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 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwMEK1OFQh|ryP Mk\QV2FPT0WU
HCC2218 NH\M[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrISWlnUUN3ME2wMlA2OzJ4IN88US=> NYXaSG9TW0GQR1XS
OCUB-M MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMEW3OEDPxE1? MUfTRW5ITVJ?
ECC12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwMEmyN|Eh|ryP NWPwU49{W0GQR1XS
DSH1 NGPC[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f2ZWlEPTB;MD6wPVM6PiEQvF2= NHOzT|hUSU6JRWK=
BT-474 NHXJbZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTJ[otKSzVyPUCuNlE{OTVizszN Mn7VV2FPT0WU
BB30-HNC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnUTWM2OD1yLkK0OlU1KM7:TR?= NH3VTVlUSU6JRWK=
EKVX MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPIUldKSzVyPUCuOFQ5PzRizszN NFnrc4ZUSU6JRWK=
TE-12 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Kx[WlEPTB;MD60PVA2PyEQvF2= MXrTRW5ITVJ?
A388 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3QVnJKSzVyPUCuO|IzPThizszN NFr4bIdUSU6JRWK=
TE-9 M{G1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXFfI1KSzVyPUCuO|Q1PTNizszN NUC2VIduW0GQR1XS
LB2241-RCC MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfmTWM2OD1zLkG1OFA{KM7:TR?= MmDWV2FPT0WU
LB996-RCC NGroNoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfI[YlKSzVyPUGuN|YzOjhizszN NEHxdYZUSU6JRWK=
LC-1F NYLoOW5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL2XppiUUN3ME2xMlM5OjR2IN88US=> NVjmcHBMW0GQR1XS
TE-6 M1r6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fk[2lEPTB;MT61OVIxOSEQvF2= NFe5OVlUSU6JRWK=
A253 M3vMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTFwOUezN|Uh|ryP Mn;QV2FPT0WU
OS-RC-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFwOUmxPVkh|ryP NV;v[5VqW0GQR1XS
TE-1 MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVznW4JQUUN3ME2yMlA1QDNizszN M{L2TXNCVkeHUh?=
RL95-2 MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLJVZllUUN3ME2zMlE2PjdizszN M{XIUHNCVkeHUh?=
LS-513 NH\sdolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHNTHQ{UUN3ME2zMlQxODRzIN88US=> MV3TRW5ITVJ?
DJM-1 NXLrToY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\ScZJKSzVyPUOuOFY6PzVizszN NX3qZotvW0GQR1XS
NMC-G1 NUnLVHVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DTc2lEPTB;Mz61OFUxOSEQvF2= MYfTRW5ITVJ?
TE-10 M37SdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\3UmlEPTB;Mz61OVM2PiEQvF2= MV;TRW5ITVJ?
TE-5 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33QOWlEPTB;ND6wN|c{KM7:TR?= NFTORYxUSU6JRWK=
TK10 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnToTWM2OD12LkG2OVIzKM7:TR?= NHP4dlFUSU6JRWK=
UACC-812 NW\re5N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjo[nhKSzVyPUSuOVYyPTNizszN MlLHV2FPT0WU
SW962 NUWwbHBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrpdm82UUN3ME21MlAzOTV7IN88US=> MlfNV2FPT0WU
SW954 Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PBSWlEPTB;NT6zPVI1PSEQvF2= NVuzTFJqW0GQR1XS
COLO-668 M2G5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;FPYVKSzVyPUWuO|I3PjdizszN NEPIRodUSU6JRWK=
LB1047-RCC NHLidYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvGZ2VKSzVyPUWuPFAxPDZizszN NH\1WWJUSU6JRWK=
NB5 MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnGVWhGUUN3ME22MlIyODBzIN88US=> MYDTRW5ITVJ?
NTERA-S-cl-D1 M4rOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrQTWM2OD14LkK2OVYyKM7:TR?= M2HFTXNCVkeHUh?=
IST-MEL1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;vTWM2OD14LkSzOlk1KM7:TR?= MV7TRW5ITVJ?
GI-1 NUXj[5dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7UTWM2OD14LkWxOlgzKM7:TR?= M1voV3NCVkeHUh?=
TGBC1TKB MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TKOWlEPTB;Nz6wO|E5OyEQvF2= MXvTRW5ITVJ?
GT3TKB MlHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y2NWlEPTB;Nz6yNlc1PCEQvF2= NGnONHJUSU6JRWK=
EVSA-T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDjNIJIUUN3ME23MlQzQDFzIN88US=> NVi1[IR7W0GQR1XS
D-502MG NXP3VHptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrQTWM2OD15LkS4PFk1KM7:TR?= MV\TRW5ITVJ?
TE-8 M3v3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;kW2lEPTB;Nz63OlE2QSEQvF2= MX7TRW5ITVJ?
OVCAR-4 MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTlwMUG2O|Uh|ryP NGLJNW1USU6JRWK=
D-336MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX5TWM2OD17LkS3N|k2KM7:TR?= NIHLR5pUSU6JRWK=
GCIY MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fnWWlEPTB;OT61O|QzKM7:TR?= M3zYbXNCVkeHUh?=
KS-1 M1niXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X4N2lEPTB;OT62OlI5PyEQvF2= NH70W2RUSU6JRWK=
HCC2998 MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzXTWM2OD17Lkm2N|A4KM7:TR?= NYnVVXd2W0GQR1XS
D-247MG MoDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwOUiyPVEh|ryP NXm0[4V4W0GQR1XS
TE-15 NXXtb3lGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFyLkK0OUDPxE1? Ml:5V2FPT0WU
IST-MES1 NXiyXGVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVniSZZYUUN3ME2xNE4zPTZ3IN88US=> M4DIOXNCVkeHUh?=
ETK-1 NYnRWWY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17uWmlEPTB;MUCuOlI{KM7:TR?= NH24[XNUSU6JRWK=
RCC10RGB MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml62TWM2OD1zMD65OlEh|ryP NFHQNnBUSU6JRWK=
KNS-42 M{[3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFzLkeyOVUh|ryP Mo\MV2FPT0WU
LB771-HNC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K0[mlEPTB;MUKuNVcyOiEQvF2= NGL4N21USU6JRWK=
SR MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i3SGlEPTB;MUKuNlA3PCEQvF2= M1TEZXNCVkeHUh?=
NCI-H1355 M{j4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXqT4RpUUN3ME2xNk45QTh3IN88US=> Ml3vV2FPT0WU
ES6 NFfxTWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWyTWM2OD1zMz6wO|gh|ryP NFLPdY1USU6JRWK=
SK-NEP-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTF|LkK1O|ch|ryP NHzUS5dUSU6JRWK=
D-392MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33LZ2lEPTB;MUOuOlQzQCEQvF2= NFLYWJJUSU6JRWK=
NB7 NWLHOY9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n5SGlEPTB;MUSuNlM4PCEQvF2= NIG2VmpUSU6JRWK=
SK-LMS-1 MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzPTWM2OD1zND61NVQ2KM7:TR?= M4m4[XNCVkeHUh?=
SK-UT-1 NX3ie25{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5VWdKSzVyPUG0Mlc5QDlizszN NXHrN2N[W0GQR1XS
CA46 M4PRVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDpfm5KSzVyPUG1MlA2QDZizszN MV;TRW5ITVJ?
IST-SL2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HWcGlEPTB;MUWuNVkxOSEQvF2= MnTOV2FPT0WU
BC-1 NH\3c2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[5TWM2OD1zNT6zN|E1KM7:TR?= Mm\tV2FPT0WU
LS-123 NWTtdWhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\jW3VKSzVyPUG1MlgyPzNizszN MVzTRW5ITVJ?
Ramos-2G6-4C10 M4\Xcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPaTWM2OD1zNj6wPVI1KM7:TR?= M3TWSXNCVkeHUh?=
MZ1-PC NV;ObXBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfGTWM2OD1zNj63N|E{KM7:TR?= NV3ad2hnW0GQR1XS
LB647-SCLC M2XoPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHyU|BKSzVyPUG2Mlk{PzJizszN M3fROHNCVkeHUh?=
NCI-H1694 NEH6XHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCzTWM2OD1zNz6xOVI6KM7:TR?= NUTsb4RnW0GQR1XS
NCI-H322M MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TZZmlEPTB;MUeuOFM3PiEQvF2= M3rGWnNCVkeHUh?=
ES7 NXvuXFlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvpTWM2OD1zOD6zPVE1KM7:TR?= MW\TRW5ITVJ?
LC-2-ad M1naNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7FTWM2OD1zOD60N|g3KM7:TR?= NF3NNWNUSU6JRWK=
SF268 M{\afmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjCSWhKSzVyPUG4Mlc1ODlizszN M4PjNHNCVkeHUh?=
RPMI-8402 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrzUplKSzVyPUG5MlA4PDJizszN NX\WPWlqW0GQR1XS
HCE-T NEDDd4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L0W2lEPTB;MkCuNlM1PCEQvF2= MWjTRW5ITVJ?
A101D NIjT[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJyLki1PFch|ryP NGLrTItUSU6JRWK=
MRK-nu-1 NEf5NmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfTc3lKSzVyPUKwMlkyOyEQvF2= M2PxXnNCVkeHUh?=
LXF-289 NYDqN5pGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEn0fJpKSzVyPUKxMlA{QCEQvF2= MonWV2FPT0WU
NALM-6 M{DnXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPoTWM2OD1{MT6xPVY4KM7:TR?= NI\6dnVUSU6JRWK=
DOHH-2 NEPCZmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJzLkS4NVMh|ryP NHHOXmFUSU6JRWK=
EW-16 M1fMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHBTWM2OD1{Mj6xOFAzKM7:TR?= NULCenFjW0GQR1XS
A4-Fuk M{\wRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJ{LkKxOFkh|ryP MUjTRW5ITVJ?
HD-MY-Z MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPxZotKSzVyPUKyMlM6PjVizszN NUKzWJV7W0GQR1XS
SKM-1 NHm5NlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTJ{LkezOVEh|ryP MoDSV2FPT0WU
DMS-153 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrrO|FUUUN3ME2yN{41OjB2IN88US=> NUD0VZJvW0GQR1XS
LB373-MEL-D NFXrcHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnsTWM2OD1{Mz61OFUzKM7:TR?= M2PmW3NCVkeHUh?=
LP-1 NI\mU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJ|LkiwPVch|ryP NVPCWFJzW0GQR1XS
GI-ME-N NIW4UoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnIRmJWUUN3ME2yOE4zQTJizszN MV3TRW5ITVJ?
MPP-89 NITWfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzs[ZdKSzVyPUK1MlIxOzZizszN NHP3[m9USU6JRWK=
U-698-M MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTmTWM2OD1{NT6yOVA{KM7:TR?= MnO0V2FPT0WU
HC-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TIdGlEPTB;MkWuOlQyQCEQvF2= Mn;6V2FPT0WU
HCC2157 NGXzOWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ3Lk[3N{DPxE1? MYnTRW5ITVJ?
MOLT-4 MkKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq5cGJKSzVyPUK2MlI4OyEQvF2= MkXYV2FPT0WU
LS-411N MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DlXmlEPTB;Mk[uN|M3QSEQvF2= NU\S[JNKW0GQR1XS
Becker NWfSR3FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjZN|lVUUN3ME2yOk42OThzIN88US=> MXzTRW5ITVJ?
NCI-H23 NH7ScVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[5RWlEPTB;Mk[uO|U4PSEQvF2= NEfmWZlUSU6JRWK=
IST-SL1 NYjWfJBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnMRmdtUUN3ME2yO{4{QDZ5IN88US=> MkPUV2FPT0WU
MZ2-MEL MlLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTJ5LkS1OlYh|ryP NXLjOld6W0GQR1XS
RKO NH7TfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q5bmlEPTB;MkiuNVQ1PiEQvF2= MX\TRW5ITVJ?
TE-441-T MlTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJ6Lke4PUDPxE1? NV;TVpRrW0GQR1XS
EW-24 NH;JeW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHhTWM2OD1{OT6xNlU6KM7:TR?= MUTTRW5ITVJ?
no-10 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJ7LkG2N|Eh|ryP MnLxV2FPT0WU
D-542MG NVnheoZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJ7LkmyNlEh|ryP M2n5RnNCVkeHUh?=
ST486 NWPMTY52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnOTWM2OD1|MD62OFUyKM7:TR?= Mn61V2FPT0WU
KURAMOCHI M4\KRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH0NnFKSzVyPUOwMlgxPTdizszN MXHTRW5ITVJ?
ES8 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXESotKSzVyPUOxMlU6PzJizszN NYjHSmhmW0GQR1XS
BL-41 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLCTWM2OD1|Mj6xNFU1KM7:TR?= MVHTRW5ITVJ?
NB6 M{\ve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6zd3RHUUN3ME2zNk4{QDV3IN88US=> MYjTRW5ITVJ?
NCI-H1304 M2nzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPEXlBzUUN3ME2zNk41QTZ5IN88US=> NUK3TJBZW0GQR1XS
MS-1 M13kW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG5OHY4UUN3ME2zNk44PzVzIN88US=> NHrOW2NUSU6JRWK=
MFH-ino MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn5NndRUUN3ME2zOE4{OjJ2IN88US=> NXTHZYRsW0GQR1XS
NOS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljqTWM2OD1|ND62O|Q5KM7:TR?= MVTTRW5ITVJ?
HUTU-80 NYnDPIY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHPfWhxUUN3ME2zOU4{PjZ5IN88US=> NF32NlJUSU6JRWK=
EB2 M2fLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTN4Lk[xPFkh|ryP MYPTRW5ITVJ?
L-540 NEfXemRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzaVHdKSzVyPUO3MlI{ODhizszN NXj0OI5HW0GQR1XS
NCI-H747 NFTj[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\3SGdKSzVyPUO4Mlg5PDZizszN M4nVOXNCVkeHUh?=
NCI-H446 MnHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\pbJpwUUN3ME2zPU46PjVzIN88US=> NIfV[GpUSU6JRWK=
MOLT-16 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jKN2lEPTB;NEKuOFE2KM7:TR?= NYjoZnNlW0GQR1XS
BC-3 NHfybY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPTUmRKSzVyPUS1MlQ5QTZizszN NEHSOFhUSU6JRWK=
SJSA-1 M2rLUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTR3LkW0O|Qh|ryP M2nZU3NCVkeHUh?=
BB65-RCC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjCU4xKSzVyPUS1MlY3PiEQvF2= MXnTRW5ITVJ?
SNB75 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL3TWM2OD12Nj6wNVgh|ryP M4OzO3NCVkeHUh?=

... 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

相关EGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID