Lapatinib (GW-572016) Ditosylate

For research use only. Not for use in humans.

目录号:S1028 中文名称:二苯磺酸拉帕替尼

Lapatinib (GW-572016) Ditosylate Chemical Structure

CAS No. 388082-77-7

Lapatinib (GW-572016) Ditosylate是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.8和9.2 nM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1564.18 现货
RMB 1214.79 现货
RMB 2104.83 现货
RMB 3286.41 现货
RMB 5487.3 现货
RMB 9746.1 现货
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客户使用Selleck生产的Lapatinib (GW-572016) Ditosylate发表文献92篇:

产品安全说明书

HER2抑制剂选择性比较

生物活性

产品描述 Lapatinib (GW-572016) Ditosylate是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.8和9.2 nM。
靶点
ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
9.2 nM 10.8 nM 367 nM
体外研究

Lapatinib 微弱抑制ErbB4活性,IC50为367 nM, 作用于EGFR和 ErbB2 比作用于其他激酶,如c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2,和 VEGFR-2选择性高300多倍。Lapatinib作用于HN5细胞时,显著抑制受体EGFR 和 ErbB2自磷酸化,这种作用存在剂量依赖性,IC50分别为170 nM和80 nM,而作用于BT474细胞时,IC50分别为210 nM 和 60 nM。与OSI-774和Iressa(ZD1839)优先抑制过量表达EGFR细胞生长不同, Lapatinib 抑制过量表达EGFR和ErbB2细胞生长。 作用于过量表达EGFR或 ErbB2的细胞具有高抑制活性,IC50为0.09-0.21 μM,而作用于表达低水平EGFR或ErbB2的细胞,IC50为3-12 μM,比作用于正常纤维细胞选择性高100倍。Lapatinib有效抑制过量表达EGFR的HN5和A-431细胞生长,也抑制过量表达ErbB2的BT474和N87细胞生长,且显著诱导HN5细胞周期停在G1期,也诱导 BT474 细胞凋亡,与抑制AKT磷酸化相关。[1] Lapatinib 作用于含EGFR的L858R和T790M突变的抗Gefitinib的H1975细胞显著抑制Stat3磷酸化,导致细胞生长受抑制,IC50为1-2 μM。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HN5 cell line MkjUVJJwdGmoZYLheIlwdiCjc4PhfS=> MlvQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkWgZ4VtdCCuaX7lMEBKSzVyPUCuNFI2KM7:TR?= NH3xVoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkS4N|c4Oid-MU[0PFM4PzJ:L3G+
BT474 cell line MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MnvxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVES3OEBk\WyuIHzpcoUtKEmFNUC9NE4xOjVizszN NIDBcpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkS4N|c4Oid-MU[0PFM4PzJ:L3G+
HN5 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{HZfmlvcGmkaYTpc44hd2ZiSF61JINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czygTWM2OD1yLkGyJO69VQ>? NYHNRVh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[3O|c1OTBpPkG2O|c4PDFyPD;hQi=>
BT474 cell MnzUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2jscGlvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP NWjiVoJsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[3O|c1OTBpPkG2O|c4PDFyPD;hQi=>
N87 cell NXjIUmZCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKE56NzDj[YxtKGe{b4f0bEBi\nSncjC3NkBpenNuIFnDOVA:OC5yODFOwG0> NUHBdGxvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[3O|c1OTBpPkG2O|c4PDFyPD;hQi=>
HFF cell NHjBSGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLGRmE5UW6qaXLpeIlwdiCxZjDISmYh[2WubDDndo94fGhuIFnDOVA:QS57IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjd5N{SxNEc,OTZ5N{e0NVA9N2F-
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MIAPaCa MkS4SpVv[3Srb36gZZN{[Xl? MnXQTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2zszN Mm\1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6MUe1NlMoRjJyOEG3OVI{RC:jPh?=
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NTERA-S-cl-D1 cell NGXtSIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkK2OVYyKM7:TR?= MlPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
OCUB-M cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1W5[mlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTd2IN88US=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
OS-RC-2 cell M3r6S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWHzXIF5UW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS57OUG5PUDPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
OVCAR-4 cell NYPQS4p5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rpZmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
RL95-2 cell M2PESGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnKwTY5pcWKrdHnvckBw\iCqdX3hckBTVDl3LUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2PjdizszN Mke2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
SW954 cell NX\YbnNST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGC3bZZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> MnXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
SW962 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1SzfWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6OjR3IN88US=> Ml\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
TE-1 cell M3T1OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\TbGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNFIyPTlizszN NEnPdIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
A253 cell NVL3eZR[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkTFTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NWDNW|VQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
A388 cell NWm2dlE4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUHJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP NVHLW5p2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
BB30-HNC cell NVnZWmpPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKGi3bXHuJGJDOzBvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PzN|NTFOwG0> M2rJc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
TE-12 cell Ml;oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37sSWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlczOjV6IN88US=> M3zvcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
TE-5 cell NID3ZopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\TOo5YUW6qaXLpeIlwdiCxZjDoeY1idiCWRT21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDZ3NDFOwG0> NYe3THllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
TE-6 cell Ml7lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEj3TnpKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ6ODV5IN88US=> MmfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU1Nyd-U1HOS2VTRC:jPh?=
TE-8 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mm\JTY5pcWKrdHnvckBw\iCqdX3hckBVTS16IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6wN|c{KM7:TR?= NV31W3NkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
TE-9 cell MnfVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\oWpBNUW6qaXLpeIlwdiCxZjDoeY1idiCWRT25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTJyMTFOwG0> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
TK10 cell MljrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\X[mlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN M13ycVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
DSH1 cell MkL5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3Hr[mlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk{QTZizszN NEmy[|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
ECC12 cell Mor6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGGxR|lKdmirYnn0bY9vKG:oIHj1cYFvKEWFQ{GyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTJ|MTFOwG0> M{W0TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
EKVX cell MknoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjDTY5pcWKrdHnvckBw\iCqdX3hckBGU1[[IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OFg4PCEQvF2= NFnVNWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+
HCC2218 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnraTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> NYHhXW1VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV2Lze+V2FPT0WUPD;hQi=>
LB2241-RCC cell NWnMclFmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MojJTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zNUSwN{DPxE1? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
LB996-RCC cell NVzONoNqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnjWTY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVQwLz6VQV7HSXI9N2F-
LC-1F cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFq5OGNKdmirYnn0bY9vKG:oIHj1cYFvKEyFLUHGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{QDJ2NDFOwG0> M4fhSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2PC9pPmPBUmdGWjxxYU6=
LS-513 cell M4P4bWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFAxPDFizszN NFfEcGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTRxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
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
体内研究 Lapatinib 按~100 mg/kg剂量口服处理,每天两次,显著抑制BT474和HN5移植瘤生长,这种作用存在剂量依赖性。[1] 与在体外活性一致,Lapatinib按100-150 mg/kg剂量处理携带H1975肿瘤的小鼠,延迟肿瘤生长。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外激酶实验:

通过测量抑制肽底物磷酸化的情况而获得抑制酶活性的IC50值。通过杆状病毒表达系统纯化EGFR 和 ErbB2的细胞外激酶域。在96孔圆底板上进行EGFR和ErbB2反应,终体积为45 μL。反应混合物含50 mM 4-吗啉丙磺酸(pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi [γ33P] ATP/每次反应, 50 μM 肽 A [生物素-(氨基)-EEEEYFELVAKKK-CONH2], 1 mM 二流苏糖醇,及 1 μL DMSO(含连续稀释的Lapatinib,起始浓度为10 μM)。加入指定纯化的 1型受体胞内域,开始反应。加入的酶量为为1 pmol/每组反应(20 nM)在23oC下反应10分钟,加入45 μL 0.5%溶于水的磷酸,终止反应。终止反应混合物(75 μL) 转移到磷酸纤维过滤板上。板过滤,然后使用200 μL 0.5% 磷酸冲洗3次。每孔加入闪烁剂(50 μL) , 在Packard Topcount上测量每组反应。通过10点剂量反应曲线获得IC50值。
细胞实验:[1]
- 合并
  • Cell lines: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, 和 HB4a c5.2
  • Concentrations: 溶于 DMSO,终浓度为~100 μM
  • Incubation Time: 72小时
  • Method: 使用不同浓度Lapatinib处理细胞72小时。使用亚甲基蓝染色测定相对细胞数。使用Spectra酶标仪在620 nm 处测定吸光值。通过碘化丙啶染色和渗透BrdUrd的抗体检测,测量细胞死亡和细胞周期分析。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下移植HN5细胞的CD-1雌性裸鼠,皮下移植BT474细胞的 C.B-17 SCID 雌性小鼠
  • Dosages: ~100 mg/kg
  • Administration: 口服处理,每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (108.05 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+40% PEG 300+5% Tween 80+53% ddH2O
1.25 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 925.46
化学式

C29H26ClFN4O4S.2C7H8O3S

CAS号 388082-77-7
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04608409 Recruiting Drug: Lapatinib and Paclitaxel Ovarian Cancer Frederick R. Ueland M.D.|University of Kentucky November 16 2020 Phase 1
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
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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID