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 NEjnW|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\M[GFSUUN3ME2wMlAzPTR2IN88US=> MWLTRW5ITVJ?
HCC2218 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMEWzNlYh|ryP NI\tZ4ZUSU6JRWK=
OCUB-M NWO2TJN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4G1dGlEPTB;MD6wOVc1KM7:TR?= M3\yfnNCVkeHUh?=
ECC12 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwMEmyN|Eh|ryP M3;zV3NCVkeHUh?=
DSH1 M4q5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjPPY5KSzVyPUCuNFk{QTZizszN NWPINGk{W0GQR1XS
BT-474 NFTNWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLNTWM2OD1yLkKxN|E2KM7:TR?= M{\1fXNCVkeHUh?=
BB30-HNC NWiyVnVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPMZVR1UUN3ME2wMlI1PjV2IN88US=> NUe5UodRW0GQR1XS
EKVX NYjnWm5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzoNFZKSzVyPUCuOFQ5PzRizszN MWfTRW5ITVJ?
TE-12 NH;FeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwNEmwOVch|ryP NHLWOmxUSU6JRWK=
A388 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jobWlEPTB;MD63NlI2QCEQvF2= NGH5e4tUSU6JRWK=
TE-9 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3pdoVKSzVyPUCuO|Q1PTNizszN NY[yTmwyW0GQR1XS
LB2241-RCC NX3rW2dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPtWJpCUUN3ME2xMlE2PDB|IN88US=> NHLm[IJUSU6JRWK=
LB996-RCC NXztWFZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrKTXBlUUN3ME2xMlM3OjJ6IN88US=> NVLzfldRW0GQR1XS
LC-1F MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKwfVQyUUN3ME2xMlM5OjR2IN88US=> NXj6RlRTW0GQR1XS
TE-6 MnjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTFwNUWyNFEh|ryP Ml;TV2FPT0WU
A253 NVLFe|lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDSO4NKSzVyPUGuPVc{OzVizszN MkP6V2FPT0WU
OS-RC-2 M2HoR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrCTWM2OD1zLkm5NVk6KM7:TR?= NE\INGxUSU6JRWK=
TE-1 M{\xUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJwMES4N{DPxE1? M2rLOHNCVkeHUh?=
RL95-2 NVfxNYc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\FfHU3UUN3ME2zMlE2PjdizszN NITRSoRUSU6JRWK=
LS-513 NHTPfHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfPPFJrUUN3ME2zMlQxODRzIN88US=> M1XlTHNCVkeHUh?=
DJM-1 M1XMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn:2TWM2OD1|LkS2PVc2KM7:TR?= M{jnPXNCVkeHUh?=
NMC-G1 M2H1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13JO2lEPTB;Mz61OFUxOSEQvF2= NUKzUpp4W0GQR1XS
TE-10 M2\4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLTcI97UUN3ME2zMlU2OzV4IN88US=> NITVXZNUSU6JRWK=
TE-5 MnexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7UTWM2OD12LkCzO|Mh|ryP MUHTRW5ITVJ?
TK10 M4H0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTRwMU[1NlIh|ryP NYexTVBQW0GQR1XS
UACC-812 NITzW|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TjSGlEPTB;ND61OlE2OyEQvF2= MWLTRW5ITVJ?
SW962 NHjaZmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPqTWM2OD13LkCyNVU6KM7:TR?= NIW1WJNUSU6JRWK=
SW954 NWrDZplpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTVwM{myOFUh|ryP NHG0Z4lUSU6JRWK=
COLO-668 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTVwN{K2Olch|ryP MlKyV2FPT0WU
LB1047-RCC NGHvXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXvfIhKSzVyPUWuPFAxPDZizszN MVjTRW5ITVJ?
NB5 MnuxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2naW2lEPTB;Nj6yNVAxOSEQvF2= NHywTpJUSU6JRWK=
NTERA-S-cl-D1 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXOTWM2OD14LkK2OVYyKM7:TR?= MnrFV2FPT0WU
IST-MEL1 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofLTWM2OD14LkSzOlk1KM7:TR?= M4DPW3NCVkeHUh?=
GI-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTZwNUG2PFIh|ryP NV:wSINwW0GQR1XS
TGBC1TKB NUH1fHZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17q[WlEPTB;Nz6wO|E5OyEQvF2= NWnYb3EzW0GQR1XS
GT3TKB NU\Cbo01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\EOJN3UUN3ME23MlIzPzR2IN88US=> MnjuV2FPT0WU
EVSA-T M3i0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX6OWFKSzVyPUeuOFI5OTFizszN MXrTRW5ITVJ?
D-502MG NWTmcVR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHZd|luUUN3ME23MlQ5QDl2IN88US=> NF;EZndUSU6JRWK=
TE-8 NFv2TVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfXTJZNUUN3ME23Mlc3OTV7IN88US=> NVPTbGtvW0GQR1XS
OVCAR-4 M3W3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTlwMUG2O|Uh|ryP M2TNT3NCVkeHUh?=
D-336MG MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO3TWM2OD17LkS3N|k2KM7:TR?= M4GxcHNCVkeHUh?=
GCIY NVzZWG1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF60SWtKSzVyPUmuOVc1OiEQvF2= M1XXXHNCVkeHUh?=
KS-1 MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTlwNk[yPFch|ryP NYTsZlV[W0GQR1XS
HCC2998 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHLWmlKSzVyPUmuPVY{ODdizszN NHXNZ2tUSU6JRWK=
D-247MG NHSwNZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHP2VFNKSzVyPUmuPVgzQTFizszN NXz6fXpsW0GQR1XS
TE-15 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfGZVZKSzVyPUGwMlI1PSEQvF2= MVTTRW5ITVJ?
IST-MES1 NIjP[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXqTWM2OD1zMD6yOVY2KM7:TR?= NX3TZopjW0GQR1XS
ETK-1 MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjyTWM2OD1zMD62NlMh|ryP M{D2RXNCVkeHUh?=
RCC10RGB M2T4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HZbGlEPTB;MUCuPVYyKM7:TR?= M1vvWXNCVkeHUh?=
KNS-42 NFuxZ25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLlTWM2OD1zMT63NlU2KM7:TR?= NHizUGVUSU6JRWK=
LB771-HNC MlGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f0dGlEPTB;MUKuNVcyOiEQvF2= NFXuPWVUSU6JRWK=
SR Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXGVlhPUUN3ME2xNk4zODZ2IN88US=> NXT5NpV1W0GQR1XS
NCI-H1355 NULPNFR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF{Lki5PFUh|ryP NUHIWY8yW0GQR1XS
ES6 NHfkR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTF|LkC3PEDPxE1? Mk\nV2FPT0WU
SK-NEP-1 Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrG[IdKSzVyPUGzMlI2PzdizszN NFj3eWZUSU6JRWK=
D-392MG NVvDTIZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF|Lk[0Nlgh|ryP NH3OO45USU6JRWK=
NB7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\OfHBKSzVyPUG0MlI{PzRizszN M2PNUnNCVkeHUh?=
SK-LMS-1 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTjPHlJUUN3ME2xOE42OTR3IN88US=> MWfTRW5ITVJ?
SK-UT-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrZTWM2OD1zND63PFg6KM7:TR?= NVXBO4l3W0GQR1XS
CA46 NIXLZ3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTrTWM2OD1zNT6wOVg3KM7:TR?= NFLOOVlUSU6JRWK=
IST-SL2 M3iyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF3LkG5NFEh|ryP M3S5WXNCVkeHUh?=
BC-1 NEXONGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjqTWM2OD1zNT6zN|E1KM7:TR?= MofDV2FPT0WU
LS-123 M1LYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1e1PWlEPTB;MUWuPFE4OyEQvF2= M4fSZnNCVkeHUh?=
Ramos-2G6-4C10 M3HPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF4LkC5NlQh|ryP NVLsZ2RrW0GQR1XS
MZ1-PC NUHYZ3oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHoe|hWUUN3ME2xOk44OzF|IN88US=> NFLqTHZUSU6JRWK=
LB647-SCLC NGLqNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HBV2lEPTB;MU[uPVM4OiEQvF2= MnfhV2FPT0WU
NCI-H1694 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HvfGlEPTB;MUeuNVUzQSEQvF2= NULkdocxW0GQR1XS
NCI-H322M NEfYT3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\sTWM2OD1zNz60N|Y3KM7:TR?= MVTTRW5ITVJ?
ES7 NF3mfWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zkdGlEPTB;MUiuN|kyPCEQvF2= NHzRVnFUSU6JRWK=
LC-2-ad NFHIVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7yTWM2OD1zOD60N|g3KM7:TR?= NFPqUXRUSU6JRWK=
SF268 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzlcJNiUUN3ME2xPE44PDB7IN88US=> M1;3fnNCVkeHUh?=
RPMI-8402 NWDsVmhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLwTWM2OD1zOT6wO|QzKM7:TR?= MoKxV2FPT0WU
HCE-T Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjTc4RMUUN3ME2yNE4zOzR2IN88US=> MlPUV2FPT0WU
A101D NFrnOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DGS2lEPTB;MkCuPFU5PyEQvF2= MnfiV2FPT0WU
MRK-nu-1 M4HaRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PX[GlEPTB;MkCuPVE{KM7:TR?= MYPTRW5ITVJ?
LXF-289 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTJzLkCzPEDPxE1? Mn\YV2FPT0WU
NALM-6 NUnuR494T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rDU2lEPTB;MkGuNVk3PyEQvF2= NGT1b5ZUSU6JRWK=
DOHH-2 NXXvSZZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7US2VKSzVyPUKxMlQ5OTNizszN MXnTRW5ITVJ?
EW-16 NXPC[5VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WwdmlEPTB;MkKuNVQxOiEQvF2= M4H1eXNCVkeHUh?=
A4-Fuk MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\JWmlEPTB;MkKuNlE1QSEQvF2= MmizV2FPT0WU
HD-MY-Z MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLDSnBsUUN3ME2yNk4{QTZ3IN88US=> MkPxV2FPT0WU
SKM-1 NUjYWotWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJ{LkezOVEh|ryP MYrTRW5ITVJ?
DMS-153 M1vaVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJ|LkSyNFQh|ryP NU\CbHpVW0GQR1XS
LB373-MEL-D M3XxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ|LkW0OVIh|ryP M13lPXNCVkeHUh?=
LP-1 NFi4b3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP1RXZkUUN3ME2yN{45ODl5IN88US=> M4L2[HNCVkeHUh?=
GI-ME-N NHLvO|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jCSWlEPTB;MkSuNlkzKM7:TR?= MljhV2FPT0WU
MPP-89 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\6cYsxUUN3ME2yOU4zODN4IN88US=> NWS2fnVOW0GQR1XS
U-698-M MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f4eGlEPTB;MkWuNlUxOyEQvF2= MVPTRW5ITVJ?
HC-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPGeFFKSzVyPUK1MlY1OThizszN M1mxUnNCVkeHUh?=
HCC2157 NGXUWnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXj[o1KSzVyPUK1MlY4OyEQvF2= M{j0O3NCVkeHUh?=
MOLT-4 MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW3fo5KSzVyPUK2MlI4OyEQvF2= MljnV2FPT0WU
LS-411N M3rYWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXIcYNKSzVyPUK2MlM{PjlizszN Ml3ZV2FPT0WU
Becker NVr0dnNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjOTWM2OD1{Nj61NVgyKM7:TR?= M2jsPHNCVkeHUh?=
NCI-H23 NE\v[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fyfGlEPTB;Mk[uO|U4PSEQvF2= NFzzVVFUSU6JRWK=
IST-SL1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonTTWM2OD1{Nz6zPFY4KM7:TR?= MXvTRW5ITVJ?
MZ2-MEL MkjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO4TWM2OD1{Nz60OVY3KM7:TR?= NWLJ[HZJW0GQR1XS
RKO M{Hkbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHriU4tKSzVyPUK4MlE1PDZizszN MnntV2FPT0WU
TE-441-T NEWwbHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ6Lke4PUDPxE1? M1jnbXNCVkeHUh?=
EW-24 M1OyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfDS2JKSzVyPUK5MlEzPTlizszN MV;TRW5ITVJ?
no-10 MnLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7sZ4dKSzVyPUK5MlE3OzFizszN NEOxfIhUSU6JRWK=
D-542MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{GzXGlEPTB;MkmuPVIzOSEQvF2= MV\TRW5ITVJ?
ST486 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT1TWM2OD1|MD62OFUyKM7:TR?= MWjTRW5ITVJ?
KURAMOCHI NG[yeHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXwTWM2OD1|MD64NFU4KM7:TR?= M4HoWHNCVkeHUh?=
ES8 NXexWZhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTNzLkW5O|Ih|ryP NVLM[HpTW0GQR1XS
BL-41 NUHLe2xTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHtOJNUUUN3ME2zNk4yODV2IN88US=> NF;4OmZUSU6JRWK=
NB6 MmrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTN{LkO4OVUh|ryP NIToeIVUSU6JRWK=
NCI-H1304 M{C2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrqTWM2OD1|Mj60PVY4KM7:TR?= M2PVe3NCVkeHUh?=
MS-1 NXS0Nm04T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknFTWM2OD1|Mj63O|UyKM7:TR?= MoTxV2FPT0WU
MFH-ino M4e5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2G3Z2lEPTB;M{SuN|IzPCEQvF2= NITOPVNUSU6JRWK=
NOS-1 NEPifnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTN2Lk[3OFgh|ryP MonOV2FPT0WU
HUTU-80 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\GTWM2OD1|NT6zOlY4KM7:TR?= NWPyUmdrW0GQR1XS
EB2 NGrDelNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{niTWlEPTB;M{[uOlE5QSEQvF2= NULET3c{W0GQR1XS
L-540 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN5LkKzNFgh|ryP M2PCcnNCVkeHUh?=
NCI-H747 NHzmUpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTN6Lki4OFYh|ryP MUjTRW5ITVJ?
NCI-H446 NF3HOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITESmNKSzVyPUO5Mlk3PTFizszN MlfVV2FPT0WU
MOLT-16 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXUVnlKSzVyPUSyMlQyPSEQvF2= MXPTRW5ITVJ?
BC-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LqPGlEPTB;NEWuOFg6PiEQvF2= M3vuT3NCVkeHUh?=
SJSA-1 M3vNTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3NRYNMUUN3ME20OU42PDd2IN88US=> NVrCdoM4W0GQR1XS
BB65-RCC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjPN4VKSzVyPUS1MlY3PiEQvF2= NFP3[otUSU6JRWK=
SNB75 NUHBOHFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR4LkCxPEDPxE1? NGjabpBUSU6JRWK=

... 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]
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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 从左到右依次加入纯溶剂:
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.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID