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Lapatinib ditosylate monohydrate
CAS No. : 388082-78-8
MCE 国际站：Lapatinib ditosylate monohydrate
产品活性：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。
研究领域：JAK/STAT Signaling | Protein Tyrosine Kinase/RTK | Autophagy | Apoptosis
作用靶点：EGFR | Autophagy | Ferroptosis
In Vitro: 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.
In Vivo: 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.
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