Lapatinib ditosylate - CAS:388082-78-8

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Lapatinib ditosylate (Synonyms:GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate)

目录号 : KM17972 CAS No. : 388082-78-8 纯度 : 98%

Data Sheet 产品使用指南

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

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500mg	询价	In-stock

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生物活性

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

体外研究

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) 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.
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines.
Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest.

Western Blot Analysis

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.

Cell Proliferation Assay

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

Cell Cycle Analysis

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

体内研究

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) 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.

Animal Model:	CD-1 nude female mice (4-6 weeks old) with HN5 cells
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.

分子式

C₂₉H₂₆ClFN₄O₄S

分子量

1868.94

CAS号

388082-78-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

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