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 NIDKfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGSyNHNKSzVyPUCuNFI2PDRizszN NGL5bVVUSU6JRWK=
HCC2218 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwMEWzNlYh|ryP NWe0SpR1W0GQR1XS
OCUB-M NFKyWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HWUGlEPTB;MD6wOVc1KM7:TR?= M3W3b3NCVkeHUh?=
ECC12 M4TBUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDpTWM2OD1yLkC5NlMyKM7:TR?= MkTIV2FPT0WU
DSH1 NGrhN2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMEmzPVYh|ryP M{PXZXNCVkeHUh?=
BT-474 MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37CXWlEPTB;MD6yNVMyPSEQvF2= NXzMUHVXW0GQR1XS
BB30-HNC M{TIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknqTWM2OD1yLkK0OlU1KM7:TR?= NFvVT|lUSU6JRWK=
EKVX NULDd5pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHKTWM2OD1yLkS0PFc1KM7:TR?= M1HNNXNCVkeHUh?=
TE-12 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HqfmlEPTB;MD60PVA2PyEQvF2= NW[xZXBnW0GQR1XS
A388 M3\qSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjMNYxKSzVyPUCuO|IzPThizszN MVHTRW5ITVJ?
TE-9 Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jNc2lEPTB;MD63OFQ2OyEQvF2= M1jHcXNCVkeHUh?=
LB2241-RCC M{LrfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v0[GlEPTB;MT6xOVQxOyEQvF2= M3vud3NCVkeHUh?=
LB996-RCC NEH5ZVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHoTWM2OD1zLkO2NlI5KM7:TR?= MlzMV2FPT0WU
LC-1F M2W0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHKWHJIUUN3ME2xMlM5OjR2IN88US=> NH\rVotUSU6JRWK=
TE-6 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW4bYFzUUN3ME2xMlU2OjBzIN88US=> M1\3bHNCVkeHUh?=
A253 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXuTWM2OD1zLkm3N|M2KM7:TR?= MUPTRW5ITVJ?
OS-RC-2 NUXod25rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXNb2JKSzVyPUGuPVkyQTlizszN NF23WFNUSU6JRWK=
TE-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLzTWM2OD1{LkC0PFMh|ryP MVXTRW5ITVJ?
RL95-2 NYHCWFduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\lZW46UUN3ME2zMlE2PjdizszN M1\YVHNCVkeHUh?=
LS-513 NG\HflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7ETWM2OD1|LkSwNFQyKM7:TR?= MmHGV2FPT0WU
DJM-1 Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNwNE[5O|Uh|ryP MoTSV2FPT0WU
NMC-G1 NITFcYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv0TWM2OD1|LkW0OVAyKM7:TR?= MVTTRW5ITVJ?
TE-10 MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNwNUWzOVYh|ryP M2LaRXNCVkeHUh?=
TE-5 M3TPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe5fFU2UUN3ME20MlA{PzNizszN M{L3SHNCVkeHUh?=
TK10 NHHIUlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX3TWM2OD12LkG2OVIzKM7:TR?= MYjTRW5ITVJ?
UACC-812 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEGzcIRKSzVyPUSuOVYyPTNizszN NFjWSYFUSU6JRWK=
SW962 Mm\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ywbWlEPTB;NT6wNlE2QSEQvF2= NIrOeY1USU6JRWK=
SW954 MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTVTWM2OD13LkO5NlQ2KM7:TR?= NYq5UGg{W0GQR1XS
COLO-668 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nk[GlEPTB;NT63NlY3PyEQvF2= M1H1W3NCVkeHUh?=
LB1047-RCC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[zZoJKSzVyPUWuPFAxPDZizszN NF63bHFUSU6JRWK=
NB5 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PhcWlEPTB;Nj6yNVAxOSEQvF2= M3i2RnNCVkeHUh?=
NTERA-S-cl-D1 NGnVOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHT[YExUUN3ME22MlI3PTZzIN88US=> M3zkfXNCVkeHUh?=
IST-MEL1 NGPhVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDVTWM2OD14LkSzOlk1KM7:TR?= NGj4NW5USU6JRWK=
GI-1 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTZwNUG2PFIh|ryP M3;JbnNCVkeHUh?=
TGBC1TKB Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjoZ2xMUUN3ME23MlA4OTh|IN88US=> NGr3SpVUSU6JRWK=
GT3TKB NEe1cJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\VO49KSzVyPUeuNlI4PDRizszN NV3hcGJGW0GQR1XS
EVSA-T MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPrVldKSzVyPUeuOFI5OTFizszN NYH3d|Q5W0GQR1XS
D-502MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDOSZJKSzVyPUeuOFg5QTRizszN MkTwV2FPT0WU
TE-8 NFfwXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDOTWM2OD15Lke2NVU6KM7:TR?= Mo\aV2FPT0WU
OVCAR-4 MmD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3VTWM2OD17LkGxOlc2KM7:TR?= NYXtXotmW0GQR1XS
D-336MG Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTUTWM2OD17LkS3N|k2KM7:TR?= NWHXfW9PW0GQR1XS
GCIY MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHjZ5VKSzVyPUmuOVc1OiEQvF2= MX3TRW5ITVJ?
KS-1 M4fTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3DPZBFUUN3ME25MlY3Ojh5IN88US=> NFPx[mVUSU6JRWK=
HCC2998 NXv3NG9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTlwOU[zNFch|ryP NWHtbFBNW0GQR1XS
D-247MG MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTlwOUiyPVEh|ryP NXPuW4tPW0GQR1XS
TE-15 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TBNmlEPTB;MUCuNlQ2KM7:TR?= NYDiWXhPW0GQR1XS
IST-MES1 MmO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;uXGFKSzVyPUGwMlI2PjVizszN MUjTRW5ITVJ?
ETK-1 MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfTTJNKSzVyPUGwMlYzOyEQvF2= NV7tXJltW0GQR1XS
RCC10RGB MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInJdG9KSzVyPUGwMlk3OSEQvF2= MnrGV2FPT0WU
KNS-42 M2XVcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnvbVc6UUN3ME2xNU44OjV3IN88US=> M1jWOXNCVkeHUh?=
LB771-HNC NWD6cJRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDBTWM2OD1zMj6xO|EzKM7:TR?= NYHpOWZZW0GQR1XS
SR M1XLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nJdWlEPTB;MUKuNlA3PCEQvF2= M2TOTnNCVkeHUh?=
NCI-H1355 M4rteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv2TWM2OD1zMj64PVg2KM7:TR?= NXXVclFEW0GQR1XS
ES6 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWntR|diUUN3ME2xN{4xPzhizszN MWPTRW5ITVJ?
SK-NEP-1 M124[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i0UmlEPTB;MUOuNlU4PyEQvF2= NIK4NYJUSU6JRWK=
D-392MG MkLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnLR3NYUUN3ME2xN{43PDJ6IN88US=> M1LDe3NCVkeHUh?=
NB7 M2rPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj0Sm9KSzVyPUG0MlI{PzRizszN NFfld5NUSU6JRWK=
SK-LMS-1 M1K5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTF2LkWxOFUh|ryP MmLQV2FPT0WU
SK-UT-1 MoWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf2TWM2OD1zND63PFg6KM7:TR?= M2\renNCVkeHUh?=
CA46 NHHQc|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInxNXhKSzVyPUG1MlA2QDZizszN MWTTRW5ITVJ?
IST-SL2 M3vPVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1noXmlEPTB;MUWuNVkxOSEQvF2= NFjPV|RUSU6JRWK=
BC-1 M1\TNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjpdm5vUUN3ME2xOU4{OzF2IN88US=> MkjGV2FPT0WU
LS-123 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrSZ3FHUUN3ME2xOU45OTd|IN88US=> NH3hOphUSU6JRWK=
Ramos-2G6-4C10 NXjwbXRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjPZ45mUUN3ME2xOk4xQTJ2IN88US=> Mnq1V2FPT0WU
MZ1-PC NXPqXHptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF4LkezNVMh|ryP NXPp[2gzW0GQR1XS
LB647-SCLC MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml71TWM2OD1zNj65N|czKM7:TR?= NHH4emtUSU6JRWK=
NCI-H1694 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTF5LkG1Nlkh|ryP MYTTRW5ITVJ?
NCI-H322M MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDnRYJKSzVyPUG3MlQ{PjZizszN NIW0R3lUSU6JRWK=
ES7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{GxUmlEPTB;MUiuN|kyPCEQvF2= NGXBVlVUSU6JRWK=
LC-2-ad NVSzXVR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DiZ2lEPTB;MUiuOFM5PiEQvF2= MW\TRW5ITVJ?
SF268 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17xTGlEPTB;MUiuO|QxQSEQvF2= MVTTRW5ITVJ?
RPMI-8402 NIrLW|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fldWlEPTB;MUmuNFc1OiEQvF2= M4rie3NCVkeHUh?=
HCE-T MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDTc25KSzVyPUKwMlI{PDRizszN MYnTRW5ITVJ?
A101D NI\QPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DZSWlEPTB;MkCuPFU5PyEQvF2= NFTBNHVUSU6JRWK=
MRK-nu-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PhU2lEPTB;MkCuPVE{KM7:TR?= MlL6V2FPT0WU
LXF-289 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLWTWM2OD1{MT6wN|gh|ryP M2XPRnNCVkeHUh?=
NALM-6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjsOYZKSzVyPUKxMlE6PjdizszN NYnTWWo{W0GQR1XS
DOHH-2 NUDRfJBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvaS5lKSzVyPUKxMlQ5OTNizszN MonRV2FPT0WU
EW-16 NUnMR4dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jhNWlEPTB;MkKuNVQxOiEQvF2= MmL5V2FPT0WU
A4-Fuk MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJ{LkKxOFkh|ryP MYHTRW5ITVJ?
HD-MY-Z M{\GSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fmTWlEPTB;MkKuN|k3PSEQvF2= MUPTRW5ITVJ?
SKM-1 M4nqbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPSepJKSzVyPUKyMlc{PTFizszN NXLMXHJOW0GQR1XS
DMS-153 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ|LkSyNFQh|ryP NGrXeG5USU6JRWK=
LB373-MEL-D NU[4e|h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfGTWM2OD1{Mz61OFUzKM7:TR?= NEPOXm1USU6JRWK=
LP-1 NWq3TJg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fOOGlEPTB;MkOuPFA6PyEQvF2= MV3TRW5ITVJ?
GI-ME-N Ml\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjle|lKSzVyPUK0MlI6OiEQvF2= NF3zS5ZUSU6JRWK=
MPP-89 NIG4S4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zLbGlEPTB;MkWuNlA{PiEQvF2= M3fhOXNCVkeHUh?=
U-698-M MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJ3LkK1NFMh|ryP MomxV2FPT0WU
HC-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\SNWlEPTB;MkWuOlQyQCEQvF2= M3S1[nNCVkeHUh?=
HCC2157 M2\mU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly3TWM2OD1{NT62O|Mh|ryP MlO4V2FPT0WU
MOLT-4 NYXDZoRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJ4LkK3N{DPxE1? MX;TRW5ITVJ?
LS-411N NULMR2I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjnTWM2OD1{Nj6zN|Y6KM7:TR?= MnnrV2FPT0WU
Becker MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP6TWM2OD1{Nj61NVgyKM7:TR?= MWrTRW5ITVJ?
NCI-H23 NIPJ[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXXdZh6UUN3ME2yOk44PTd3IN88US=> NFLPcJdUSU6JRWK=
IST-SL1 M1;1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M131NWlEPTB;MkeuN|g3PyEQvF2= NVH5boU6W0GQR1XS
MZ2-MEL NVTPfo57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof2TWM2OD1{Nz60OVY3KM7:TR?= MXPTRW5ITVJ?
RKO MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nhemlEPTB;MkiuNVQ1PiEQvF2= NELoZlRUSU6JRWK=
TE-441-T NETO[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPLTWM2OD1{OD63PFkh|ryP MWnTRW5ITVJ?
EW-24 M1u4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDGTWM2OD1{OT6xNlU6KM7:TR?= MWXTRW5ITVJ?
no-10 M{LMXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC1TWM2OD1{OT6xOlMyKM7:TR?= NHLQU3dUSU6JRWK=
D-542MG MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fM[2lEPTB;MkmuPVIzOSEQvF2= NFXJXWJUSU6JRWK=
ST486 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTNyLk[0OVEh|ryP NHz5eotUSU6JRWK=
KURAMOCHI MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\od4I5UUN3ME2zNE45ODV5IN88US=> NH\JfFlUSU6JRWK=
ES8 NV\CfXNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFu3RmNKSzVyPUOxMlU6PzJizszN MYPTRW5ITVJ?
BL-41 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILublRKSzVyPUOyMlExPTRizszN MUTTRW5ITVJ?
NB6 NYDBUFVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTN{LkO4OVUh|ryP M2LKS3NCVkeHUh?=
NCI-H1304 NWf3S3VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXlTWM2OD1|Mj60PVY4KM7:TR?= M{TNc3NCVkeHUh?=
MS-1 NVXO[2l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4L4W2lEPTB;M{KuO|c2OSEQvF2= MkDVV2FPT0WU
MFH-ino MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rRdGlEPTB;M{SuN|IzPCEQvF2= MXnTRW5ITVJ?
NOS-1 M33B[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTN2Lk[3OFgh|ryP NV[zcmtsW0GQR1XS
HUTU-80 NF\mZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnIZ|AzUUN3ME2zOU4{PjZ5IN88US=> NUTFdnhqW0GQR1XS
EB2 MnLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3Bd2hVUUN3ME2zOk43OTh7IN88US=> Mk\RV2FPT0WU
L-540 NHW3TZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M374VWlEPTB;M{euNlMxQCEQvF2= NXTDOGh7W0GQR1XS
NCI-H747 NFfkNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DFWmlEPTB;M{iuPFg1PiEQvF2= MYXTRW5ITVJ?
NCI-H446 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;hd5BKSzVyPUO5Mlk3PTFizszN NIq0TopUSU6JRWK=
MOLT-16 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7QfnBKSzVyPUSyMlQyPSEQvF2= M3HlXnNCVkeHUh?=
BC-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnNc|ZbUUN3ME20OU41QDl4IN88US=> NFnGV5VUSU6JRWK=
SJSA-1 M{POZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DNVWlEPTB;NEWuOVQ4PCEQvF2= MlvuV2FPT0WU
BB65-RCC NWfvPZRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvEdJREUUN3ME20OU43PjZizszN MmnkV2FPT0WU
SNB75 NV76N4dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTGR4t{UUN3ME20Ok4xOThizszN NWTJfVdOW0GQR1XS

... 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:
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
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