Lapatinib tosylate

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Lapatinib tosylate

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CAS NO:

1187538-35-7

GW572016 tosylate
GW2016 tosylate

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.