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EGFR 和 ErbB2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81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EGFR 和 ErbB2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 M{PTc3Bzd2yrZnXyZZRqd25iYYPzZZk> MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiQNTDj[YxtKGyrbnWsJGlEPTB;MD6wNlUh|ryP NF;GblkyPjR6M{e3Ni=>
BT474 cell line MlXQVJJwdGmoZYLheIlwdiCjc4PhfS=> MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNEe0JINmdGxibHnu[UwhUUN3ME2wMlAzPSEQvF2= M3mwe|E3PDh|N{ey
HN5 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnrITY5pcWKrdHnvckBw\iCKTkWgZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKg{txO NHe0U2IyPjd5N{SxNC=>
BT474 cell MlTmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M332fmlvcGmkaYTpc44hd2ZiQmS0O|Qh[2WubDDndo94fGhiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNFgh|ryP NVH6fIs{OTZ5N{e0NVA>
N87 cell NWrEPGc{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmLKTY5pcWKrdHnvckBw\iCQOEegZ4VtdCCpcn;3eIgh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEig{txO NG\5NG8yPjd5N{SxNC=>
HFF cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXhTY5pcWKrdHnvckBw\iCKRl[gZ4VtdCCpcn;3eIgtKEmFNUC9PU46KM7:TR?= NVvSZVJnOTZ5N{e0NVA>
SKBR3 cells M1ftXWN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn7PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAyPyEQvF2= MlrRNVkxOjh2MkW=
A431 cells NEDROlNEgXSxdH;4bYNqfHliYYPzZZk> MmPlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVA1KM7:TR?= MVexPVg5QDd4MR?=
SKBR3 cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFI6KM7:TR?= M3K1T|E6QDh6N{[x
HepG2 cells NFvDV2dRem:uaX\ldoF1cW:wIHHzd4F6 MnTtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiCqcoOgZpkhSVSSIHPvcpRmdnRiYYPzZZktKEmFNUC9Ok4zPyEQvF2= MYGyNFE1Ozd5OB?=
Hep3B2 cells MkTTVJJwdGmoZYLheIlwdiCjc4PhfS=> NIfucGdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldFNDOiClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS52OTFOwG0> NYL1SIU{OjBzNEO3O|g>
SKHEP1 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NHf1d5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLTGVROSClZXzsd{Bi\nSncjDodpMh[nliQWTQJINwdnSnboSgZZN{[XluIFnDOVA:PS5|IN88US=> Mo\3NlAyPDN5N{i=
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MDA-MB-231 cells MlvtVJJwdGmoZYLheIlwdiCjc4PhfS=> Mki2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJIhzeyCkeTDBWHAh[2:wdHXueEBie3OjeTygTWM2OD13LkSg{txO M2PTTVIxOTR|N{e4
SK-BR-3 cells NVK5VnNLWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlPPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3CVk0{KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NF0xNjB2IN88US=> NIToeoszODF2M{e3PC=>
A431 cells NHPqXHpHfW6ldHnvckBie3OjeR?= NHPDR4lKdmirYnn0bY9vKG:oIFXHSnIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQUSzNUBk\WyuczDifUBGVEmVQTygTWM2OD1yLkC1NkDPxE1? NWfXOY95OjB|NE[2OVU>
N87 cells M{nzNGZ2dmO2aX;uJIF{e2G7 M2rTfmlvcGmkaYTpc44hd2ZiRYLiRlIhcW62cnHj[YxtfWyjcjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTki3JINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMTFOwG0> NVP4WG1qOjB|NE[2OVU>
MIAPaCa cells MXHGeY5kfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKEWJRmKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3JRXBiS2FiY3XscJMh[nliRVzJV2EtKEmFNUC9NE41OzNizszN NWTUO5RXOjB6MUe1NlM>
MIAPaCa cells NIToZnJHfW6ldHnvckBie3OjeR?= Ml\nTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjF2IN88US=> MYeyNFgyPzV{Mx?=
CAL27 cells NHPXTZBEgXSxdH;4bYNqfHliYYPzZZk> MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDRWwzPyClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFS2ZTKGK7IILld4F7fXKrbjDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNFA4KM7:TT6= M3jsWlIyODhyNkK5
SKOV3 cells NH;rNlBEgXSxdH;4bYNqfHliYYPzZZk> NG\3OIZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJTVJ{IHL5JJJme2G8dYLpckBlgWVicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVAvODB|IN88UU4> NW[yWFMzOjFyOEC2Nlk>
CAL27 cells NGnMUVNHfW6ldHnvckBie3OjeR?= M1nj[VE3KGh? MkLOTY5pcWKrdHnvckBw\iCHR1[tbY5lfWOnZDDFS2ZTKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBESUx{NzDj[YxteyCxdnXy[ZhxemW|c3nu[{BGT0[UIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4SsJGlEPTB;MD6wN|Ih|ryP NYX1cYhCOjFyOEC2Nlk>
SK-BR-3 cells NX[5cWZGWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEfrRpVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGVz[kJ{IH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJHNMNUKULUOgZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFMzKM7:TR?= M4\JR|IyPTdyOESz
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CXF 269L cells MUPDfZRwfG:6aXPpeJkh[XO|YYm= NFHlSnM1KGSjeYO= M3;zdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNZTiB{NknMJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{b33leJJq[yCjbnHsfZNqeyxiSVO1NF05NjN4IN88US=> NVvj[Xd{OjJzNkm2NFE>
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HT-29 cells NYLSdW4zS3m2b4TvfIlkcXS7IHHzd4F6 NX;lfXJFPCCmYYnz NVP3V4VbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwQVQvPjJizszN MXuyNlE3QTZyMR?=
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MCF7 cells M2HvO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MW[0JIRigXN? NHrWbZBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME20Mlg{KM7:TR?= MViyNlE3QTZyMR?=
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PC3M cells M1zCSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MkPkOEBl[Xm| M1PIdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEO01iY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyPUSuOVUh|ryP NXvG[5hyOjJzNkm2NFE>
NIH/3T3 cells M1H2b3Bzd2yrZnXyZZRqd25iYYPzZZk> NHqxWFY4OiCq MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12LkOg{txO M{[zO|IzPTl3MUe3
NCI-H1648 cell NHXDPG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzQTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB{NUS0JO69VQ>? M1TlOHNCVkeHUh?=
NMC-G1 cell NV3rNGVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXLxNmJVUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV2NUCxJO69VQ>? MULTRW5ITVJ?
NTERA-S-cl-D1 cell MkLZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFywN2tKdmirYnn0bY9vKG:oIHj1cYFvKE6WRWLBMXMu[2xvREGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlI3PTZzIN88US=> M2HjXnNCVkeHUh?=
OCUB-M cell MonJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFU4PCEQvF2= NUHQRnF6W0GQR1XS
OS-RC-2 cell M1vrUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIPq[GxKdmirYnn0bY9vKG:oIHj1cYFvKE:VLWLDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjl7MUm5JO69VQ>? M1PZZ3NCVkeHUh?=
OVCAR-4 cell NF3hfGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2jFcGlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTF4N{Wg{txO MXvTRW5ITVJ?
RL95-2 cell MnrVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJHJNQTVvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVU3PyEQvF2= NFrkSGhUSU6JRWK=
SW954 cell MoT1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH\5PHpKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{QTJ2NTFOwG0> M1;Ib3NCVkeHUh?=
SW962 cell NXqzNm1ST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVTHbppRUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl{NEWg{txO M4XuTHNCVkeHUh?=
TE-1 cell NUTYSVhiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{PJbmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNFIyPTlizszN MXHTRW5ITVJ?
A253 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkfGTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6wOFg{KM7:TR?= NXi5S2xyW0GQR1XS
A388 cell NXvtV3VbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGE{QDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkC0PFMh|ryP MofmV2FPT0WU
BB30-HNC cell NF\JcnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWGwO5RbUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOUezN|Uh|ryP Mn;5V2FPT0WU
TE-12 cell NFnNZ5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmrFTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|IzPThizszN NE\oPGpUSU6JRWK=
TE-5 cell NGXDbXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\h[nZKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1PjV2IN88US=> MlLNV2FPT0WU
TE-6 cell NF3Ed25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NG\Ld3JKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ6ODV5IN88US=> M1zTdXNCVkeHUh?=
TE-8 cell NV75dFdxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoTlTY5pcWKrdHnvckBw\iCqdX3hckBVTS16IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6wN|c{KM7:TR?= MYXTRW5ITVJ?
TE-9 cell MnzWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW1NlAyKM7:TR?= Mo\PV2FPT0WU
TK10 cell NHS0d5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fXfGlvcGmkaYTpc44hd2ZiaIXtZY4hXEtzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVY2OjJizszN M4\5UnNCVkeHUh?=
DSH1 cell NED4dW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlr6TY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVM6PiEQvF2= M13Cc3NCVkeHUh?=
ECC12 cell Mnr1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGjXdJZKdmirYnn0bY9vKG:oIHj1cYFvKEWFQ{GyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xQTJ|MTFOwG0> Mnz3V2FPT0WU
EKVX cell NGHLRphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWr6U|ZzUW6qaXLpeIlwdiCxZjDoeY1idiCHS2\YJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PDh5NDFOwG0> M4HtS3NCVkeHUh?=
HCC2218 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGC4W25KdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{KyNVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB3M{K2JO69VQ>? M{PINHNCVkeHUh?=
LB2241-RCC cell M3zrV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2\sUGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMUW0NFMh|ryP MX\TRW5ITVJ?
LB996-RCC cell M{HE[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mom2TY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4MkK4JO69VQ>? NY\4RXFoW0GQR1XS
LC-1F cell M1nGXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJGxENTGIIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zPFI1PCEQvF2= MofDV2FPT0WU
LS-513 cell NX[1b4FtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFnWNJlKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDByNEGg{txO NHvWW3NUSU6JRWK=

... 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 只
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
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
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 --

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.

Selleck产品目录册

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

  • 选择性强的EGFR抑制剂

    Erlotinib HCl (OSI-744) : EGFR-selective, IC50=2 nM.

  • 活性最高的EGFR抑制剂

    Afatinib (BIBW2992) : EGFR(wt), IC50=0.5 nM; EGFR(L858R), IC50=0.4 nM; EGFR(L858R/T790M), IC50=10 nM; HER2, IC50=14 nM.

  • FDA批准的EGFR抑制剂

    Lapatinib : Approved by FDA for breast cancer.

  • 最新的EGFR抑制剂

    CO-1686 (AVL-301) New : Irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively.

相关HER2产品

  • Erlotinib New

    Erlotinib (CP358774, NSC 718781)是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。

  • Bemcentinib (R428) New

    Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。

  • Pexidartinib (PLX3397) New

    Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R，Kit (c-Kit)，和 FLT3受体酪氨酸激酶抑制剂，其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死，并具有抗肿瘤活性。Phase 3。

  • AC480 (BMS-599626)

    AC480 (BMS-599626)是一种选择性的，高效效的HER1和HER2抑制剂，IC50分别为20 nM和30 nM。比对HER4效果强8倍左右，而比对VEGFR2， c-Kit， Lck， MET等的作用强100倍以上。Phase 1。

    Features:BMS-599626是口服生物有效性的人表皮生长因子受体 (HER) 激酶HER1/HER2选择性抑制剂。

  • CP-724714

    CP-724714是一种有效的，选择性HER2/ErbB2抑制剂，IC50为10 nM，无细胞试验中比作用于EGFR，InsR，IRG-1R，PDGFR，VEGFR2，Abl，Src，c-Met等选择性高640多倍。Phase 2。

    Features:CP-724,714可用于治疗抗Trastuzumab的过量表达erbB2的肿瘤。

  • Neratinib (HKI-272)

    Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂，在无细胞试验中IC50分别为59 nM 和 92 nM；微弱抑制KDR和Src，对Akt，CDK1/2/4，IKK-2，MK-2，PDK1，c-Raf和c-Met没有显著的抑制作用。Phase 3。

  • Sapitinib (AZD8931)

    Sapitinib (AZD8931)是一种可逆的，ATP竞争性EGFR，ErbB2和ErbB3抑制剂，无细胞试验中IC50分别为4 nM，3 nM和4 nM，作用于NSCLC细胞比Gefitinib或Lapatinib更有效，作用于ErbB家族比作用于MNK1和Flt选择性强100倍。Phase 2。

  • Mubritinib (TAK 165)

    Mubritinib (TAK 165)是一种有效的HER2/ErbB2抑制剂，在BT-474细胞中IC50为6 nM；而在BT-474细胞系中对EGFR，FGFR，PDGFR，JAK1，Src和Blk没有抑制作用。Phase 1。

  • Tyrphostin AG 879

    Tyrphostin AG 879有效抑制HER2/ErbB2，IC50为1 μM，作用于ErbB2比作用于PDGFR和EGFR选择性高100到500倍。

  • Gefitinib (ZD1839)

    Gefitinib (ZD1839)是一种EGFR抑制剂，作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992，IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。

    Features:Gefitinib是有效的EGFR酪氨酸激酶抑制剂。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID