Lapatinib

For research use only. Not for use in humans.

目录号:S2111 别名: GW-572016, GSK572016 中文名称:拉帕替尼

Lapatinib Chemical Structure

CAS No. 231277-92-2

Lapatinib (GSK572016),以 Lapatinib Ditosylate的形式使用,是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。

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RMB 2192.38 现货
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客户使用Selleck生产的Lapatinib发表文献359篇:

产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述 Lapatinib (GSK572016),以 Lapatinib Ditosylate的形式使用,是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。Lapatinib 可诱导 ferroptosis 和细胞自噬。
特性 Lapatinib 已经批准用于治疗HER-2阳性转移性乳腺癌。[2]
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

除了ErbB-4例外, Lapatinib 作用于EGFR 和 ErbB-2比作用于其他测试的激酶,如c-Src, MEK和ERK选择性高300多倍。Lapatinib处理,抑制EGFR 和ErbB-2受体自磷酸化,这种作用存在剂量依赖性,作用于 BT474 和HN5 细胞时,IC50 分别为 0.17 和  0.08 μM。Lapatinib作用于EGFR-和ErbB-2-过量表达的肿瘤细胞,抑制EGFR 和ErbB-2自磷酸化,比作用于纯化酶的效力低10倍左右。Lapatinib 抑制 EGFR- 和ErbB-2过量表达的细胞生长,而OSI-774和 Iressa(都为EGFR选择性抑制剂)优先抑制 EGFR过量表达的细胞生长。Lapatinib作用于肿瘤细胞比作用于正常成纤维细胞效果高100倍左右。ErbB-2转染的乳腺上皮细胞HB4a c5.2,对 Lapatinib的反应敏感度比未转染的亲本对照细胞HB4a高40倍左右。使用不含Lapatinib 的培养基培养HN5 细胞群2周左右后,使用30 μM Lapatinib 短暂处理,完全抑制细胞生长。浓度>3.3 μM时抑制50%生长。浓度为0.37 μM时抑制20%生长。另一种EGFR过量表达的细胞A-431, 与HN5反应相似。Lapatinib在抑制 EGFR过量表达的细胞生长方面与 OSI-774 相似。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1648 NIHDflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDKVGJXUUN3ME2wMlAzPTR2IN88US=> M4i5O3NCVkeHUh?=
HCC2218 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3reFhnUUN3ME2wMlA2OzJ4IN88US=> NEO3V|ZUSU6JRWK=
OCUB-M MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[wZVV7UUN3ME2wMlA2PzRizszN MYXTRW5ITVJ?
ECC12 NEfseGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwMEmyN|Eh|ryP M4rjOnNCVkeHUh?=
DSH1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PnOWlEPTB;MD6wPVM6PiEQvF2= MX;TRW5ITVJ?
BT-474 NEHTN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDBTWM2OD1yLkKxN|E2KM7:TR?= MX\TRW5ITVJ?
BB30-HNC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnXXHNKSzVyPUCuNlQ3PTRizszN Mk\sV2FPT0WU
EKVX MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHIPGVwUUN3ME2wMlQ1QDd2IN88US=> NUi5copzW0GQR1XS
TE-12 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\YSZVJUUN3ME2wMlQ6ODV5IN88US=> NX3VPY0{W0GQR1XS
A388 NGjoVW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCyPVY5UUN3ME2wMlczOjV6IN88US=> M2ftXXNCVkeHUh?=
TE-9 MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwN{S0OVMh|ryP MXzTRW5ITVJ?
LB2241-RCC NHLQNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3tbWxKSzVyPUGuNVU1ODNizszN MkPUV2FPT0WU
LB996-RCC NVjuUpp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zhcGlEPTB;MT6zOlIzQCEQvF2= NXnKdYlWW0GQR1XS
LC-1F NYPDOnM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PyOGlEPTB;MT6zPFI1PCEQvF2= NIXROWxUSU6JRWK=
TE-6 NV7HZVM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nGXmlEPTB;MT61OVIxOSEQvF2= NE\sepJUSU6JRWK=
A253 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTFwOUezN|Uh|ryP MoKwV2FPT0WU
OS-RC-2 M2\YbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwOUmxPVkh|ryP Mn;KV2FPT0WU
TE-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TJXWlEPTB;Mj6wOFg{KM7:TR?= MULTRW5ITVJ?
RL95-2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNwMUW2O{DPxE1? NVXCNZBzW0GQR1XS
LS-513 NE\2VlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDReGxKSzVyPUOuOFAxPDFizszN MmPmV2FPT0WU
DJM-1 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7TeHBpUUN3ME2zMlQ3QTd3IN88US=> MWHTRW5ITVJ?
NMC-G1 NX;Td4ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknaTWM2OD1|LkW0OVAyKM7:TR?= NF22W|hUSU6JRWK=
TE-10 NYGw[5prT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTNwNUWzOVYh|ryP MoHyV2FPT0WU
TE-5 NVTYSZRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPHNY5KSzVyPUSuNFM4OyEQvF2= M3\sXHNCVkeHUh?=
TK10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HGOWlEPTB;ND6xOlUzOiEQvF2= M{K5c3NCVkeHUh?=
UACC-812 M2PqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfUXGVlUUN3ME20MlU3OTV|IN88US=> MnHWV2FPT0WU
SW962 M{DMeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq1TWM2OD13LkCyNVU6KM7:TR?= MnrkV2FPT0WU
SW954 MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml60TWM2OD13LkO5NlQ2KM7:TR?= M1rxTXNCVkeHUh?=
COLO-668 NFPmS|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\RTWM2OD13LkeyOlY4KM7:TR?= NE\ie4ZUSU6JRWK=
LB1047-RCC NVrQRZI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTVTWM2OD13LkiwNFQ3KM7:TR?= MWPTRW5ITVJ?
NB5 NH;POGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moq5TWM2OD14LkKxNFAyKM7:TR?= NGrlendUSU6JRWK=
NTERA-S-cl-D1 M4DwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTZwMk[1OlEh|ryP NI\m[nJUSU6JRWK=
IST-MEL1 M4LkTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTZwNEO2PVQh|ryP MUPTRW5ITVJ?
GI-1 M2TNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTZwNUG2PFIh|ryP MWnTRW5ITVJ?
TGBC1TKB NXTRco95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHyweY1KSzVyPUeuNFcyQDNizszN NYHhcXlTW0GQR1XS
GT3TKB NVrQcIl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4KxNWlEPTB;Nz6yNlc1PCEQvF2= MVfTRW5ITVJ?
EVSA-T MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPWclFyUUN3ME23MlQzQDFzIN88US=> M4WwZnNCVkeHUh?=
D-502MG Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2SxOWlEPTB;Nz60PFg6PCEQvF2= MYHTRW5ITVJ?
TE-8 MkLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTdwN{[xOVkh|ryP MmfnV2FPT0WU
OVCAR-4 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIixdI9KSzVyPUmuNVE3PzVizszN NXXpe4FUW0GQR1XS
D-336MG NFvOTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoW4TWM2OD17LkS3N|k2KM7:TR?= MoDLV2FPT0WU
GCIY NH;vZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\ybmJ7UUN3ME25MlU4PDJizszN NHm0Z2ZUSU6JRWK=
KS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXMepVIUUN3ME25MlY3Ojh5IN88US=> NXrNUHBOW0GQR1XS
HCC2998 M4TNfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT5c4NKSzVyPUmuPVY{ODdizszN NIn5VHJUSU6JRWK=
D-247MG NX;mfIR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\ifmlEPTB;OT65PFI6OSEQvF2= NGnISnpUSU6JRWK=
TE-15 NHPDWJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFyLkK0OUDPxE1? M{PUT3NCVkeHUh?=
IST-MES1 NGjGWZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTyU2VyUUN3ME2xNE4zPTZ3IN88US=> NFnMfIFUSU6JRWK=
ETK-1 M2XPcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTFyLk[yN{DPxE1? NFrWT2NUSU6JRWK=
RCC10RGB NVu1NldvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFyLkm2NUDPxE1? M2HyZnNCVkeHUh?=
KNS-42 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zBNmlEPTB;MUGuO|I2PSEQvF2= MnuxV2FPT0WU
LB771-HNC M{jHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfqOnBsUUN3ME2xNk4yPzF{IN88US=> NX34OmRZW0GQR1XS
SR NF\TOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF63[oNKSzVyPUGyMlIxPjRizszN M33KSnNCVkeHUh?=
NCI-H1355 M{XXS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7PTWM2OD1zMj64PVg2KM7:TR?= M{XR[nNCVkeHUh?=
ES6 M2DrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HMcWlEPTB;MUOuNFc5KM7:TR?= MoDGV2FPT0WU
SK-NEP-1 NWnU[5luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFmwOplKSzVyPUGzMlI2PzdizszN NGPwPVlUSU6JRWK=
D-392MG Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF|Lk[0Nlgh|ryP MkjwV2FPT0WU
NB7 M3HWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j3PGlEPTB;MUSuNlM4PCEQvF2= NYPwVVNkW0GQR1XS
SK-LMS-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5V2lEPTB;MUSuOVE1PSEQvF2= MnTDV2FPT0WU
SK-UT-1 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3voZmlEPTB;MUSuO|g5QSEQvF2= NUi3ZWVXW0GQR1XS
CA46 NX31T3RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly5TWM2OD1zNT6wOVg3KM7:TR?= MXLTRW5ITVJ?
IST-SL2 NGXCUYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrLTWM2OD1zNT6xPVAyKM7:TR?= NVmwVI1FW0GQR1XS
BC-1 NFnieW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLrSmNMUUN3ME2xOU4{OzF2IN88US=> NFH5cY5USU6JRWK=
LS-123 NXvSe|NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\3VmlEPTB;MUWuPFE4OyEQvF2= MkDyV2FPT0WU
Ramos-2G6-4C10 NXv4NnF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPjTWM2OD1zNj6wPVI1KM7:TR?= NXz0RXROW0GQR1XS
MZ1-PC Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;WcVNkUUN3ME2xOk44OzF|IN88US=> MWjTRW5ITVJ?
LB647-SCLC M1;uUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXh[HFKSzVyPUG2Mlk{PzJizszN NHTjWXdUSU6JRWK=
NCI-H1694 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPJVHlKSzVyPUG3MlE2OjlizszN M{TmeHNCVkeHUh?=
NCI-H322M MnyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXDPJZKSzVyPUG3MlQ{PjZizszN MUDTRW5ITVJ?
ES7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXGeoZKSzVyPUG4MlM6OTRizszN NH3QcopUSU6JRWK=
LC-2-ad MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDRTWM2OD1zOD60N|g3KM7:TR?= MWnTRW5ITVJ?
SF268 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnIfGlQUUN3ME2xPE44PDB7IN88US=> MXnTRW5ITVJ?
RPMI-8402 NXe5XFBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTF7LkC3OFIh|ryP M4TXOXNCVkeHUh?=
HCE-T M4PaTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK5VHRKSzVyPUKwMlI{PDRizszN MV3TRW5ITVJ?
A101D NXz2OFZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJyLki1PFch|ryP M2f5OnNCVkeHUh?=
MRK-nu-1 NW\sOHVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTYTWM2OD1{MD65NVMh|ryP NIPxelFUSU6JRWK=
LXF-289 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXOWI1NUUN3ME2yNU4xOzhizszN NHH4bmpUSU6JRWK=
NALM-6 NXXKPJNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13QV2lEPTB;MkGuNVk3PyEQvF2= M2DFS3NCVkeHUh?=
DOHH-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnt[GNPUUN3ME2yNU41QDF|IN88US=> MWrTRW5ITVJ?
EW-16 MlrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknQTWM2OD1{Mj6xOFAzKM7:TR?= NGOxcWZUSU6JRWK=
A4-Fuk MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rTfGlEPTB;MkKuNlE1QSEQvF2= MlnOV2FPT0WU
HD-MY-Z MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnYXIZQUUN3ME2yNk4{QTZ3IN88US=> M3vrNXNCVkeHUh?=
SKM-1 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJ{LkezOVEh|ryP M3;mTnNCVkeHUh?=
DMS-153 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXsfnU6UUN3ME2yN{41OjB2IN88US=> NH33bY5USU6JRWK=
LB373-MEL-D NFfsdGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV73VY1iUUN3ME2yN{42PDV{IN88US=> NGDINoxUSU6JRWK=
LP-1 M{LYUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnpWHRFUUN3ME2yN{45ODl5IN88US=> NXLZZZl{W0GQR1XS
GI-ME-N MnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ2LkK5NkDPxE1? M{G3RXNCVkeHUh?=
MPP-89 NFPzSG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWmybG9DUUN3ME2yOU4zODN4IN88US=> Mk\6V2FPT0WU
U-698-M MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\2TWM2OD1{NT6yOVA{KM7:TR?= M1K2WnNCVkeHUh?=
HC-1 NInKV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK0eVlKSzVyPUK1MlY1OThizszN MWrTRW5ITVJ?
HCC2157 NUfNeIs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TrUWlEPTB;MkWuOlc{KM7:TR?= NUHZTWZ{W0GQR1XS
MOLT-4 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX24UIhuUUN3ME2yOk4zPzNizszN M3fqS3NCVkeHUh?=
LS-411N MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjtclRsUUN3ME2yOk4{OzZ7IN88US=> M4TofXNCVkeHUh?=
Becker NW\qTWNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;LeYxKSzVyPUK2MlUyQDFizszN NHvVSHdUSU6JRWK=
NCI-H23 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C5fmlEPTB;Mk[uO|U4PSEQvF2= NUfB[JVoW0GQR1XS
IST-SL1 M1zUOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnj[ldKSzVyPUK3MlM5PjdizszN Mm\TV2FPT0WU
MZ2-MEL MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJ5LkS1OlYh|ryP NGSycWhUSU6JRWK=
RKO NVr5N|JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HOPWlEPTB;MkiuNVQ1PiEQvF2= MWXTRW5ITVJ?
TE-441-T NUjvWphYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJ6Lke4PUDPxE1? M1\6NHNCVkeHUh?=
EW-24 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fNWmlEPTB;MkmuNVI2QSEQvF2= M4XxTXNCVkeHUh?=
no-10 NX21TpI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXsdlRKSzVyPUK5MlE3OzFizszN NFHNenJUSU6JRWK=
D-542MG NFPoSGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL0TWM2OD1{OT65NlIyKM7:TR?= MonNV2FPT0WU
ST486 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLESYU{UUN3ME2zNE43PDVzIN88US=> MYPTRW5ITVJ?
KURAMOCHI M3LSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f1bmlEPTB;M{CuPFA2PyEQvF2= NWfTcmRvW0GQR1XS
ES8 NIfoV4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHPRm1KSzVyPUOxMlU6PzJizszN MnnUV2FPT0WU
BL-41 NWjlRlFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPUZnVoUUN3ME2zNk4yODV2IN88US=> NHPyenJUSU6JRWK=
NB6 NETZcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu1NVhKSzVyPUOyMlM5PTVizszN NV[xdmpMW0GQR1XS
NCI-H1304 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TGVGlEPTB;M{KuOFk3PyEQvF2= MlrQV2FPT0WU
MS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn6cZpCUUN3ME2zNk44PzVzIN88US=> MUnTRW5ITVJ?
MFH-ino MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPDTWM2OD1|ND6zNlI1KM7:TR?= Moe3V2FPT0WU
NOS-1 M1jpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;LT3pKSzVyPUO0MlY4PDhizszN MnzzV2FPT0WU
HUTU-80 M1L5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWruZ|ZrUUN3ME2zOU4{PjZ5IN88US=> MnjzV2FPT0WU
EB2 NX\5bGhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL1TWM2OD1|Nj62NVg6KM7:TR?= MnLoV2FPT0WU
L-540 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjiPYwyUUN3ME2zO{4zOzB6IN88US=> MVzTRW5ITVJ?
NCI-H747 NX;iPXlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\mdZlKSzVyPUO4Mlg5PDZizszN NHfpNINUSU6JRWK=
NCI-H446 MoTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT4OlY2UUN3ME2zPU46PjVzIN88US=> MnvVV2FPT0WU
MOLT-16 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR{LkSxOUDPxE1? M1uxNHNCVkeHUh?=
BC-3 MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTR3LkS4PVYh|ryP M{nwVXNCVkeHUh?=
SJSA-1 NF3pO3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPoTWM2OD12NT61OFc1KM7:TR?= MlLYV2FPT0WU
BB65-RCC M1nkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTR3Lk[2OkDPxE1? MY\TRW5ITVJ?
SNB75 MmDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDmTWM2OD12Nj6wNVgh|ryP NGrGepJUSU6JRWK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 ; 

PubMed: 29799521     


Downregulation of HSF1, mutp53, and Mdm2 in lapatinib-sensitive parental BT474, but not in lapatinib-resistant BT474R cells, treated with indicated lapatinib concentrations for 24 h.

pEGFR / EGFR / pAkt / Akt / pmTOR / 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. 

p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1; 

PubMed: 22853430     


A panel of HER2-amplified breast cancer cells were treated with 200nM lapatinib for up to 72 hours to detect the initial downregulation and subsequent upregulation of HER2-HER3 and downstream signaling. Immunoblots were performed using the indicated antibodies.

29799521 28938602 22853430
Immunofluorescence
LC3 ; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 6 days and UACC893 GFP-LC3 cells were cultured for 7 days with 5 μM EZN3046 or EZN4150 .

Vimentin / E-cadherin; 

PubMed: 28243326     


Cells treated with lapatinib (5µM) increased the expression of E-cadherin and inhibited the expression of Vimentin by immunofluorescence. (Magnification: 1000×).

26637440 28243326
Growth inhibition assay
Cell viability (OE19); 

PubMed: 25350844     


Dose-response curves from escalated dose of lapatinib in the presence of 1 µM concentration of saracatinib. The calculated values of IC50 for lapatinib were following; 207.3 nM and 145 nM, respectively, after lapatinib alone and in the presence of saracatinib for parental OE19; >1,000 nM after lapatinib alone for LR2A and LR2B; 91.66 nM and 224.0 nM in the presence of saracatinib in LR2A and LR2B, respectively. Values were presented as relative cellular viability relative to vehicle-treated controls with the mean ± S.E. of quadruplicate from a representative experiment. The p values calculated by two-way ANOVA were <0.0001 comparing lapatinib alone with lapatinib plus saracatinib both in the LR2A and LR2B.

Cell viability (A431 cells); 

PubMed: 28243326     


The MTT assay was performed on the viability of A431 cells by lapatinib at different concentrations (0.1-50μM) and IC50 value was analyzed as indicated on the plot (t-test).

25350844 28243326
体内研究 Lapatinib有效抑制BT474 和HN5 人类移植瘤生长。使用30和 100 mg/kg Lapatinib 口服给药携带肿瘤的小鼠,每天两次,抑制肿瘤生长,这种作用存在剂量依赖性。按100 mg/kg 剂量处理完全抑制肿瘤生长。按这种剂量处理,在处理21天期间,有<10%肿瘤损失。[1]

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EGFR, ErbB-2,和 ErbB4激酶实验 :

从杆状病毒表达系统中纯化EGFR, ErbB-2, 和 ErbB4的细胞内激酶域。EGFR, ErbB-2, 和 ErbB-4 反应在96孔聚苯乙烯圆底板中进行,终体积为45 μL。反应混合物含50 mM 4-吗啉基丙磺酸(pH 7.5), 2 mM MnCl2,10 μM ATP, 1 μCi [γ-33 P] ATP/每次反应,50 μM Peptide A [生物素-(氨基酸)-EEEEYFELVAKKK-CONH2],1 mM 二硫苏糖醇, 及 1 μL 含连续稀释Lapatinib(初浓度为10 μM)的 DMSO。加入指定纯化的1型受体细胞内域开始反应。加入的酶量为1 pmol/每次反应 (20 nM)。在23oC反应10分钟,加入溶于水的 45 μL 0.5% 磷酸后,终止反应。最终反应混合物(75 μL) 转移到磷酸纤维素过滤板上。过滤实验板,使用200 μL 0.5% 磷酸冲洗三次。每孔中加入闪烁混合物(50 μL),使用Packard Topcount计数而量化实验结果。
细胞实验:[1]
- 合并
  • Cell lines: HFF , BT474, MCF-7, N87, CaLu-3, HN5, A-431, T47D, HB4a, 和 HB4a c5.2
  • Concentrations: 0 到 100 nM
  • Incubation Time: 3 天
  • Method: 按以下密度接种细胞:HFF, 1.5×104 个细胞/cm2; BT474, MCF-7, N87, 和 CaLu-3, 3×104 个细胞/cm2; 及HN5, A-431, T47D, HB4a, 和 HB4a c5.2, 1×104 个细胞/cm2,使在实验期间细胞处于对数生长期。24 小时后,使用浓度范围为0 到 100 nM的Lapatinib处理细胞。在含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM培养基中处理HFF, BT474,HN5, 和 N87 细胞。在50% 高糖DMEM,和50%含5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的低糖DMEM中处理MCF-7细胞。在 50% RPMI,50%含 5% FBS, 50 μg/mL gentamicin, 和 0.3% v/v DMSO 的低糖DMEM中处理T47D, A-431, 和CaLu-3 细胞。在50% DMEM, 50% 含5% FBS, 2.5 μg/mL hydrocortisone, 2.5 μg/mL 胰岛素, 25 μg/mL hygromycin B, 50 μg/mL gentamicin, 和 0.3% v/v DMSO的RPMI 1640中处理HB4a 和 HB4a c5.2细胞。3天后, 使用亚甲基蓝染色测评相对细胞数。移除培养基,每孔加入溶解在 50% 乙醇和50% 水中的100 μL 0.5% w/v亚甲基蓝。浸泡在去离子水中洗涤实验板,然后在空气中烘干。每孔加入溶解在PBS的1% w/v n-lauroylsarcosine(100 μL), 然后实验板在室温下温育30分钟。使用Spectra酶标仪在620 nm处测定吸光值。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 雌性CD-1裸鼠和雌性C.B-17 SCID 小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服,每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (172.09 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+5% Tween 80+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 581.06
化学式

C29H26ClFN4O4S

CAS号 231277-92-2
储存条件 粉状
溶于溶剂
别名 GW-572016, GSK572016

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 want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

  • 回答:

    For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID