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 M1P3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTrXYxKSzVyPUCuNFI2PDRizszN NFfSWItUSU6JRWK=
HCC2218 M4rsZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7BcnFKSzVyPUCuNFU{OjZizszN NFq0enJUSU6JRWK=
OCUB-M Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHITWM2OD1yLkC1O|Qh|ryP NF;3PHNUSU6JRWK=
ECC12 M3H1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMEmyN|Eh|ryP MUfTRW5ITVJ?
DSH1 NFfSV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LGT2lEPTB;MD6wPVM6PiEQvF2= NHTz[ldUSU6JRWK=
BT-474 NGLSOZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zLdGlEPTB;MD6yNVMyPSEQvF2= Ml\PV2FPT0WU
BB30-HNC NIG5OYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P1OWlEPTB;MD6yOFY2PCEQvF2= NIrLXFBUSU6JRWK=
EKVX NFjSdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnTOo5KSzVyPUCuOFQ5PzRizszN MUTTRW5ITVJ?
TE-12 NGO1SnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LzfmlEPTB;MD60PVA2PyEQvF2= MVTTRW5ITVJ?
A388 NVLpPZNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX3Npk5UUN3ME2wMlczOjV6IN88US=> NYfieWt2W0GQR1XS
TE-9 NV\NSJh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvoTWM2OD1yLke0OFU{KM7:TR?= NWHr[JZnW0GQR1XS
LB2241-RCC M3nDUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFwMUW0NFMh|ryP MXTTRW5ITVJ?
LB996-RCC MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwM{[yNlgh|ryP M3;zeXNCVkeHUh?=
LC-1F MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwM{iyOFQh|ryP MnzUV2FPT0WU
TE-6 M162OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\kOmlEPTB;MT61OVIxOSEQvF2= M4i1NHNCVkeHUh?=
A253 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTPVVJKSzVyPUGuPVc{OzVizszN MkTtV2FPT0WU
OS-RC-2 MlLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnK5TWM2OD1zLkm5NVk6KM7:TR?= MV;TRW5ITVJ?
TE-1 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3Icmt4UUN3ME2yMlA1QDNizszN M4fKS3NCVkeHUh?=
RL95-2 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfve25KSzVyPUOuNVU3PyEQvF2= NWDrUmRYW0GQR1XS
LS-513 MoDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTNwNECwOFEh|ryP MkDXV2FPT0WU
DJM-1 MmDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;ITWM2OD1|LkS2PVc2KM7:TR?= M3jkdHNCVkeHUh?=
NMC-G1 M2PKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK3RZdOUUN3ME2zMlU1PTBzIN88US=> MoHEV2FPT0WU
TE-10 MnuxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLBTWM2OD1|LkW1N|U3KM7:TR?= MW\TRW5ITVJ?
TE-5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmflTWM2OD12LkCzO|Mh|ryP M3nRdXNCVkeHUh?=
TK10 MmHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nmXWlEPTB;ND6xOlUzOiEQvF2= NGnkNo9USU6JRWK=
UACC-812 NEm1b|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7a[oJHUUN3ME20MlU3OTV|IN88US=> MV7TRW5ITVJ?
SW962 NV7nSVZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTVwMEKxOVkh|ryP MYPTRW5ITVJ?
SW954 MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XG[GlEPTB;NT6zPVI1PSEQvF2= M3y0e3NCVkeHUh?=
COLO-668 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPEcpFuUUN3ME21MlczPjZ5IN88US=> MlLWV2FPT0WU
LB1047-RCC NEDMTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq0Z2NKSzVyPUWuPFAxPDZizszN MYfTRW5ITVJ?
NB5 NFjwcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHDTWM2OD14LkKxNFAyKM7:TR?= MkHUV2FPT0WU
NTERA-S-cl-D1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP2TG5KSzVyPU[uNlY2PjFizszN Mn7sV2FPT0WU
IST-MEL1 M{e3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvMPZo6UUN3ME22MlQ{Pjl2IN88US=> NUfUTlh[W0GQR1XS
GI-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHVRVB4UUN3ME22MlUyPjh{IN88US=> MUHTRW5ITVJ?
TGBC1TKB NX\wU4lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnH6TWM2OD15LkC3NVg{KM7:TR?= NVTIbI1yW0GQR1XS
GT3TKB NYPveIJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTdwMkK3OFQh|ryP NUPl[HZrW0GQR1XS
EVSA-T Mn31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrEV4ZLUUN3ME23MlQzQDFzIN88US=> NYDzVY5nW0GQR1XS
D-502MG NVrIU5Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L1VWlEPTB;Nz60PFg6PCEQvF2= MX3TRW5ITVJ?
TE-8 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorhTWM2OD15Lke2NVU6KM7:TR?= NETvd2lUSU6JRWK=
OVCAR-4 NYDu[XduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXsTWM2OD17LkGxOlc2KM7:TR?= Mlu0V2FPT0WU
D-336MG M{HJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\3TWM2OD17LkS3N|k2KM7:TR?= MXfTRW5ITVJ?
GCIY NEHofWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTlwNUe0NkDPxE1? NYC4SW9OW0GQR1XS
KS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;5TWM2OD17Lk[2Nlg4KM7:TR?= NIDnfIdUSU6JRWK=
HCC2998 NXnTb4ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HKfWlEPTB;OT65OlMxPyEQvF2= MXHTRW5ITVJ?
D-247MG MmTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7vTWM2OD17Lkm4NlkyKM7:TR?= MkjUV2FPT0WU
TE-15 NWnid2xyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm3TWM2OD1zMD6yOFUh|ryP M4DYW3NCVkeHUh?=
IST-MES1 M4X2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml72TWM2OD1zMD6yOVY2KM7:TR?= NGHJUpRUSU6JRWK=
ETK-1 NVjE[JptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\1R|NKSzVyPUGwMlYzOyEQvF2= Ml\NV2FPT0WU
RCC10RGB NVrv[WNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XX[WlEPTB;MUCuPVYyKM7:TR?= NFjEZYpUSU6JRWK=
KNS-42 MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTFzLkeyOVUh|ryP NFzMUHBUSU6JRWK=
LB771-HNC NVzwR45bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nXV2lEPTB;MUKuNVcyOiEQvF2= MYPTRW5ITVJ?
SR MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TqeWlEPTB;MUKuNlA3PCEQvF2= MUDTRW5ITVJ?
NCI-H1355 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzPTWM2OD1zMj64PVg2KM7:TR?= NWPuV|F2W0GQR1XS
ES6 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vZSmlEPTB;MUOuNFc5KM7:TR?= NG\TWVFUSU6JRWK=
SK-NEP-1 M1Plb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDXeVFKSzVyPUGzMlI2PzdizszN M2G2RXNCVkeHUh?=
D-392MG MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37nSmlEPTB;MUOuOlQzQCEQvF2= NYfwSFFLW0GQR1XS
NB7 NFXvSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LEWmlEPTB;MUSuNlM4PCEQvF2= NUHpSFg6W0GQR1XS
SK-LMS-1 M1G1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\OU2lEPTB;MUSuOVE1PSEQvF2= MYnTRW5ITVJ?
SK-UT-1 NWXrWXJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDhTWM2OD1zND63PFg6KM7:TR?= NVi2TXptW0GQR1XS
CA46 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPpTWM2OD1zNT6wOVg3KM7:TR?= NHvnZWxUSU6JRWK=
IST-SL2 M4H6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXl[YY3UUN3ME2xOU4yQTBzIN88US=> M1HnWnNCVkeHUh?=
BC-1 MlvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XaXGlEPTB;MUWuN|MyPCEQvF2= MnLVV2FPT0WU
LS-123 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTBTWM2OD1zNT64NVc{KM7:TR?= NUTyO3VjW0GQR1XS
Ramos-2G6-4C10 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF4LkC5NlQh|ryP MlXtV2FPT0WU
MZ1-PC NGPtT2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK3cpZEUUN3ME2xOk44OzF|IN88US=> NHvGeoVUSU6JRWK=
LB647-SCLC MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnVRYZKSzVyPUG2Mlk{PzJizszN M4TsTXNCVkeHUh?=
NCI-H1694 Ml:yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF5LkG1Nlkh|ryP M2LkfXNCVkeHUh?=
NCI-H322M M13QSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF5LkSzOlYh|ryP NVrnVlJvW0GQR1XS
ES7 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnHbJQ{UUN3ME2xPE4{QTF2IN88US=> NYSzbpFyW0GQR1XS
LC-2-ad MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHnTWM2OD1zOD60N|g3KM7:TR?= Mki5V2FPT0WU
SF268 MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPCXIZKSzVyPUG4Mlc1ODlizszN NWrjfW9CW0GQR1XS
RPMI-8402 NFvmd41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HuW2lEPTB;MUmuNFc1OiEQvF2= NEO5NHBUSU6JRWK=
HCE-T NIjHZplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJyLkKzOFQh|ryP NWHlZ3ZFW0GQR1XS
A101D NFXiZm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJyLki1PFch|ryP NXjhcIp5W0GQR1XS
MRK-nu-1 MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJyLkmxN{DPxE1? M1qwV3NCVkeHUh?=
LXF-289 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTrZ3N{UUN3ME2yNU4xOzhizszN NF3vN2hUSU6JRWK=
NALM-6 NHnyT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfOTWM2OD1{MT6xPVY4KM7:TR?= MkXMV2FPT0WU
DOHH-2 MnXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\3c4NUUUN3ME2yNU41QDF|IN88US=> MoW2V2FPT0WU
EW-16 MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHmzbJZKSzVyPUKyMlE1ODJizszN M1XH[HNCVkeHUh?=
A4-Fuk NVvTTGxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljKTWM2OD1{Mj6yNVQ6KM7:TR?= NH31bGZUSU6JRWK=
HD-MY-Z M3KxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LzcWlEPTB;MkKuN|k3PSEQvF2= MmHvV2FPT0WU
SKM-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rmWWlEPTB;MkKuO|M2OSEQvF2= M4jvfXNCVkeHUh?=
DMS-153 NVvXWWZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPkXXdKSzVyPUKzMlQzODRizszN NWi3cVI6W0GQR1XS
LB373-MEL-D NIHEZVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrBO2NKUUN3ME2yN{42PDV{IN88US=> NHnl[o9USU6JRWK=
LP-1 NUTpUlVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ|LkiwPVch|ryP M2e3[3NCVkeHUh?=
GI-ME-N NHu4fHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7yR45TUUN3ME2yOE4zQTJizszN NXuzTXY5W0GQR1XS
MPP-89 NVntWXhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\MTWM2OD1{NT6yNFM3KM7:TR?= NWnEOlhsW0GQR1XS
U-698-M MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV30O3V[UUN3ME2yOU4zPTB|IN88US=> MoLkV2FPT0WU
HC-1 NGqyOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rjUmlEPTB;MkWuOlQyQCEQvF2= M{fWZ3NCVkeHUh?=
HCC2157 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvLTWM2OD1{NT62O|Mh|ryP MWLTRW5ITVJ?
MOLT-4 M4H4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:1Z2lEPTB;Mk[uNlc{KM7:TR?= NXL0dHA3W0GQR1XS
LS-411N MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i1V2lEPTB;Mk[uN|M3QSEQvF2= M2XDWXNCVkeHUh?=
Becker NHH0ZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjobItKSzVyPUK2MlUyQDFizszN M3HjOXNCVkeHUh?=
NCI-H23 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17DdWlEPTB;Mk[uO|U4PSEQvF2= Mo\aV2FPT0WU
IST-SL1 NF7ZVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi0cXdKSzVyPUK3MlM5PjdizszN NVz3W5hQW0GQR1XS
MZ2-MEL MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nnU2lEPTB;MkeuOFU3PiEQvF2= NYHkUllDW0GQR1XS
RKO M1Wze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTJ6LkG0OFYh|ryP NYDpZmM3W0GQR1XS
TE-441-T M1HvRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\pXmlEPTB;MkiuO|g6KM7:TR?= M{HYbXNCVkeHUh?=
EW-24 NYXQVVBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTJ7LkGyOVkh|ryP NEi1OG5USU6JRWK=
no-10 NEnlTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTkTWhVUUN3ME2yPU4yPjNzIN88US=> NH24fIJUSU6JRWK=
D-542MG M37mWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\4TWM2OD1{OT65NlIyKM7:TR?= NGC0d|FUSU6JRWK=
ST486 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;1WnYyUUN3ME2zNE43PDVzIN88US=> MnLmV2FPT0WU
KURAMOCHI M1u0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz0TWM2OD1|MD64NFU4KM7:TR?= Mn\3V2FPT0WU
ES8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLkTWM2OD1|MT61PVczKM7:TR?= M1LmdnNCVkeHUh?=
BL-41 NVfS[4JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvrTWM2OD1|Mj6xNFU1KM7:TR?= M3z5U3NCVkeHUh?=
NB6 NHrCWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrVOYpKUUN3ME2zNk4{QDV3IN88US=> MVXTRW5ITVJ?
NCI-H1304 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW2TWM2OD1|Mj60PVY4KM7:TR?= MkjLV2FPT0WU
MS-1 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz5TWM2OD1|Mj63O|UyKM7:TR?= M2TKUXNCVkeHUh?=
MFH-ino MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jFcGlEPTB;M{SuN|IzPCEQvF2= M{jn[nNCVkeHUh?=
NOS-1 NIH0bVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH74N2dKSzVyPUO0MlY4PDhizszN NV\GN5hxW0GQR1XS
HUTU-80 NWGwVmJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTN3LkO2Olch|ryP MUfTRW5ITVJ?
EB2 M3vDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTN4Lk[xPFkh|ryP Mn7vV2FPT0WU
L-540 M2jLNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i4[2lEPTB;M{euNlMxQCEQvF2= M4nHTnNCVkeHUh?=
NCI-H747 M4fwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\iTGlEPTB;M{iuPFg1PiEQvF2= M2[1[nNCVkeHUh?=
NCI-H446 NXe4S49PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTN7Lkm2OVEh|ryP NY\yRYtXW0GQR1XS
MOLT-16 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXTWFFvUUN3ME20Nk41OTVizszN NX;pfJJZW0GQR1XS
BC-3 NVHNOGYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fxbWlEPTB;NEWuOFg6PiEQvF2= NWj6[lN{W0GQR1XS
SJSA-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfqO5ZKSzVyPUS1MlU1PzRizszN MlzFV2FPT0WU
BB65-RCC M324NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;yZ4xKSzVyPUS1MlY3PiEQvF2= NH\HW2ZUSU6JRWK=
SNB75 MoiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrMTWM2OD12Nj6wNVgh|ryP MnLSV2FPT0WU

... 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
NCT02015169 Completed HER2-positive Gastric Cancer Patients With Liver Metastasis Samsung Medical Center July 9 2012 Phase 2
NCT00073528 Completed Neoplasms Breast Novartis Pharmaceuticals|Novartis December 9 2003 Phase 3
NCT01591577 Recruiting Newly Diagnosed Glioblastoma Multiforme Jonsson Comprehensive Cancer Center|GlaxoSmithKline December 7 2012 Phase 2
NCT00667251 Active not recruiting Breast Cancer Novartis Pharmaceuticals|NCIC Clinical Trials Group|Novartis October 7 2008 Phase 3
NCT00367471 Active not recruiting Neoplasms Breast Novartis Pharmaceuticals|Novartis December 7 2006 Phase 1
NCT02650752 Active not recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 6 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