW:wIHHzd4F6 M{jV[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVYvOjdizszN NVzGfnVxOjBzNEO3O|g>
Hep3B2 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NW\LOlFySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZA{SjJiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwNEmg{txO MlzWNlAyPDN5N{i=
SKHEP1 cells MmTaVJJwdGmoZYLheIlwdiCjc4PhfS=> MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONSFXQNUBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU4{KM7:TR?= NXXDd3JNOjBzNEO3O|g>
MCF7 cells Mo\WVJJwdGmoZYLheIlwdiCjc4PhfS=> M3n2R2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok43KM7:TR?= NWe2ZXZ6OjBzNEO3O|g>
MDA-MB-231 cells M{fyVXBzd2yrZnXyZZRqd25iYYPzZZk> NVfMPGp5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME21MlQh|ryP MlXFNlAyPDN5N{i=
SK-BR-3 cells NV;hdolKWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHm5emVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMWJTNTNiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTBwMESg{txO NWDzWXJxOjBzNEO3O|g>
A431 cells NHixVVJHfW6ldHnvckBie3OjeR?= M4rLc2lvcGmkaYTpc44hd2ZiRVfGVkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDNEOxJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMEWyJO69VQ>? M1fu[|IxOzR4NkW1
N87 cells NWTGO2lmTnWwY4Tpc44h[XO|YYm= NV7QUlJsUW6qaXLpeIlwdiCxZjDFdoJDOiCrboTyZYNmdGy3bHHyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOPFch[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6xJO69VQ>? M1e1SlIxOzR4NkW1
MIAPaCa cells M4H3dmZ2dmO2aX;uJIF{e2G7 NFvHdVlKdmirYnn0bY9vKG:oIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC52M{Og{txO NYD2bGl6OjB6MUe1NlM>
MIAPaCa cells MV7GeY5kfGmxbjDhd5NigQ>? MofOTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> NEe4fIozODhzN{WyNy=>
CAL27 cells M3nkR2N6fG:2b4jpZ4l1gSCjc4PhfS=> MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDRWwzPyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFS2ZTKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA4KM7:TT6= M3X1VlIyODhyNkK5
SKOV3 cells NFvEO49EgXSxdH;4bYNqfHliYYPzZZk> NFewXJpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJTVJ{IHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB|IN88UU4> NHniPG0zOTB6ME[yPS=>
CAL27 cells NVz1UFJITnWwY4Tpc44h[XO|YYm= MWCxOkBp M2HBcWlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgSWdHWiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hS0GOMkegZ4VtdHNib4\ldoV5eHKnc4PpcochTUeIUjDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0MEBKSzVyPUCuNFMzKM7:TR?= MnTGNlExQDB4Mkm=
SK-BR-3 cells NV7wU4c4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHT5T3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVz[kJ{IH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJHNMNUKULUOgZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFMzKM7:TR?= Mk\oNlE2PzB6NEO=
BXF T24 cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= NHu5NJM1KGSjeYO= NEfRSmREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDYEZiVEK0JINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF06NjZ3IN88US=> NEThZmczOjF4OU[wNS=>
CXF 269L cells NH;MWHBEgXSxdH;4bYNqfHliYYPzZZk> NHTMcYw1KGSjeYO= MmfXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR3hHKDJ4OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVgvOzZizszN MmfiNlIyPjl4MEG=
DIFI cells MnHCR5l1d3SxeHnjbZR6KGG|c3H5 NFvrSm01KGSjeYO= M3z6bmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= NGCzSoczOjF4OU[wNS=>
HT-29 cells NVHHT5BXS3m2b4TvfIlkcXS7IHHzd4F6 M{PVdlQh\GG7cx?= M365VGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20MlYzKM7:TR?= NWrkSmpVOjJzNkm2NFE>
RKO cells MWjDfZRwfG:6aXPpeJkh[XO|YYm= MmDyOEBl[Xm| M1KyWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJMVyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;NT6zOUDPxE1? M1TE[|IzOTZ7NkCx
GXF251L cells NGnnXFNEgXSxdH;4bYNqfHliYYPzZZk> MUm0JIRigXN? NEDxb2NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIYEZ{NUHMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0yNjR6IN88US=> MoHFNlIyPjl4MEG=
LIXF 575L cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= NYnhWYtYPCCmYYnz NIK3b3JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNUViIIEW3OWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwMUig{txO Mn;oNlIyPjl4MEG=
LXFA 289L cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= MXS0JIRigXN? MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZCKDJ6OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVUvPzlizszN NYfVXo1mOjJzNkm2NFE>
LXFA 526L MnvZR5l1d3SxeHnjbZR6KGG|c3H5 NEDQfoo1KGSjeYO= NYqwfGlIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiIQTC1NlZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkKxJO69VQ>? M1v1WlIzOTZ7NkCx
LXFA 629L cells NGHHOo1EgXSxdH;4bYNqfHliYYPzZZk> NGDrVZQ1KGSjeYO= NGPsUpFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIE[yPWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTJwOEeg{txO Mn61NlIyPjl4MEG=
LXFL 1121L cells NFXMVHREgXSxdH;4bYNqfHliYYPzZZk> NYfHSWVRPCCmYYnz NWTufIxVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVFiITDCxNVIyVCClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Nz63N{DPxE1? NGLRXoQzOjF4OU[wNS=>
LXFL 529L cells NUjCOJhGS3m2b4TvfIlkcXS7IHHzd4F6 NEHWOVE1KGSjeYO= MlroR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHVCB3MknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjVzIN88US=> M2HWVlIzOTZ7NkCx
MCF7 cells NV;HTZF4S3m2b4TvfIlkcXS7IHHzd4F6 NWDmTo97PCCmYYnz MnP2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;ND64N{DPxE1? MUCyNlE3QTZyMR?=
MDA231 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= NGHtcmU1KGSjeYO= NIXpeWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF{M{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvPyEQvF2= MXyyNlE3QTZyMR?=
OVXF 899L NHTQU5hEgXSxdH;4bYNqfHliYYPzZZk> NH3meGo1KGSjeYO= MmO2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZZTiB6OUnMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0{NjN3IN88US=> NEXlSoQzOjF4OU[wNS=>
PAXF 546L cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= MVW0JIRigXN? NWCxToQzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEG[RjC1OFZNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD14LkGyJO69VQ>? NFLHdlEzOjF4OU[wNS=>
PANC1 cells NEfOSZlEgXSxdH;4bYNqfHliYYPzZZk> NUW5VoJKPCCmYYnz M1XoVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME24MlEzKM7:TR?= M1\3ZlIzOTZ7NkCx
22Rv1 cell M{LjTGN6fG:2b4jpZ4l1gSCjc4PhfS=> NXXBcpdFPCCmYYnz Mn;2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNlJTfjFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPU[uNFYh|ryP MmfoNlIyPjl4MEG=
DU145 cells NFr0dZVEgXSxdH;4bYNqfHliYYPzZZk> M1XFZVQh\GG7cx?= MlvoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUKuPVkh|ryP MlO4NlIyPjl4MEG=
LNCAP cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= NUnGS2ZPPCCmYYnz NWjIToh5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN M1vYe|IzOTZ7NkCx
PC3M cells M13qcmN6fG:2b4jpZ4l1gSCjc4PhfS=> M{K0PVQh\GG7cx?= MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|NOKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD12LkW1JO69VQ>? NGfubmQzOjF4OU[wNS=>
NIH/3T3 cells M2T1XnBzd2yrZnXyZZRqd25iYYPzZZk> MlH1O|IhcA>? MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12LkOg{txO MlX0NlI2QTVzN{e=
NCI-H1648 cell M{HtXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXm4NJR3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCyOVQ1KM7:TR?= M13uS3NCVkeHUh?=
NMC-G1 cell NW\KcppbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIW0SnNKdmirYnn0bY9vKG:oIHj1cYFvKE6PQz3HNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTR3MEGg{txO M132SnNCVkeHUh?=
NTERA-S-cl-D1 cell NFm0cpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTD[o5FUW6qaXLpeIlwdiCxZjDoeY1idiCQVFXSRU1UNWOuLVSxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPjV4MTFOwG0> NHzYdVNUSU6JRWK=
OCUB-M cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFO1dmRKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODV5NDFOwG0> MUTTRW5ITVJ?
OS-RC-2 cell M4rEN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWC1WGd6UW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57OUG5PUDPxE1? NUfkcm1TW0GQR1XS
OVCAR-4 cell M2Owe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIjHOmpKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjFzNke1JO69VQ>? M2fSOnNCVkeHUh?=
RL95-2 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfVTY5pcWKrdHnvckBw\iCqdX3hckBTVDl3LUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2PjdizszN NFXobmdUSU6JRWK=
SW954 cell M2S2NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= NFHpelFUSU6JRWK=
SW962 cell MmHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3e5bGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6OjR3IN88US=> MYDTRW5ITVJ?
TE-1 cell NYHQdopDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkCyNVU6KM7:TR?= M1\ZfHNCVkeHUh?=
A253 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LTPWlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ3MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFQ5OyEQvF2= MYnTRW5ITVJ?
A388 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX\DcVdoUW6qaXLpeIlwdiCxZjDoeY1idiCDM{i4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPDh|IN88US=> MX7TRW5ITVJ?
BB30-HNC cell MlflS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGJDOzBvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PzN|NTFOwG0> NFTiR4FUSU6JRWK=
TE-12 cell MnuwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLORW9KdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjJ3ODFOwG0> NX:zU3MyW0GQR1XS
TE-5 cell NG[xVHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= NEjaZ3pUSU6JRWK=
TE-6 cell NIP2SY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfhTY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVA2PyEQvF2= NEfuTlVUSU6JRWK=
TE-8 cell NYn6eYwzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2Tj[mlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNFM4OyEQvF2= MmHoV2FPT0WU
TE-9 cell NVLJWZJYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH\ze2lKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU2OjBzIN88US=> M1LTdXNCVkeHUh?=
TK10 cell NYryblFGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlv6TY5pcWKrdHnvckBw\iCqdX3hckBVUzFyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlUzOiEQvF2= NFv3fnJUSU6JRWK=
DSH1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJGRUUDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5N|k3KM7:TR?= NV;lSm1MW0GQR1XS
ECC12 cell M2HrNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mk\NTY5pcWKrdHnvckBw\iCqdX3hckBGS0NzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFkzOzFizszN MUjTRW5ITVJ?
EKVX cell NV3vTFJVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{f0WmlvcGmkaYTpc44hd2ZiaIXtZY4hTUuYWDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5PzRizszN NHLhUGFUSU6JRWK=
HCC2218 cell NYnMfJA3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXnUb|ZEUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNlE5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNUOyOkDPxE1? NGLFWnVUSU6JRWK=
LB2241-RCC cell MojhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETXT4lKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkK0NU1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkG1OFA{KM7:TR?= M2TmbnNCVkeHUh?=
LB996-RCC cell MljGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1LUeGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ7OU[tVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|NkKyPEDPxE1? M2r6[nNCVkeHUh?=
LC-1F cell NX63bo9PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUHSelB3UW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO NXX0bHBmW0GQR1XS
LS-513 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PVeWlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41ODB2MTFOwG0> MkfXV2FPT0WU

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
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID