Lapatinib ditosylate二甲苯磺酸拉帕替尼,

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Lapatinib ditosylate

CAS No. : 388082-77-7

MCE 国际站：Lapatinib ditosylate

产品活性：Lapatinib ditosylate (GW572016 ditosylate) 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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