Lapatinib (GW-572016) Ditosylate

For research use only. Not for use in humans.

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) 在庫  
10mM (1mL in DMSO) JPY 33700 あり
JPY 26400 あり
JPY 68400 あり
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文献中Selleckの製品使用例(75)

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 MlLUVJJwdGmoZYLheIlwdiCjc4PhfS=> NFnReHlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjOOUBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN MWexOlQ5Ozd5Mh?=
BT474 cell line NVHKcWluWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFezUoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> M2PzT|E3PDh|N{ey
HN5 cell M1OxVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVu0eJJDUW6qaXLpeIlwdiCxZjDIUlUh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNVIh|ryP Moj6NVY4Pzd2MUC=
BT474 cell M3XBb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVPJcohq[mm2aX;uJI9nKEKWNEe0JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkC4JO69VQ>? NFn4c2syPjd5N{SxNC=>
N87 cell M1nZVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3ztfWlvcGmkaYTpc44hd2ZiTki3JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkC4JO69VQ>? NX2ybotpOTZ5N{e0NVA>
HFF cell M4XZWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjw[mh2UW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> NXWzO|JkOTZ5N{e0NVA>
SKBR3 cells MkDvR5l1d3SxeHnjbZR6KGG|c3H5 MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFE4KM7:TR?= NEXhVXYyQTB{OESyOS=>
A431 cells NGCy[VNEgXSxdH;4bYNqfHliYYPzZZk> NFrYTGhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4yODRizszN NWHuXYl6OTl6OEi3OlE>
SKBR3 cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFI6KM7:TR?= MVexPVg5QDd4MR?=
HepG2 cells Ml3BVJJwdGmoZYLheIlwdiCjc4PhfS=> Ml7FRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= NWLzdYxUOjBzNEO3O|g>
Hep3B2 cells NHHJenlRem:uaX\ldoF1cW:wIHHzd4F6 M3TDO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwN2IzKGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF02NjR7IN88US=> MXWyNFE1Ozd5OB?=
SKHEP1 cells NWTUVWh4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlX4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwQVUvOyEQvF2= M3ziZVIxOTR|N{e4
MCF7 cells NFL5OGFRem:uaX\ldoF1cW:wIHHzd4F6 M4\kNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok43KM7:TR?= NIPRbZczODF2M{e3PC=>
MDA-MB-231 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 NF7WZ2JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhcHK|IHL5JGFVWCClb370[Y51KGG|c3H5MEBKSzVyPUWuOEDPxE1? MXuyNFE1Ozd5OB?=
SK-BR-3 cells M{n1XXBzd2yrZnXyZZRqd25iYYPzZZk> NIXpfFFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMWJTNTNiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTBwMESg{txO MnLxNlAyPDN5N{i=
A431 cells NEfP[mtHfW6ldHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKEWJRmKgbY51emGlZXzseYxieiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hSTR|MTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjB3MjFOwG0> M{H3d|IxOzR4NkW1
N87 cells NFjwbnJHfW6ldHnvckBie3OjeR?= MkT3TY5pcWKrdHnvckBw\iCHcnLCNkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCQOEegZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zIN88US=> MoXDNlA{PDZ4NUW=
MIAPaCa cells NFPWWpRHfW6ldHnvckBie3OjeR?= MXnJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3JRXBiS2FiY3XscJMh[nliRVzJV2EtKEmFNUC9NE41OzNizszN NHHWN2ozODhzN{WyNy=>
MIAPaCa cells M2n1e2Z2dmO2aX;uJIF{e2G7 NYPtTZNwUW6qaXLpeIlwdiCxZjDFVmJjOiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVUmDUHHDZUBk\WyuczDifUBGVEmVQTygTWM2OD1yLkG0JO69VQ>? Mn3rNlA5OTd3MkO=
CAL27 cells M4\pbmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHziOGdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB5IN88UU4> MmPYNlExQDB4Mkm=
SKOV3 cells NF\POlBEgXSxdH;4bYNqfHliYYPzZZk> NVHreIU6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNib4\ldoV5eHKnc4PpcochUEWUMjDifUBz\XOjeoXybY4h\HmnIILl[JVkfGmxbjDhd5NigSxiSVO1NF0xNjByMzFOwG0v NX73eIw4OjFyOEC2Nlk>
CAL27 cells MmHpSpVv[3Srb36gZZN{[Xl? NXLUO2d1OTZiaB?= MWTJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? M3T3U|IyODhyNkK5
SK-BR-3 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 NYjJWmRnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBGemKEMjDveoVz\XiycnXzd4lv\yCqdX3hckBUUy2EUj2zJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA{OiEQvF2= M17xUVIyPTdyOESz
BXF T24 cells M1XBU2N6fG:2b4jpZ4l1gSCjc4PhfS=> NIPyVWw1KGSjeYO= MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCXGYhXDJ2IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME25MlY2KM7:TR?= M4Ty[|IzOTZ7NkCx
CXF 269L cells MnXsR5l1d3SxeHnjbZR6KGG|c3H5 MVm0JIRigXN? MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDXGYhOjZ7TDDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9PE4{PiEQvF2= NUnWcZhiOjJzNkm2NFE>
DIFI cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= NEXxe5o1KGSjeYO= M1zpbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= NG\l[VEzOjF4OU[wNS=>
HT-29 cells NW\4OYg2S3m2b4TvfIlkcXS7IHHzd4F6 Mlq0OEBl[Xm| MoXXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOlIh|ryP MYGyNlE3QTZyMR?=
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LIXF 575L cells NUPlVIVtS3m2b4TvfIlkcXS7IHHzd4F6 M{n1SlQh\GG7cx?= NED3VXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNUViIIEW3OWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwMUig{txO NYLzeGJpOjJzNkm2NFE>
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LXFA 629L cells M{LVSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUK0JIRigXN? MkHqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUHhHSSB4MknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF0zNjh5IN88US=> NInjNW0zOjF4OU[wNS=>
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LNCAP cells M3u0emN6fG:2b4jpZ4l1gSCjc4PhfS=> M4iy[FQh\GG7cx?= NVz6VW9WS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN NUjwepp7OjJzNkm2NFE>
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NIH/3T3 cells NEK5U2lRem:uaX\ldoF1cW:wIHHzd4F6 MYC3NkBp M1nCdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTlnIM|NVOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuN{DPxE1? NHu0bJIzOjV7NUG3Oy=>
NCI-H1648 cell NG\UZVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDiV3c{UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCyOVQ1KM7:TR?= NYjyNpoxW0GQR1XS
NMC-G1 cell NEDydXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnuR2dbUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV2NUCxJO69VQ>? M{nsNHNCVkeHUh?=
NTERA-S-cl-D1 cell M17sXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H0OGlvcGmkaYTpc44hd2ZiaIXtZY4hVlSHUlGtV{1kdC2GMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNlY2PjFizszN M3TaNnNCVkeHUh?=
OCUB-M cell M4HlZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2TtfmlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTd2IN88US=> NW\HXpVNW0GQR1XS
OS-RC-2 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LQNmlvcGmkaYTpc44hd2ZiaIXtZY4hV1NvUlOtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTlzOUmg{txO NVr2fXduW0GQR1XS
OVCAR-4 cell NXnBNZFNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGjlbZlKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjFzNke1JO69VQ>? MnqyV2FPT0WU
RL95-2 cell NHHPbmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJHJNQTVvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVU3PyEQvF2= MknKV2FPT0WU
SW954 cell NFe3clBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXrJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTV2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zPVI1PSEQvF2= MkDJV2FPT0WU
SW962 cell MnfwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTUTY5pcWKrdHnvckBw\iCqdX3hckBUXzl4MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|kzPDVizszN NH3yXFBUSU6JRWK=
TE-1 cell M4HJcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\xTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6wNlE2QSEQvF2= NHjFTm9USU6JRWK=
A253 cell Ml\DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnnsTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= MXjTRW5ITVJ?
A388 cell M1LBdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknnTY5pcWKrdHnvckBw\iCqdX3hckBCOzh6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= MU\TRW5ITVJ?
BB30-HNC cell NUHJ[3ZUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3\KfGlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl5M{O1JO69VQ>? NFOwVphUSU6JRWK=
TE-12 cell NFnaTnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILNeYJKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjJ3ODFOwG0> NYTMPYRKW0GQR1XS
TE-5 cell NIHkSXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkK0OlU1KM7:TR?= M1nkR3NCVkeHUh?=
TE-6 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVjtNYtJUW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QTB3NzFOwG0> MVvTRW5ITVJ?
TE-8 cell NUnHRVNOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFT4RXZKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{PzNizszN NVzuXWZiW0GQR1XS
TE-9 cell MlLDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NULTcYRXUW6qaXLpeIlwdiCxZjDoeY1idiCWRT25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTJyMTFOwG0> M2rpe3NCVkeHUh?=
TK10 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJHRMOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2OVIzKM7:TR?= MUnTRW5ITVJ?
DSH1 cell M2C3[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M376[WlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN NX;LcmtzW0GQR1XS
ECC12 cell NGTLW|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXLJcohq[mm2aX;uJI9nKGi3bXHuJGVESzF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVI{OSEQvF2= MmjRV2FPT0WU
EKVX cell MnvyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1LoNGlvcGmkaYTpc44hd2ZiaIXtZY4hTUuYWDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5PzRizszN NEf1TmpUSU6JRWK=
HCC2218 cell NUXoZmh5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWqyV3RjUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNlE5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yNUOyOkDPxE1? Mne0V2FPT0WU
LB2241-RCC cell MkHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYrt[2x{UW6qaXLpeIlwdiCxZjDoeY1idiCOQkKyOFEuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6xOVQxOyEQvF2= MWHTRW5ITVJ?
LB996-RCC cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13Kc2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJ7OU[tVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|NkKyPEDPxE1? M4LSRXNCVkeHUh?=
LC-1F cell NV\M[WgxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVXmO|BxUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2xSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzh{NESg{txO M2H4SHNCVkeHUh?=
LS-513 cell NHLhfXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFAxPDFizszN NIPWVplUSU6JRWK=

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
p-ErbB2 / t-ErbB2 / p-Akt / t-Akt / p-Erk / t-Erk; 

PubMed: 25238247     


Dose response of lapatinib and PD168393 on phosphorylation of ErbB2, AKT and ERK in Calu3 and SkBr3 cells in response to EGF treatment. p-ErbB2: phosphorylated ErbB2; t-ErbB2: total-ErbB2; p-AKT: phosphorylated AKT; t-AKT: total AKT; p-ERK: phosphorylated ERK; t-ERK: total ERK.

pEGFR / EGFR / p-mTOR / 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. All values are presented as the mean ± standard error (S.E.) (**p < 0.01).

25238247 28938602
Growth inhibition assay
Cell viability ; 

PubMed: 24947784     


Huh7 (A), HepG2 (B), or HA22T (C) HCC cells were left untreated or treated with 0.1% DMSO (vehicle, D) or with DMSO containing various concentrations of lapatinib (1.25, 2.5, 5, or 10 μM) for 3 days. Relative amounts of viable cells were detected by MTS assay. O.D. values from DMSO-treated control cells were designated 100%.

24947784
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]
- 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
  • 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 (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
Smiles CC1=CC=C(C=C1)[S](O)(=O)=O.CC2=CC=C(C=C2)[S](O)(=O)=O.C[S](=O)(=O)CCNCC3=CC=C(O3)C4=CC=C5N=CN=C(NC6=CC=C(OCC7=CC=CC(=C7)F)C(=C6)Cl)C5=C4

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 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

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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
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID