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。

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RMB 1171.97 现货
RMB 903.45 现货
RMB 2192.38 现货
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客户使用Selleck该产品发表文献42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 M1;pUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C3dGlEPTB;MD6wNlU1PCEQvF2= MYHTRW5ITVJ?
HCC2218 NXPZZoJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLwRppxUUN3ME2wMlA2OzJ4IN88US=> MlrDV2FPT0WU
OCUB-M NXKzSGc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwMEW3OEDPxE1? NInkbXpUSU6JRWK=
ECC12 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HaeWlEPTB;MD6wPVI{OSEQvF2= NF\pbXZUSU6JRWK=
DSH1 NHjDSnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMEmzPVYh|ryP M4nhfHNCVkeHUh?=
BT-474 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1juVGlEPTB;MD6yNVMyPSEQvF2= NHXPb2lUSU6JRWK=
BB30-HNC NYHTS2lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwMkS2OVQh|ryP NWHOOWtKW0GQR1XS
EKVX MnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXF[XhnUUN3ME2wMlQ1QDd2IN88US=> MkL3V2FPT0WU
TE-12 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf2TVhKSzVyPUCuOFkxPTdizszN Mn:yV2FPT0WU
A388 M2\m[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwN{KyOVgh|ryP NEnT[GZUSU6JRWK=
TE-9 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHHZotKSzVyPUCuO|Q1PTNizszN MV\TRW5ITVJ?
LB2241-RCC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwMUW0NFMh|ryP M1flSXNCVkeHUh?=
LB996-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHThbWpKSzVyPUGuN|YzOjhizszN M4HTNnNCVkeHUh?=
LC-1F M3u4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\XUnlGUUN3ME2xMlM5OjR2IN88US=> MlWxV2FPT0WU
TE-6 NVHIblk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K4bWlEPTB;MT61OVIxOSEQvF2= Mny4V2FPT0WU
A253 M1GzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3Yd|hvUUN3ME2xMlk4OzN3IN88US=> M3;kXHNCVkeHUh?=
OS-RC-2 M3:z[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzZeo1vUUN3ME2xMlk6OTl7IN88US=> NH7hR4tUSU6JRWK=
TE-1 M4DoR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJwMES4N{DPxE1? NWToZXFlW0GQR1XS
RL95-2 MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfBSWtJUUN3ME2zMlE2PjdizszN MVvTRW5ITVJ?
LS-513 Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTNwNECwOFEh|ryP Mmf5V2FPT0WU
DJM-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHNcWxlUUN3ME2zMlQ3QTd3IN88US=> NUnsN3g6W0GQR1XS
NMC-G1 NV3PWGFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LtZWlEPTB;Mz61OFUxOSEQvF2= M3\acnNCVkeHUh?=
TE-10 M2\ZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj5ephKSzVyPUOuOVU{PTZizszN Mmj1V2FPT0WU
TE-5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTRwMEO3N{DPxE1? NIHTTldUSU6JRWK=
TK10 MkexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPmOGllUUN3ME20MlE3PTJ{IN88US=> MV3TRW5ITVJ?
UACC-812 M1f3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LJZmlEPTB;ND61OlE2OyEQvF2= NWW5XFRxW0GQR1XS
SW962 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHIWplKSzVyPUWuNFIyPTlizszN NVPkNWFGW0GQR1XS
SW954 M4LkZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XtTmlEPTB;NT6zPVI1PSEQvF2= NF;KVFlUSU6JRWK=
COLO-668 NEXQXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHHeJdKSzVyPUWuO|I3PjdizszN NVLBclJHW0GQR1XS
LB1047-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjCUYJOUUN3ME21MlgxODR4IN88US=> NGq1U5FUSU6JRWK=
NB5 NHHDcW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;ufGlEPTB;Nj6yNVAxOSEQvF2= MY\TRW5ITVJ?
NTERA-S-cl-D1 MlrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXyWVFKSzVyPU[uNlY2PjFizszN NEfSOYVUSU6JRWK=
IST-MEL1 NEDafGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonzTWM2OD14LkSzOlk1KM7:TR?= NUnLN3Y1W0GQR1XS
GI-1 NFHDbFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[0UVRKSzVyPU[uOVE3QDJizszN NV[0RVZGW0GQR1XS
TGBC1TKB NHzXNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;DOW5KSzVyPUeuNFcyQDNizszN NGj2UFVUSU6JRWK=
GT3TKB Ml6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnnb2tIUUN3ME23MlIzPzR2IN88US=> NFXtXHpUSU6JRWK=
EVSA-T NEG5[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf6bIlKSzVyPUeuOFI5OTFizszN Mom3V2FPT0WU
D-502MG M2i5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXk[JZYUUN3ME23MlQ5QDl2IN88US=> Mn74V2FPT0WU
TE-8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO5bmtKSzVyPUeuO|YyPTlizszN MX7TRW5ITVJ?
OVCAR-4 NVzT[Vk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;Re2tPUUN3ME25MlEyPjd3IN88US=> MUHTRW5ITVJ?
D-336MG NUmyOFZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnSXY1KSzVyPUmuOFc{QTVizszN MYXTRW5ITVJ?
GCIY MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\YPY4zUUN3ME25MlU4PDJizszN MkTRV2FPT0WU
KS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTlwNk[yPFch|ryP MYTTRW5ITVJ?
HCC2998 MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXZZpdKSzVyPUmuPVY{ODdizszN MYrTRW5ITVJ?
D-247MG M3LGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf0S|h[UUN3ME25Mlk5OjlzIN88US=> NYr5NJFOW0GQR1XS
TE-15 M3LZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjxTWM2OD1zMD6yOFUh|ryP Mn;4V2FPT0WU
IST-MES1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PqWWlEPTB;MUCuNlU3PSEQvF2= NHqzfYJUSU6JRWK=
ETK-1 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH4TWM2OD1zMD62NlMh|ryP MlTJV2FPT0WU
RCC10RGB M3zEUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFyLkm2NUDPxE1? NIHrSZBUSU6JRWK=
KNS-42 NXi3O|BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\nV2lEPTB;MUGuO|I2PSEQvF2= NWrzO|VyW0GQR1XS
LB771-HNC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzye21ZUUN3ME2xNk4yPzF{IN88US=> MljKV2FPT0WU
SR NHzGeG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LYPGlEPTB;MUKuNlA3PCEQvF2= MW\TRW5ITVJ?
NCI-H1355 M3zWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF{Lki5PFUh|ryP NH3nSopUSU6JRWK=
ES6 MmX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4njbGlEPTB;MUOuNFc5KM7:TR?= M{PWTXNCVkeHUh?=
SK-NEP-1 NG\TTIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rQWmlEPTB;MUOuNlU4PyEQvF2= M2mwenNCVkeHUh?=
D-392MG NEfDPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[1eFBmUUN3ME2xN{43PDJ6IN88US=> NWXMVZViW0GQR1XS
NB7 M1zud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rmcGlEPTB;MUSuNlM4PCEQvF2= M4XpUnNCVkeHUh?=
SK-LMS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPYTWM2OD1zND61NVQ2KM7:TR?= NUflUVRNW0GQR1XS
SK-UT-1 NFTiepdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTF2Lke4PFkh|ryP MXTTRW5ITVJ?
CA46 M{m4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv0TWM2OD1zNT6wOVg3KM7:TR?= NI\Ge|hUSU6JRWK=
IST-SL2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrz[olKSzVyPUG1MlE6ODFizszN MWrTRW5ITVJ?
BC-1 M3vLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2xTWM2OD1zNT6zN|E1KM7:TR?= M1zNVHNCVkeHUh?=
LS-123 M2\TRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DOTGlEPTB;MUWuPFE4OyEQvF2= NIjUOFVUSU6JRWK=
Ramos-2G6-4C10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPuXHlKSzVyPUG2MlA6OjRizszN NGrjNlRUSU6JRWK=
MZ1-PC M{n2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjBUWlKSzVyPUG2Mlc{OTNizszN MlLXV2FPT0WU
LB647-SCLC MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHwfJg1UUN3ME2xOk46Ozd{IN88US=> MWTTRW5ITVJ?
NCI-H1694 M2rHS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIixcmJKSzVyPUG3MlE2OjlizszN M1jS[XNCVkeHUh?=
NCI-H322M NF6yN3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTP[m5kUUN3ME2xO{41OzZ4IN88US=> NEjBeJlUSU6JRWK=
ES7 NEDUZXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHCTWM2OD1zOD6zPVE1KM7:TR?= NGLGOI1USU6JRWK=
LC-2-ad MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPpTWM2OD1zOD60N|g3KM7:TR?= MlHyV2FPT0WU
SF268 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVziWYtbUUN3ME2xPE44PDB7IN88US=> NUnOV25JW0GQR1XS
RPMI-8402 M1SzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXNUnVKSzVyPUG5MlA4PDJizszN NWHqRlRVW0GQR1XS
HCE-T MnHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH2TWM2OD1{MD6yN|Q1KM7:TR?= MWXTRW5ITVJ?
A101D M1;qTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlq3TWM2OD1{MD64OVg4KM7:TR?= MmTlV2FPT0WU
MRK-nu-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITNZ|ZKSzVyPUKwMlkyOyEQvF2= NHXhdVZUSU6JRWK=
LXF-289 NYj6ZmZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrPZpFKSzVyPUKxMlA{QCEQvF2= NEHNVWNUSU6JRWK=
NALM-6 NF75UXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\qTWlEPTB;MkGuNVk3PyEQvF2= NVPVXm9CW0GQR1XS
DOHH-2 M1\OXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHOTWM2OD1{MT60PFE{KM7:TR?= NIjJRZdUSU6JRWK=
EW-16 M37wNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ{LkG0NFIh|ryP M2Ow[XNCVkeHUh?=
A4-Fuk Ml7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fqO2lEPTB;MkKuNlE1QSEQvF2= M{Ow[3NCVkeHUh?=
HD-MY-Z M{TVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ{LkO5OlUh|ryP NY\m[YU1W0GQR1XS
SKM-1 NY\IN25YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPnTWM2OD1{Mj63N|UyKM7:TR?= MmPsV2FPT0WU
DMS-153 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLH[JdPUUN3ME2yN{41OjB2IN88US=> M2P2UXNCVkeHUh?=
LB373-MEL-D NFWwcFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTJ|LkW0OVIh|ryP NVzXcml5W0GQR1XS
LP-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3KeoRKSzVyPUKzMlgxQTdizszN NIXBc3ZUSU6JRWK=
GI-ME-N NFy3coJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L6c2lEPTB;MkSuNlkzKM7:TR?= NXniTYt7W0GQR1XS
MPP-89 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrOXIpKSzVyPUK1MlIxOzZizszN MoXJV2FPT0WU
U-698-M MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJ3LkK1NFMh|ryP NV64PXJjW0GQR1XS
HC-1 Mn3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTJ3Lk[0NVgh|ryP M1u1SnNCVkeHUh?=
HCC2157 NV3xU3lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJ3Lk[3N{DPxE1? M2LsNXNCVkeHUh?=
MOLT-4 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\4N4ZGUUN3ME2yOk4zPzNizszN MnvsV2FPT0WU
LS-411N NE[zfIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTJ4LkOzOlkh|ryP NVWxWYJbW0GQR1XS
Becker MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDtNGpKSzVyPUK2MlUyQDFizszN NGDKNGpUSU6JRWK=
NCI-H23 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTVfopKSzVyPUK2Mlc2PzVizszN MlPlV2FPT0WU
IST-SL1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXXU2tKSzVyPUK3MlM5PjdizszN M{jWS3NCVkeHUh?=
MZ2-MEL Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;hTWM2OD1{Nz60OVY3KM7:TR?= M{XCS3NCVkeHUh?=
RKO NFTjUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK2[YVoUUN3ME2yPE4yPDR4IN88US=> M4LoZnNCVkeHUh?=
TE-441-T NU\w[ld3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXZZpRxUUN3ME2yPE44QDlizszN M4jETXNCVkeHUh?=
EW-24 NHzYUJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DJPWlEPTB;MkmuNVI2QSEQvF2= MljXV2FPT0WU
no-10 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\sTWM2OD1{OT6xOlMyKM7:TR?= MWLTRW5ITVJ?
D-542MG MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ7LkmyNlEh|ryP NGn0dppUSU6JRWK=
ST486 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTNyLk[0OVEh|ryP M4PjTXNCVkeHUh?=
KURAMOCHI MojES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjEdZdKSzVyPUOwMlgxPTdizszN M3fxRXNCVkeHUh?=
ES8 NWmwRmVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTNzLkW5O|Ih|ryP NX\ZVmpuW0GQR1XS
BL-41 M4XJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7YTWM2OD1|Mj6xNFU1KM7:TR?= MknDV2FPT0WU
NB6 NVPGWXp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTN{LkO4OVUh|ryP NUHRe25lW0GQR1XS
NCI-H1304 NXzvWWdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3nTWM2OD1|Mj60PVY4KM7:TR?= NIW2c4tUSU6JRWK=
MS-1 MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHjU|NKSzVyPUOyMlc4PTFizszN Mle3V2FPT0WU
MFH-ino M{DFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTGTWM2OD1|ND6zNlI1KM7:TR?= MoLsV2FPT0WU
NOS-1 Ml3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLLcppKSzVyPUO0MlY4PDhizszN MV\TRW5ITVJ?
HUTU-80 NGjOboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTN3LkO2Olch|ryP M4GyWXNCVkeHUh?=
EB2 Ml7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjxSFRKSzVyPUO2MlYyQDlizszN MXHTRW5ITVJ?
L-540 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfuVFRKSzVyPUO3MlI{ODhizszN NFLnT3NUSU6JRWK=
NCI-H747 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTW[I1nUUN3ME2zPE45QDR4IN88US=> NHrrXmZUSU6JRWK=
NCI-H446 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXqSY9KSzVyPUO5Mlk3PTFizszN NGnidnhUSU6JRWK=
MOLT-16 NEjZZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDDTWM2OD12Mj60NVUh|ryP MX3TRW5ITVJ?
BC-3 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfDdJNKSzVyPUS1MlQ5QTZizszN Ml33V2FPT0WU
SJSA-1 M1PXPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfqV5BKSzVyPUS1MlU1PzRizszN NEO4eVdUSU6JRWK=
BB65-RCC NVrjVYVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLZTWM2OD12NT62OlYh|ryP NIXCOppUSU6JRWK=
SNB75 Mnr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTYTWM2OD12Nj6wNVgh|ryP NWXFV4c2W0GQR1XS

... 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,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
稳定性 powder
in solvent
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
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03523585 Recruiting Breast Cancer Daiichi Sankyo Inc.|Daiichi Sankyo Co. Ltd. August 1 2018 Phase 3
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2
NCT03500380 Recruiting Breast Neoplasms|Breast Diseases|Capecitabine|HER2-positive Breast Cancer|HER2 Positive Breast Carcinoma RemeGen April 2018 Phase 2

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