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编 号：F062137
分子式：C36H34ClFN4O7S2
分子量：753.26
分子式：C36H34ClFN4O7S2
分子量：753.26
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CAS No: 1187538-35-7
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生物活性：
Lapatinib (GW572016) tosylate is a potent, orally active 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.
体内研究：
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.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.
体外研究：
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.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.Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest.
Lapatinib (GW572016) tosylate is a potent, orally active 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.
体内研究：
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.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.
体外研究：
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.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.Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest.
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