Lapatinib

目录号:S2111 别名: GW-572016, GSK572016

Lapatinib Chemical Structure

Molecular Weight(MW): 581.06

Lapatinib,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。

规格 价格 库存 购买数量  
RMB 1171.97 现货
RMB 903.45 现货
RMB 2192.38 现货
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客户购买Selleck的此次产品后发表的文献38篇:

客户使用该产品的7个实验数据:

  • Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice).

    Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck.

    Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies.

    Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck.

  • Inhibition of HER2 using siRNAs show a similar response measured by induced apoptosis, decreased proliferation and decreased phospho-p70-S6K staining as Lapatinib mono-treatment and combinatorial treatment with Lapatinib and trastuzumab. Trastuzumab mono-treatment is less efficient than siHER2.

    Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck.

    Lapatinib effectively inhibits EGFR activation, leading to a reduc- tion in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 μM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck.

  •  

    Endogenous associations between STAT1, EGFR, and p-STAT3 expression in breast cancer cells. (B) Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression. MDA-MB-468 cells with endogenous expression of EGFR and STAT3 were treated with 25 uM lapatinib for 24 h, harvested and subjected to western blotting for EGFR, p-EGFR, and STAT1 expression.

    Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck.

    Combination treatment with lapatinib and CZ0775 significantly induces pro-apoptotic BIM proteins in H195 cells. HCC827 (a) and H1975 (b) cells were treated with either 1 μM lapatinib alone or the combination of 1 μM lapatinib plus 1 μM AZD6244 or CZ0775 for 24 h. Cell lysates were analyzed by Western blotting using the indicated antibodies. The levels of β -actin served as a loading control

    Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck.

  •  

    EGF and TGF-α-induced CD44 expression is reduced by EGFR inhibitors in SKBR3 breast cancer cells. After serum-starvation for 24 h, the cells were pretreated with EGFR inhibitors, AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then, treated with EGF (A) or TGF-α (B) for 24 h. The level of CD44 mRNA expression was analyzed by real-time PCR. After serum-starvation for 24 h, the cells were pretreated with AG1478 or lapatinib for 30 min prior to EGF or TGF-α treatment and then treated with EGF for 24 h (C). The levels of CD44, EGFR, ERK, and β-actin protein expression were analyzed by Western blotting.

    Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck.

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,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。
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 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMEK1OFQh|ryP MnjBV2FPT0WU
HCC2218 NEjVVnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[3TWM2OD1yLkC1N|I3KM7:TR?= NWTUNIQxW0GQR1XS
OCUB-M NF\mb2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHJTFB2UUN3ME2wMlA2PzRizszN NH7tfmVUSU6JRWK=
ECC12 NYK3[4FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O1R2lEPTB;MD6wPVI{OSEQvF2= NHL4NpJUSU6JRWK=
DSH1 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorrTWM2OD1yLkC5N|k3KM7:TR?= MmLQV2FPT0WU
BT-474 MmjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv1OYlrUUN3ME2wMlIyOzF3IN88US=> M3\UOHNCVkeHUh?=
BB30-HNC MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMkS2OVQh|ryP NH7JUZlUSU6JRWK=
EKVX M2\R[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:xTWM2OD1yLkS0PFc1KM7:TR?= MYLTRW5ITVJ?
TE-12 M2DX[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrFWWFYUUN3ME2wMlQ6ODV5IN88US=> NIixc5RUSU6JRWK=
A388 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHOTWM2OD1yLkeyNlU5KM7:TR?= MULTRW5ITVJ?
TE-9 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jHTmlEPTB;MD63OFQ2OyEQvF2= NHr2TZZUSU6JRWK=
LB2241-RCC NGDUTGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj2bGpUUUN3ME2xMlE2PDB|IN88US=> NFTzSpRUSU6JRWK=
LB996-RCC NVPDXoV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r6fWlEPTB;MT6zOlIzQCEQvF2= M2XxeHNCVkeHUh?=
LC-1F NUTpdZJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG2TWM2OD1zLkO4NlQ1KM7:TR?= MUXTRW5ITVJ?
TE-6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTLSngxUUN3ME2xMlU2OjBzIN88US=> M3frR3NCVkeHUh?=
A253 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnoTWM2OD1zLkm3N|M2KM7:TR?= MnrSV2FPT0WU
OS-RC-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonTTWM2OD1zLkm5NVk6KM7:TR?= NXzhWpJ7W0GQR1XS
TE-1 NV:zVnlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPoTWM2OD1{LkC0PFMh|ryP NF;NcXJUSU6JRWK=
RL95-2 MmexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTNwMUW2O{DPxE1? M3LpOXNCVkeHUh?=
LS-513 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LZ[WlEPTB;Mz60NFA1OSEQvF2= M17FUXNCVkeHUh?=
DJM-1 NIr0WmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonsTWM2OD1|LkS2PVc2KM7:TR?= M3HuTXNCVkeHUh?=
NMC-G1 M3i0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnLZos1UUN3ME2zMlU1PTBzIN88US=> NFjHVJpUSU6JRWK=
TE-10 M{jIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILIdpNKSzVyPUOuOVU{PTZizszN MXrTRW5ITVJ?
TE-5 NXjUS|BqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fKNmlEPTB;ND6wN|c{KM7:TR?= NHHCfIRUSU6JRWK=
TK10 NXHEOnM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELsXmhKSzVyPUSuNVY2OjJizszN Ml62V2FPT0WU
UACC-812 M4DXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\MOnBiUUN3ME20MlU3OTV|IN88US=> MX7TRW5ITVJ?
SW962 NETUdpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrnUmVKSzVyPUWuNFIyPTlizszN MULTRW5ITVJ?
SW954 NVHQN2NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnO[3lKSzVyPUWuN|kzPDVizszN M{LTV3NCVkeHUh?=
COLO-668 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWTWM2OD13LkeyOlY4KM7:TR?= NVzWZ2xCW0GQR1XS
LB1047-RCC M2G3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUCwZ2gzUUN3ME21MlgxODR4IN88US=> NUXGTXR4W0GQR1XS
NB5 NE\GN5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTZwMkGwNFEh|ryP Mn31V2FPT0WU
NTERA-S-cl-D1 NHS1NG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GybmlEPTB;Nj6yOlU3OSEQvF2= Ml7mV2FPT0WU
IST-MEL1 NEGxOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fMPWlEPTB;Nj60N|Y6PCEQvF2= NUfFOXNrW0GQR1XS
GI-1 NWe3XpJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jJT2lEPTB;Nj61NVY5OiEQvF2= M3KzSHNCVkeHUh?=
TGBC1TKB NHLWVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13lVWlEPTB;Nz6wO|E5OyEQvF2= NVzzbZhNW0GQR1XS
GT3TKB MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInjfGFKSzVyPUeuNlI4PDRizszN M4LRdXNCVkeHUh?=
EVSA-T M2HmdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGG3[WdKSzVyPUeuOFI5OTFizszN NYDrVGxnW0GQR1XS
D-502MG M{exXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LFNGlEPTB;Nz60PFg6PCEQvF2= M1Pt[nNCVkeHUh?=
TE-8 NFLPWYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3IO3E6UUN3ME23Mlc3OTV7IN88US=> NEKzWlRUSU6JRWK=
OVCAR-4 M{\jVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGSwVIpKSzVyPUmuNVE3PzVizszN MV\TRW5ITVJ?
D-336MG NHf0R|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvGXVlKSzVyPUmuOFc{QTVizszN M4jTWXNCVkeHUh?=
GCIY NUPIdmU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe1THZKSzVyPUmuOVc1OiEQvF2= MnfGV2FPT0WU
KS-1 NXvETHhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTlwNk[yPFch|ryP NXrINYxMW0GQR1XS
HCC2998 NXO2RmlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7FOY9KSzVyPUmuPVY{ODdizszN NWTvNGllW0GQR1XS
D-247MG NVn0VXRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDBelRnUUN3ME25Mlk5OjlzIN88US=> M{fWRnNCVkeHUh?=
TE-15 NVHKc5FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTFyLkK0OUDPxE1? MkW4V2FPT0WU
IST-MES1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFyLkK1OlUh|ryP NFfUfJNUSU6JRWK=
ETK-1 NUDHPIl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFyLk[yN{DPxE1? MlnSV2FPT0WU
RCC10RGB M3HON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLpSnNKSzVyPUGwMlk3OSEQvF2= MVXTRW5ITVJ?
KNS-42 M1HmbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILLNlhKSzVyPUGxMlczPTVizszN NGXJUHBUSU6JRWK=
LB771-HNC NFTQWIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF{LkG3NVIh|ryP NWr6UGRzW0GQR1XS
SR Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G1SGlEPTB;MUKuNlA3PCEQvF2= NF;PeYtUSU6JRWK=
NCI-H1355 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLT[W1KSzVyPUGyMlg6QDVizszN NWrBXJY4W0GQR1XS
ES6 NIXs[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn75TWM2OD1zMz6wO|gh|ryP NFT3fJdUSU6JRWK=
SK-NEP-1 NVqyZZRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTybmVlUUN3ME2xN{4zPTd5IN88US=> NYDqO2czW0GQR1XS
D-392MG M1nD[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUGxdVBsUUN3ME2xN{43PDJ6IN88US=> MWLTRW5ITVJ?
NB7 M1;2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP6eohKSzVyPUG0MlI{PzRizszN Mo\VV2FPT0WU
SK-LMS-1 NIfOZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjZe4lKSzVyPUG0MlUyPDVizszN M3PIR3NCVkeHUh?=
SK-UT-1 NYjvXGQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF2Lke4PFkh|ryP Ml3BV2FPT0WU
CA46 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFize4ZKSzVyPUG1MlA2QDZizszN NGfSUZFUSU6JRWK=
IST-SL2 NWe0cWdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\PWFBzUUN3ME2xOU4yQTBzIN88US=> MVjTRW5ITVJ?
BC-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjkOoN6UUN3ME2xOU4{OzF2IN88US=> NF7zepdUSU6JRWK=
LS-123 NFztfWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnGUIZKSzVyPUG1MlgyPzNizszN NHvPN2lUSU6JRWK=
Ramos-2G6-4C10 M{Lw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH1PWZOUUN3ME2xOk4xQTJ2IN88US=> NYK1dmlGW0GQR1XS
MZ1-PC NHLnRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HhNmlEPTB;MU[uO|MyOyEQvF2= MoLjV2FPT0WU
LB647-SCLC NXHyV5dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkm5TWM2OD1zNj65N|czKM7:TR?= M1LBcHNCVkeHUh?=
NCI-H1694 M{nlcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PNOGlEPTB;MUeuNVUzQSEQvF2= MXfTRW5ITVJ?
NCI-H322M MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3nTWM2OD1zNz60N|Y3KM7:TR?= NInjOWJUSU6JRWK=
ES7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rVT2lEPTB;MUiuN|kyPCEQvF2= MlTRV2FPT0WU
LC-2-ad M3fEPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFz4V5NKSzVyPUG4MlQ{QDZizszN M4\xS3NCVkeHUh?=
SF268 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojJTWM2OD1zOD63OFA6KM7:TR?= MnnRV2FPT0WU
RPMI-8402 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTF7LkC3OFIh|ryP NVWweVRzW0GQR1XS
HCE-T NYflenBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn6xTWM2OD1{MD6yN|Q1KM7:TR?= Mli3V2FPT0WU
A101D MnnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJyLki1PFch|ryP NIr4PI1USU6JRWK=
MRK-nu-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJyLkmxN{DPxE1? MW\TRW5ITVJ?
LXF-289 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrGTWM2OD1{MT6wN|gh|ryP MWTTRW5ITVJ?
NALM-6 NUL6TXd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPNWGhKSzVyPUKxMlE6PjdizszN M1G0NXNCVkeHUh?=
DOHH-2 NUnLcZFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV25UHVmUUN3ME2yNU41QDF|IN88US=> MoDqV2FPT0WU
EW-16 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ{LkG0NFIh|ryP M2LTO3NCVkeHUh?=
A4-Fuk NY\oeWFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL4VJFKSzVyPUKyMlIyPDlizszN MW\TRW5ITVJ?
HD-MY-Z MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVu0SlhNUUN3ME2yNk4{QTZ3IN88US=> NEPpcYVUSU6JRWK=
SKM-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTTTWM2OD1{Mj63N|UyKM7:TR?= NEjBb2VUSU6JRWK=
DMS-153 NEnxO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rEWmlEPTB;MkOuOFIxPCEQvF2= M1:zdHNCVkeHUh?=
LB373-MEL-D MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ|LkW0OVIh|ryP MXrTRW5ITVJ?
LP-1 NEfhUG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjzOGtKSzVyPUKzMlgxQTdizszN M33mb3NCVkeHUh?=
GI-ME-N MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULBNnNnUUN3ME2yOE4zQTJizszN NG\wU2NUSU6JRWK=
MPP-89 MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H0PWlEPTB;MkWuNlA{PiEQvF2= Ml25V2FPT0WU
U-698-M NEP0RZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzY[2dKSzVyPUK1MlI2ODNizszN NETt[XdUSU6JRWK=
HC-1 NVfMe3BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJ3Lk[0NVgh|ryP MU\TRW5ITVJ?
HCC2157 M{fZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJ3Lk[3N{DPxE1? NVrnNI16W0GQR1XS
MOLT-4 MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTrTWM2OD1{Nj6yO|Mh|ryP NEf2cItUSU6JRWK=
LS-411N M2T6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ4LkOzOlkh|ryP M1v5S3NCVkeHUh?=
Becker M2P2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXrNlBiUUN3ME2yOk42OThzIN88US=> MlvQV2FPT0WU
NCI-H23 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ4Lke1O|Uh|ryP NIH6RVlUSU6JRWK=
IST-SL1 NX72VG9{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOwTWM2OD1{Nz6zPFY4KM7:TR?= NIT3[IRUSU6JRWK=
MZ2-MEL NYH3Wph3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jXW2lEPTB;MkeuOFU3PiEQvF2= MVjTRW5ITVJ?
RKO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfDPGliUUN3ME2yPE4yPDR4IN88US=> MWnTRW5ITVJ?
TE-441-T MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v2ZmlEPTB;MkiuO|g6KM7:TR?= MVLTRW5ITVJ?
EW-24 M3PGOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJ7LkGyOVkh|ryP MVLTRW5ITVJ?
no-10 MojPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJ7LkG2N|Eh|ryP Mkm0V2FPT0WU
D-542MG MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJ7LkmyNlEh|ryP M{fSNnNCVkeHUh?=
ST486 M3nJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTCdY1HUUN3ME2zNE43PDVzIN88US=> M1jiWnNCVkeHUh?=
KURAMOCHI NUHXfYt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P2RmlEPTB;M{CuPFA2PyEQvF2= NEPEZoVUSU6JRWK=
ES8 NF\RVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\QTWM2OD1|MT61PVczKM7:TR?= MX7TRW5ITVJ?
BL-41 NY\oPZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTMO4ZzUUN3ME2zNk4yODV2IN88US=> NF3XOYlUSU6JRWK=
NB6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fu[WlEPTB;M{KuN|g2PSEQvF2= M4f0W3NCVkeHUh?=
NCI-H1304 M1vHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjXOVFKSzVyPUOyMlQ6PjdizszN M2rRPHNCVkeHUh?=
MS-1 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vyemlEPTB;M{KuO|c2OSEQvF2= MWTTRW5ITVJ?
MFH-ino NGjwdWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT0cIN6UUN3ME2zOE4{OjJ2IN88US=> M4ezOnNCVkeHUh?=
NOS-1 NVnFcHVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3tOFJKSzVyPUO0MlY4PDhizszN M3PzNnNCVkeHUh?=
HUTU-80 NEnDcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLNTWM2OD1|NT6zOlY4KM7:TR?= NY[2bXF7W0GQR1XS
EB2 NVzZWphmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TEcWlEPTB;M{[uOlE5QSEQvF2= NUjxVo9QW0GQR1XS
L-540 NWPXb2xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXsVnJwUUN3ME2zO{4zOzB6IN88US=> NFG3OHJUSU6JRWK=
NCI-H747 NIj3b3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v6OGlEPTB;M{iuPFg1PiEQvF2= MnrFV2FPT0WU
NCI-H446 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHizdHNKSzVyPUO5Mlk3PTFizszN MnLjV2FPT0WU
MOLT-16 NFfwbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjY[XdDUUN3ME20Nk41OTVizszN NV33eXhLW0GQR1XS
BC-3 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7MRY1KSzVyPUS1MlQ5QTZizszN M3nrTHNCVkeHUh?=
SJSA-1 NFfvRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTR3LkW0O|Qh|ryP MYLTRW5ITVJ?
BB65-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\WPIY1UUN3ME20OU43PjZizszN NHfjUmVUSU6JRWK=
SNB75 Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y5TmlEPTB;NE[uNFE5KM7:TR?= M3S5Z3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

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]
+ 展开

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]
+ 展开
  • 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]
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  • Animal Models: 雌性CD-1裸鼠和雌性C.B-17 SCID 小鼠
  • Formulation: 磺丁基醚-β-环糊精的10%水溶液
  • 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:
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
稳定性 powder
别名 GW-572016, GSK572016

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT00107003 Completed Glioma|Brain Tumor|Glioblastoma Multiforme|GBM|Gliosarcoma|GS National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 30, 2005 Phase 2
NCT00251433 Active, not recruiting Neoplasms, Breast Novartis Pharmaceuticals|Novartis September 26, 2005 Phase 1
NCT01306045 Recruiting Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 21, 2011 Phase 2
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|Phase 2
NCT02836847 Recruiting Cholangiocarcinoma of the Extrahepatic Bile Duct|Gallbladder Cancer Shanghai Jiao Tong University School of Medicine|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Ruijin Hospital|RenJi Hospital|Eastern Hepatobiliary Surgery Hospital|Huashan Hospital July 2016 Phase 2
NCT02650752 Recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 2016 Phase 1

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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EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID