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79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 MoryVJJwdGmoZYLheIlwdiCjc4PhfS=> NULNUVJrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUlUh[2WubDDsbY5mNCCLQ{WwQVAvODJ3IN88US=> NFLZe4cyPjR6M{e3Ni=>
BT474 cell line MXjQdo9tcW[ncnH0bY9vKGG|c3H5 NGTvcotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOFc1KGOnbHygcIlv\SxiSVO1NF0xNjB{NTFOwG0> Ml22NVY1QDN5N{K=
HN5 cell NYXqTo9PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7obYJuUW6qaXLpeIlwdiCxZjDIUlUh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNVIh|ryP MlPONVY4Pzd2MUC=
BT474 cell MlHWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnVTY5pcWKrdHnvckBw\iCEVES3OEBk\WyuIHfyc5d1cCCjZoTldkA4OiCqcoOsJGlEPTB;MD6wPEDPxE1? Mny4NVY4Pzd2MUC=
N87 cell MofFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKE56NzDj[YxtKGe{b4f0bEBi\nSncjC3NkBpenNuIFnDOVA:OC5yODFOwG0> NVHBbotNOTZ5N{e0NVA>
HFF cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFfUNWNKdmirYnn0bY9vKG:oIFjGSkBk\WyuIHfyc5d1cCxiSVO1NF06NjlizszN NGTEWY0yPjd5N{SxNC=>
SKBR3 cells MorvR5l1d3SxeHnjbZR6KGG|c3H5 MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFE4KM7:TR?= NXjN[45iOTlyMki0NlU>
A431 cells NHX0Wm9EgXSxdH;4bYNqfHliYYPzZZk> NFHOXXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4yODRizszN MV:xPVg5QDd4MR?=
SKBR3 cells MVfDfZRwfG:6aXPpeJkh[XO|YYm= NVz3WHFES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB{OTFOwG0> MYKxPVg5QDd4MR?=
HepG2 cells NVnW[lhZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXK5emVMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:Pi5{NzFOwG0> NWX6WG03OjBzNEO3O|g>
Hep3B2 cells MojpVJJwdGmoZYLheIlwdiCjc4PhfS=> MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincEPCNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9OU41QSEQvF2= NFfufVUzODF2M{e3PC=>
SKHEP1 cells NUXtV2w5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVnGc41QSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxRTVwMzFOwG0> M{C2e|IxOTR|N{e4
MCF7 cells MnntVJJwdGmoZYLheIlwdiCjc4PhfS=> MoO4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME22MlYh|ryP NGWzZ5kzODF2M{e3PC=>
MDA-MB-231 cells MlWwVJJwdGmoZYLheIlwdiCjc4PhfS=> NXTJSFQxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKGi{czDifUBCXFBiY3;ueIVvfCCjc4PhfUwhUUN3ME21MlQh|ryP NHLUTIUzODF2M{e3PC=>
SK-BR-3 cells M4PpcHBzd2yrZnXyZZRqd25iYYPzZZk> MlzFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3CVk0{KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF0xNjB2IN88US=> NHHEeWszODF2M{e3PC=>
A431 cells Mkf3SpVv[3Srb36gZZN{[Xl? M2ridWlvcGmkaYTpc44hd2ZiRVfGVkBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCDNEOxJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMEWyJO69VQ>? M1LTVVIxOzR4NkW1
N87 cells M3TFW2Z2dmO2aX;uJIF{e2G7 NUWzRpBzUW6qaXLpeIlwdiCxZjDFdoJDOiCrboTyZYNmdGy3bHHyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOPFch[2WubIOgZpkhTUyLU1GsJGlEPTB;MD6xJO69VQ>? NISzXnozODN2Nk[1OS=>
MIAPaCa cells MkPVSpVv[3Srb36gZZN{[Xl? M1vkT2lvcGmkaYTpc44hd2ZiRVfGVkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjR|MzFOwG0> MVeyNFgyPzV{Mx?=
MIAPaCa cells MknPSpVv[3Srb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKEWUQnKyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNTWFR[UOjIHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVAvOTRizszN NYDHco4zOjB6MUe1NlM>
CAL27 cells NXfucIZXS3m2b4TvfIlkcXS7IHHzd4F6 M133WGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYomgdoV{[Xq3cnnuJIR6\SC{ZXT1Z5Rqd25iYYPzZZktKEmFNUC9NE4xODdizszNMi=> M3r1dlIyODhyNkK5
SKOV3 cells M3\WU2N6fG:2b4jpZ4l1gSCjc4PhfS=> M4HVd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGhGWjJiYomgdoV{[Xq3cnnuJIR6\SC{ZXT1Z5Rqd25iYYPzZZktKEmFNUC9NE4xODNizszNMi=> MkXRNlExQDB4Mkm=
CAL27 cells Ml3SSpVv[3Srb36gZZN{[Xl? NGfWW3AyPiCq MXPJcohq[mm2aX;uJI9nKEWJRj3pcoR2[2WmIFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGNCVDJ5IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJGVITlJiYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDygTWM2OD1yLkCzNkDPxE1? NXnFXVNwOjFyOEC2Nlk>
SK-BR-3 cells MoL5VJJwdGmoZYLheIlwdiCjc4PhfS=> MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFXyZmIzKG:4ZYLlfJBz\XO|aX7nJIh2dWGwIGPLMWJTNTNiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEOyJO69VQ>? NXrrZmdiOjF3N{C4OFM>
BXF T24 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MorjOEBl[Xm| M3fB[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJZTiCWMkSgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVkvPjVizszN NIDPZXUzOjF4OU[wNS=>
CXF 269L cells NIOxRVlEgXSxdH;4bYNqfHliYYPzZZk> NFH6Xo81KGSjeYO= NWH3N4wzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS1iIIEK2PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRThwM{[g{txO M32wRVIzOTZ7NkCx
DIFI cells NWrhSnVVS3m2b4TvfIlkcXS7IHHzd4F6 NXLoO2h1PCCmYYnz M4np[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRKTkliY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUCuNlM2KM7:TR?= M1LtUlIzOTZ7NkCx
HT-29 cells MmC3R5l1d3SxeHnjbZR6KGG|c3H5 MWq0JIRigXN? M3;YPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20MlYzKM7:TR?= MUKyNlE3QTZyMR?=
RKO cells NF;ZfHREgXSxdH;4bYNqfHliYYPzZZk> MmPGOEBl[Xm| NYrYfI9XS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWkuRIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME21MlM2KM7:TR?= MY[yNlE3QTZyMR?=
GXF251L cells M1TOVWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2j3XVQh\GG7cx?= M2\USWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdZTjJ3MVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVEvPDhizszN NFrKUVYzOjF4OU[wNS=>
LIXF 575L cells MnrmR5l1d3SxeHnjbZR6KGG|c3H5 NXW1cHN2PCCmYYnz MkDqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUGlZTiB3N{XMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF04NjF6IN88US=> NHXobJczOjF4OU[wNS=>
LXFA 289L cells NWH4bHhYS3m2b4TvfIlkcXS7IHHzd4F6 M{TscFQh\GG7cx?= NILiUGdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEK4PWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTVwN{mg{txO MoG0NlIyPjl4MEG=
LXFA 526L M3KyWWN6fG:2b4jpZ4l1gSCjc4PhfS=> MnfqOEBl[Xm| NGHneWZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[DIEWyOmwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTRwMkGg{txO NVT3clJVOjJzNkm2NFE>
LXFA 629L cells M3PiSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NYLKUXBuPCCmYYnz MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMXGZCKDZ{OVygZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVIvQDdizszN MlyyNlIyPjl4MEG=
LXFL 1121L cells NFz1cWhEgXSxdH;4bYNqfHliYYPzZZk> MmHaOEBl[Xm| M3;kcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxZTkxiMUGyNWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTdwN{Og{txO M4\VfFIzOTZ7NkCx
LXFL 529L cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= M4TKVFQh\GG7cx?= NGG4eplEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNYE[OIEWyPWwh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\my3b4LvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTNwNUGg{txO MUGyNlE3QTZyMR?=
MCF7 cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= NWLDPZg5PCCmYYnz M1PUTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuPFMh|ryP NHPYNGQzOjF4OU[wNS=>
MDA231 cells NUfnc4p{S3m2b4TvfIlkcXS7IHHzd4F6 NUWycJdUPCCmYYnz NFTGcldEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEF{M{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVcvPyEQvF2= MUSyNlE3QTZyMR?=
OVXF 899L MWTDfZRwfG:6aXPpeJkh[XO|YYm= NVn1S3gxPCCmYYnz NWfveHlOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[[RjC4PVlNKGOnbHzzJIFnfGW{IESg[IF6eyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;yc41mfHKrYzDhcoFtgXOrczygTWM2OD1|LkO1JO69VQ>? MXKyNlE3QTZyMR?=
PAXF 546L cells M1nO[mN6fG:2b4jpZ4l1gSCjc4PhfS=> M2T6cVQh\GG7cx?= M3PPZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCYEZiNUS2UEBk\WyuczDh[pRmeiB2IHThfZMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\y2kYYPl[EBndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:Pi5zMjFOwG0> M4nRc|IzOTZ7NkCx
PANC1 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= NITjbGQ1KGSjeYO= NYHLfnVGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEGQQ{GgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVgvOTJizszN NXrEUXNJOjJzNkm2NFE>
22Rv1 cell MYLDfZRwfG:6aXPpeJkh[XO|YYm= NIjEbYc1KGSjeYO= NHS1UlFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAzOlK4MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9Ok4xPiEQvF2= NILCTXkzOjF4OU[wNS=>
DU145 cells NYfFXoluS3m2b4TvfIlkcXS7IHHzd4F6 M3LHUlQh\GG7cx?= MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC0JIRigXNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;Mj65PUDPxE1? NWLtbJQyOjJzNkm2NFE>
LNCAP cells NFfrVndEgXSxdH;4bYNqfHliYYPzZZk> MX60JIRigXN? NUP2bYk6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVMvPjhizszN NGnyZZAzOjF4OU[wNS=>
PC3M cells NUPNc3MyS3m2b4TvfIlkcXS7IHHzd4F6 M1zaVVQh\GG7cx?= M3PUSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEO01iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOVUh|ryP M2fsUFIzOTZ7NkCx
NIH/3T3 cells NVjGcFJPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWrUXnJVPzJiaB?= MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12LkOg{txO M3;XOFIzPTl3MUe3
NCI-H1648 cell M3j6c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfR[4pRUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCyOVQ1KM7:TR?= NXvFeWp3W0GQR1XS
NMC-G1 cell M{HzSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnqR2toUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV2NUCxJO69VQ>? NUDsXXNmW0GQR1XS
NTERA-S-cl-D1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkK2OVYyKM7:TR?= NIrvZ3dUSU6JRWK=
OCUB-M cell NInMXnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PjSWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTd2IN88US=> MWLTRW5ITVJ?
OS-RC-2 cell NX3VdGRzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKGi3bXHuJG9UNVKFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk6OTl7IN88US=> MojaV2FPT0WU
OVCAR-4 cell NH\YWGxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIK3PJFKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjFzNke1JO69VQ>? MWDTRW5ITVJ?
RL95-2 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LJO2lvcGmkaYTpc44hd2ZiaIXtZY4hWkx7NT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yPTZ5IN88US=> NWPyOo9[W0GQR1XS
SW954 cell NXTpU4ZnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIHTPJBKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> MWDTRW5ITVJ?
SW962 cell Mn7kS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGfGbGJKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> NHr5eJNUSU6JRWK=
TE-1 cell MnjOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkCyNVU6KM7:TR?= MXjTRW5ITVJ?
A253 cell M3rGWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{LW[WlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ3MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFQ5OyEQvF2= NGm0UYFUSU6JRWK=
A388 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2HQTGlvcGmkaYTpc44hd2ZiaIXtZY4hSTN6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFQ5OyEQvF2= NInaRolUSU6JRWK=
BB30-HNC cell NF34R3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYP3XmpIUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP NVfFc3JyW0GQR1XS
TE-12 cell MnfuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGXQXXdKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OjJ3ODFOwG0> Mnr0V2FPT0WU
TE-5 cell NIX5PWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEfwR|hKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1PjV2IN88US=> MXfTRW5ITVJ?
TE-6 cell NVTqd|RmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7JTY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVA2PyEQvF2= M3;VfXNCVkeHUh?=
TE-8 cell NITJXJpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXzJcohq[mm2aX;uJI9nKGi3bXHuJHRGNThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkCzO|Mh|ryP NFrGeJJUSU6JRWK=
TE-9 cell NECxO3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzQTY5pcWKrdHnvckBw\iCqdX3hckBVTS17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OVIxOSEQvF2= NXHpOIw1W0GQR1XS
TK10 cell MljWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HzVGlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN NF;ubZJUSU6JRWK=
DSH1 cell M4rxTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTKW2kxUW6qaXLpeIlwdiCxZjDoeY1idiCGU1ixJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTN7NjFOwG0> M{mwbHNCVkeHUh?=
ECC12 cell MoTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml3tTY5pcWKrdHnvckBw\iCqdX3hckBGS0NzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFkzOzFizszN M4r5THNCVkeHUh?=
EKVX cell NX3GNpZ4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XDc2lvcGmkaYTpc44hd2ZiaIXtZY4hTUuYWDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ5PzRizszN M2\4PXNCVkeHUh?=
HCC2218 cell MmfiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn3oTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{MkG4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTN{NjFOwG0> M4j6UnNCVkeHUh?=
LB2241-RCC cell NUTJXJVYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrRTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zNUSwN{DPxE1? NX;sbm1nW0GQR1XS
LB996-RCC cell Mlm3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV7SZZoxUW6qaXLpeIlwdiCxZjDoeY1idiCOQkm5Ok1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkO2NlI5KM7:TR?= NH24UYZUSU6JRWK=
LC-1F cell M3LscWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn3ETY5pcWKrdHnvckBw\iCqdX3hckBNSy1zRjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|gzPDRizszN Mn70V2FPT0WU
LS-513 cell NIDrOZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjoPIlKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDByNEGg{txO NYjGeFQ1W0GQR1XS

... 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+30% PEG 300+ddH2O
10mg/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、MSDS / 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、MSDS / 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
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

HER2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID