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Lapatinib tosylate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Lapatinib tosylate图片
CAS NO:1187538-35-7
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GW572016 tosylate
GW2016 tosylate
产品介绍
Lapatinib (GW572016) tosylate 是一种有效的，具有口服活性的ErbB-2和EGFR酪氨酸激酶结构域的抑制剂，对纯化的EGFR和ErbB-2的IC50值分别为 10.2 和 9.8 nM。
生物活性

Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of theErbB-2andEGFRtyrosine kinase domains withIC50values against purifiedEGFRandErbB-2of 10.2 and 9.8 nM, respectively[1].

IC50& Target[1]

EGFR

10.2 nM (IC50)

ErbB2

9.8 nM (IC50)

体外研究
(In Vitro)

Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) tosylate treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) tosylate treatment has a selective inhibition of the proliferation of human tumor cell lines[1].
Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1].

Cell Proliferation Assay[1]

Cell Line:HN5, A-43, BT474, N87, and CaLu-3 cells
Concentration:1 nM-100 μM
Incubation Time:72 hours
Result:Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

Cell Cycle Analysis[1]

Cell Line:HN5 cells
Concentration:1 μM, or 10 μM
Incubation Time:72 hours
Result:Resulted in induction of G1 arrest.

Western Blot Analysis[1]

Cell Line:BT474 and HN5 cells
Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, or 10 μM
Incubation Time:6 hours
Result:Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.
体内研究
(In Vivo)

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) tosylate treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[1].

Animal Model:CD-1 nude female mice (4-6 weeks old) with HN5 cells[1]
Dosage:30 mg/kg, 100 mg/kg
Administration:Oral administration; twice daily; for 21 days
Result:Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.
Clinical Trial
分子量

753.26

Formula

C36H34ClFN4O7S2

CAS 号

1187538-35-7

中文名称

甲苯磺酸拉帕替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.