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 NYOzXHdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nyOmlEPTB;MD6wNlU1PCEQvF2= NGjpTHFUSU6JRWK=
HCC2218 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXoSHdkUUN3ME2wMlA2OzJ4IN88US=> MWnTRW5ITVJ?
OCUB-M NGPsb4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwMEW3OEDPxE1? MkLSV2FPT0WU
ECC12 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMEmyN|Eh|ryP NX3IdJhHW0GQR1XS
DSH1 NI\qTVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETUemZKSzVyPUCuNFk{QTZizszN M3P1dnNCVkeHUh?=
BT-474 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf6SVFGUUN3ME2wMlIyOzF3IN88US=> MnjiV2FPT0WU
BB30-HNC NGrEUGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TKe2lEPTB;MD6yOFY2PCEQvF2= MnPVV2FPT0WU
EKVX NHzqZ3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTOR|lKSzVyPUCuOFQ5PzRizszN Mk\hV2FPT0WU
TE-12 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfCTIxrUUN3ME2wMlQ6ODV5IN88US=> MmDEV2FPT0WU
A388 M2XJSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T1ZWlEPTB;MD63NlI2QCEQvF2= M4XZR3NCVkeHUh?=
TE-9 NVPBR21PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLqNnV{UUN3ME2wMlc1PDV|IN88US=> NFnuT4ZUSU6JRWK=
LB2241-RCC M4fBb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Ho[mlEPTB;MT6xOVQxOyEQvF2= NXrZN4VFW0GQR1XS
LB996-RCC NFjDbVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP4eVlKSzVyPUGuN|YzOjhizszN M3fOSHNCVkeHUh?=
LC-1F NF[4doFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPUclVKSzVyPUGuN|gzPDRizszN NWmzZ3FtW0GQR1XS
TE-6 NYC1TZJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL1[2NKSzVyPUGuOVUzODFizszN MoDRV2FPT0WU
A253 MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHNSIFKSzVyPUGuPVc{OzVizszN NVjySZY2W0GQR1XS
OS-RC-2 NHvX[lVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPnTWM2OD1zLkm5NVk6KM7:TR?= NG\N[o1USU6JRWK=
TE-1 NU\mZW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPMfYhKSzVyPUKuNFQ5OyEQvF2= MnLiV2FPT0WU
RL95-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn63TWM2OD1|LkG1Olch|ryP MXHTRW5ITVJ?
LS-513 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXNfI1JUUN3ME2zMlQxODRzIN88US=> NFfTfXdUSU6JRWK=
DJM-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETmUVNKSzVyPUOuOFY6PzVizszN NIH3V4NUSU6JRWK=
NMC-G1 NGfLdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTNwNUS1NFEh|ryP NYSz[ZVkW0GQR1XS
TE-10 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\WSJRKSzVyPUOuOVU{PTZizszN MXfTRW5ITVJ?
TE-5 Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjuZVhRUUN3ME20MlA{PzNizszN NXvnVJVDW0GQR1XS
TK10 M3[0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK2TWM2OD12LkG2OVIzKM7:TR?= MYfTRW5ITVJ?
UACC-812 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPsTWM2OD12LkW2NVU{KM7:TR?= Ml3NV2FPT0WU
SW962 MkjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH31dFRKSzVyPUWuNFIyPTlizszN MlvJV2FPT0WU
SW954 NGT0[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPhNlBKSzVyPUWuN|kzPDVizszN Mnz0V2FPT0WU
COLO-668 NEXEflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTVwN{K2Olch|ryP NWTZRnE{W0GQR1XS
LB1047-RCC NHTIZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3WTWM2OD13LkiwNFQ3KM7:TR?= MWTTRW5ITVJ?
NB5 NGDycnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjncYJKSzVyPU[uNlExODFizszN MYTTRW5ITVJ?
NTERA-S-cl-D1 NH;qV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TldGlEPTB;Nj6yOlU3OSEQvF2= M{nIN3NCVkeHUh?=
IST-MEL1 M{C4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rCWWlEPTB;Nj60N|Y6PCEQvF2= NXra[3dYW0GQR1XS
GI-1 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTZwNUG2PFIh|ryP NX\nd3VGW0GQR1XS
TGBC1TKB M{HzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HB[mlEPTB;Nz6wO|E5OyEQvF2= NGfnRWtUSU6JRWK=
GT3TKB NWPPc2wyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\NdWlEPTB;Nz6yNlc1PCEQvF2= Mm\IV2FPT0WU
EVSA-T M1vMVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mme5TWM2OD15LkSyPFEyKM7:TR?= NETHOmlUSU6JRWK=
D-502MG Ml\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrUUoJKSzVyPUeuOFg5QTRizszN M3vHfnNCVkeHUh?=
TE-8 M2jGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4TWM2OD15Lke2NVU6KM7:TR?= MVzTRW5ITVJ?
OVCAR-4 M2fLU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTlwMUG2O|Uh|ryP M4rhbHNCVkeHUh?=
D-336MG NYHOe45RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC2TYUyUUN3ME25MlQ4Ozl3IN88US=> NUPYbJY1W0GQR1XS
GCIY NUfJSZg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjOfHNKSzVyPUmuOVc1OiEQvF2= Mn\TV2FPT0WU
KS-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTlwNk[yPFch|ryP NHXvWYpUSU6JRWK=
HCC2998 MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDzTWM2OD17Lkm2N|A4KM7:TR?= MVXTRW5ITVJ?
D-247MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFra[IxKSzVyPUmuPVgzQTFizszN MUjTRW5ITVJ?
TE-15 NH7TOJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ETWM2OD1zMD6yOFUh|ryP NHOxTJlUSU6JRWK=
IST-MES1 M2HacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFyLkK1OlUh|ryP MlvPV2FPT0WU
ETK-1 M2L5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPKTWM2OD1zMD62NlMh|ryP NYm3cXJjW0GQR1XS
RCC10RGB MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\he2lEPTB;MUCuPVYyKM7:TR?= NEn2eXZUSU6JRWK=
KNS-42 MonxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLKV2xKSzVyPUGxMlczPTVizszN NIfxNWxUSU6JRWK=
LB771-HNC NYOzO3hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITDS4RKSzVyPUGyMlE4OTJizszN MknCV2FPT0WU
SR MljKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTmXnpKSzVyPUGyMlIxPjRizszN M3jVSnNCVkeHUh?=
NCI-H1355 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiwW4pIUUN3ME2xNk45QTh3IN88US=> NH;Ec|lUSU6JRWK=
ES6 NGPXNo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r4N2lEPTB;MUOuNFc5KM7:TR?= NEHWVpJUSU6JRWK=
SK-NEP-1 M17YUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTF|LkK1O|ch|ryP NF\ld25USU6JRWK=
D-392MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHKOVVXUUN3ME2xN{43PDJ6IN88US=> Mk\EV2FPT0WU
NB7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{flS2lEPTB;MUSuNlM4PCEQvF2= MYrTRW5ITVJ?
SK-LMS-1 NVrq[ZVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK4TWM2OD1zND61NVQ2KM7:TR?= M4nTZnNCVkeHUh?=
SK-UT-1 MmjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXyWY1qUUN3ME2xOE44QDh7IN88US=> NFfyTm5USU6JRWK=
CA46 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3iTWM2OD1zNT6wOVg3KM7:TR?= NFHvVllUSU6JRWK=
IST-SL2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vZXGlEPTB;MUWuNVkxOSEQvF2= M{LiSXNCVkeHUh?=
BC-1 M{PscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF3LkOzNVQh|ryP NGXuc|VUSU6JRWK=
LS-123 NGj6b29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7WSFFKSzVyPUG1MlgyPzNizszN MWjTRW5ITVJ?
Ramos-2G6-4C10 NVG1cnE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HkO2lEPTB;MU[uNFkzPCEQvF2= Ml7aV2FPT0WU
MZ1-PC M{G1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;Te2lEPTB;MU[uO|MyOyEQvF2= Mln4V2FPT0WU
LB647-SCLC M2jU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPJco9KSzVyPUG2Mlk{PzJizszN MUXTRW5ITVJ?
NCI-H1694 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fhPWlEPTB;MUeuNVUzQSEQvF2= MWDTRW5ITVJ?
NCI-H322M MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXZR2huUUN3ME2xO{41OzZ4IN88US=> M4\kU3NCVkeHUh?=
ES7 NGTJ[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;EWlVLUUN3ME2xPE4{QTF2IN88US=> MVLTRW5ITVJ?
LC-2-ad MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LvdmlEPTB;MUiuOFM5PiEQvF2= M2LnPHNCVkeHUh?=
SF268 NUK2T2U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rjW2lEPTB;MUiuO|QxQSEQvF2= MmnJV2FPT0WU
RPMI-8402 M2TqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF7LkC3OFIh|ryP Ml\tV2FPT0WU
HCE-T MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHQeJFKSzVyPUKwMlI{PDRizszN NX\4XlY2W0GQR1XS
A101D NHPXUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nNNmlEPTB;MkCuPFU5PyEQvF2= MmTRV2FPT0WU
MRK-nu-1 NXjQWlRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TpWmlEPTB;MkCuPVE{KM7:TR?= MkC4V2FPT0WU
LXF-289 NWH1[HlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHThS3hKSzVyPUKxMlA{QCEQvF2= NHXkXGtUSU6JRWK=
NALM-6 NFvHSJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfyZYZmUUN3ME2yNU4yQTZ5IN88US=> M2rM[HNCVkeHUh?=
DOHH-2 NVfienduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHDTWM2OD1{MT60PFE{KM7:TR?= MoHDV2FPT0WU
EW-16 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUG0cGN4UUN3ME2yNk4yPDB{IN88US=> MVnTRW5ITVJ?
A4-Fuk NIiybHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LjcGlEPTB;MkKuNlE1QSEQvF2= NXO5U2p7W0GQR1XS
HD-MY-Z NFjFZ5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLxRm5KSzVyPUKyMlM6PjVizszN NFfke5hUSU6JRWK=
SKM-1 NX\GWXZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLRVZVyUUN3ME2yNk44OzVzIN88US=> Mn3MV2FPT0WU
DMS-153 M2XY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEK3R2FKSzVyPUKzMlQzODRizszN M3fWfXNCVkeHUh?=
LB373-MEL-D NVTWbnVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j1cWlEPTB;MkOuOVQ2OiEQvF2= NGjTb|BUSU6JRWK=
LP-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPSTWM2OD1{Mz64NFk4KM7:TR?= MVLTRW5ITVJ?
GI-ME-N NYPkNIxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfFTWM2OD1{ND6yPVIh|ryP NYnvfoJTW0GQR1XS
MPP-89 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkO4TWM2OD1{NT6yNFM3KM7:TR?= NWXWTVY{W0GQR1XS
U-698-M NFX2[YVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJ3LkK1NFMh|ryP NHPJNZdUSU6JRWK=
HC-1 M3TmWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJ3Lk[0NVgh|ryP M4HrZ3NCVkeHUh?=
HCC2157 NGLvc3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K3XGlEPTB;MkWuOlc{KM7:TR?= Moi0V2FPT0WU
MOLT-4 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJ4LkK3N{DPxE1? NIDQUFlUSU6JRWK=
LS-411N MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zmNWlEPTB;Mk[uN|M3QSEQvF2= M3O5dnNCVkeHUh?=
Becker NWfOVHo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX4e3pbUUN3ME2yOk42OThzIN88US=> NHrrW4FUSU6JRWK=
NCI-H23 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf5OXFKSzVyPUK2Mlc2PzVizszN M3LCV3NCVkeHUh?=
IST-SL1 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTPOoNKSzVyPUK3MlM5PjdizszN NEHuWpNUSU6JRWK=
MZ2-MEL NH3henZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTJ5LkS1OlYh|ryP MYfTRW5ITVJ?
RKO NIfyNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\KeGlEPTB;MkiuNVQ1PiEQvF2= MXjTRW5ITVJ?
TE-441-T NFTsdnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TJVWlEPTB;MkiuO|g6KM7:TR?= Mn7KV2FPT0WU
EW-24 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;WZpBFUUN3ME2yPU4yOjV7IN88US=> NETPeGZUSU6JRWK=
no-10 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ7LkG2N|Eh|ryP M2DYSHNCVkeHUh?=
D-542MG M1jXSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ7LkmyNlEh|ryP MYfTRW5ITVJ?
ST486 NF3hOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfWSVkxUUN3ME2zNE43PDVzIN88US=> NEXHVZJUSU6JRWK=
KURAMOCHI MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTNyLkiwOVch|ryP NV3qXHV6W0GQR1XS
ES8 NEPQfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNzLkW5O|Ih|ryP NF;GfVZUSU6JRWK=
BL-41 M2DWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;NXppKSzVyPUOyMlExPTRizszN M3rlTnNCVkeHUh?=
NB6 M1vmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M372O2lEPTB;M{KuN|g2PSEQvF2= NGjldItUSU6JRWK=
NCI-H1304 M1TvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f4bGlEPTB;M{KuOFk3PyEQvF2= MY\TRW5ITVJ?
MS-1 MmnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\oTWM2OD1|Mj63O|UyKM7:TR?= M1LIS3NCVkeHUh?=
MFH-ino MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvnTWM2OD1|ND6zNlI1KM7:TR?= MXPTRW5ITVJ?
NOS-1 M1;YXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDGTWM2OD1|ND62O|Q5KM7:TR?= MlLyV2FPT0WU
HUTU-80 NHzvVpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfLTWM2OD1|NT6zOlY4KM7:TR?= M1fDPHNCVkeHUh?=
EB2 NVLPZnBKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIqxTGtKSzVyPUO2MlYyQDlizszN NYfuW5pCW0GQR1XS
L-540 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHyZ4RKSzVyPUO3MlI{ODhizszN NYr1UJR5W0GQR1XS
NCI-H747 MmH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXyTWM2OD1|OD64PFQ3KM7:TR?= MYfTRW5ITVJ?
NCI-H446 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTN7Lkm2OVEh|ryP NH7LT4hUSU6JRWK=
MOLT-16 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPO[nR{UUN3ME20Nk41OTVizszN NUD4UWt4W0GQR1XS
BC-3 NUO5OIlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\KTWM2OD12NT60PFk3KM7:TR?= NY\WRW4xW0GQR1XS
SJSA-1 Mlz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4X4WGlEPTB;NEWuOVQ4PCEQvF2= NE\wXlFUSU6JRWK=
BB65-RCC MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGyTWM2OD12NT62OlYh|ryP MUXTRW5ITVJ?
SNB75 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG3TWM2OD12Nj6wNVgh|ryP M1nCNHNCVkeHUh?=

... 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]
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  • 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
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
NCT03080805 Recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co. Ltd. May 3 2017 Phase 3
NCT03084939 Recruiting Breast Cancer Hoffmann-La Roche April 24 2017 Phase 3
NCT03085368 Recruiting HER2-positive Breast Cancer Peking Union Medical College Hospital|EddingPharm Oncology Co. LTD. March 1 2017 Phase 2|Phase 3
NCT03052634 Recruiting Advanced Breast Cancer RemeGen November 2016 Phase 1|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.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

相关EGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID